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RTK and Angiogenesis Related
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RTK and Angiogenesis
Related Products
Inhibitors
VEGFR
EGFR
PDGFR
Src
Bcr-Abl
c-Met
ALK
wtth
ow
Grro
G
t rs
cto
ac
Fa
F
HER2
IGF-1R
TGF-R
R
T
K
c-Kit
Flt
FGFR
HIF
VDA
Syk
JAK/STAT
Pathway
Tie-2
FAK
STAT
PAK
c-RET
PLC
c-Src
Pho
PKC
ROCK
JAK
PDK-1
ROCK
IKK
Akt
TGF
Pathway
c-Jun
Cell
Cycle
GSK-3
c-Fos
PI3K/Akt
Pathway
NF-kB
Pathway
JAK
Receptor Tyrosine Kinases and Angiogenesis
Receptor tyrosine kinases (RTKs) are an integral component of many signaling pathways
including growth factor receptors, Mast/stem cell growth factor receptors (c-Kit) and
numerous oncogenes. Examples of growth factor receptors include EGFR, ErbB2/HER2,
VEGFR, PDGFR, FGFR and IGF-1R. Others targets include Endothelin receptor type A (ETA
Receptor), Fms-like tyrosine kinase receptor-3 (Flt3) and kinases such as Spleen tyrosine
kinase (Syk), Tie2 kinase, and Anaplastic lymphoma kinase (ALK).
The main focus of recent research has been on growth factor receptors as a means to
suppress tumors. Especially, inhibitors of VEGFR, PDGFR and HER2 have been a primary
area of focus for tumor suppression. They include Cediranib (AZD2171), BIBW2992 (Tovok),
BIBF1120 (Vargatef), ABT-869 (Linifanib), Imatinib Mesylate, Lapatinib Ditosylate and
Sunitinib Malate (Sutent).
Angiogenesis is the physiological process entailing the growth of new blood vessels from
pre-existing vessels. Under certain conditions, angiogenesis can be induced from solid
tumors with oxygen and the nutrients needed. There are many important targets related to
angiogenesis including EGFR, HER2, VEGFR, PDGFR, FGFR, Flt3, HIF, ALK, VDA and S1P
receptors, and they are mainly RTKs.
Growth Factors
VEGFR
Vascular Endothelial Growth Factor Receptor
1~3
EGFR
Epidermal Growth Factor Receptor
3~4
PDGFR
Platelet-derived Growth Factor Receptor
5~6
Src
Proto-oncogene Tyrosine-protein Kinase Src
6~7
Bcr-Abl
7
c-Met
Hepatocyte Growth Factor Receptor
8
ALK
Anaplastic Lymphoma Kinase, CD246
9
HER2
Human Epidermal Growth Factor Receptor 2
9
IGF-1R
Insulin-like Growth Factor 1 Receptor
c-Kit
Proto-oncogene c-Kit, CD117
11~12
Flt
Fms-like Tyrosine Kinase
13~14
FGFR
Fibroblast Growth Factor Receptor
14
HIF
Hypoxia-inducible Factor
15
VDA
Vascular Disrupting Agent
15
Syk
Spleen Tyrosine Kinase
15
Tie-2
Angiopoietin Receptor
15
FAK
Focal Adhesion Kinase
16
c-RET
RET Proto-oncogene
16
JAK
Janus Kinase
17
10
S1P
EGFR,VEGFR,PDGFR,
HER-2,c-Kit,c-Met,IGF-1R
TGF-R
JAK/STAT
Pathway
ALK
Rho
PAK
G-protein
STAT
PLC
TGF
Pathway
c-Src
ROCK
Bcr-Abl
JAK
PDK-1
Cell
Cycle
Flt/KDR
S1PR
PKC
c-Jun
un
n
c-Fos
Ras
GSK-3
Akt
A
Raf
IKK
PI3K/Akt
Pathway
HIF
MAPK
Pathway
NF-kB
Pathway
NOS
mTOR
NO
Angiogenesis
VEGFR
VEGFR
VEGFR
S2161
RAF265
(CHIR-265)
An oral, highly selective Raf and VEGFR kinase
inhibitor. VEGFR, IC50=10 μM; Raf, IC50=5 μM.
S1084
Brivanib
(BMS-540215)
A VEGFR2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
VEGFR1, IC50=0.38 μM; VEGFR3, IC50=10 nM; FGFR1,
IC50=148 nM; FGFR2, IC50=125 nM; FGFR3, IC50=68 nM.
S1181
ENMD-2076
An antiangiogenic and Aurora kinase inhibitor. VEGFR2,
IC50=93 nM; KDR, IC50=40 nM; Flt3, IC50=3 nM; AurA, IC50=13 nM;
AurB, IC50=0.35 μM; Src, IC50=23 nM; FGFR1, IC50=0.12 μM.
S1486
AEE788
A novel multitargeted HER1/2 and VEGFR1/2 inhibitor. EGFR,
IC50= 2 nM; ErbB2, IC50=6 nM; KDR, IC50=77 nM; Flt1, IC50=59 nM.
S1361
MGCD-265
A multi-targeted kinase inhibitor, which targets the c-Met,
VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron.
S1164
E7080
An inhibitor of VEGFR3 (IC50=5.2 nM) and VEGFR2 (IC50=4.0 nM).
S1220
OSI-930
An inhibitor of c-Kit (IC50=9.5nM) and VEGFR2 (IC50=10.1nM).
S1171
CYC116
A VEGFR2, Aurora kinase A and B inhibitor.
S1470
TSU-68
(SU6668)
A novel multiple receptor tyrosine kinase inhibitor. VEGFR1,
IC50=2.1 μM; , IC50=8 nM; FGFR1, IC50=1.2 μM.
pFRS2
A potent ATP-competitive, reversible FGFR and VEGFR
inhibitor. FGFR3, IC50=5 nM; FGFR1, IC50=21.5 nM; VEGFR2,
IC50 of ~100 nM; PDGFR, IC50=17.6 μM; c-Src, IC50=19.8 μM.
pERK1/2
Vascular Endothelial Growth Factor Receptor
VEGFR Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S1017
Cediranib
(AZD2171)
A VEGFR2 inhibitor. It inhibits VEGF-stimulated
proliferation and KDR phosphorylation with IC50s of
0.4 nM and 0.5 nM, respectively.
BIBF1120
(Vargatef)
An inhibitor of VEGFR, PDGFR and FGFR. VEGFR,
IC50=13-34 nM; PDGFRa, IC50=59 nM; PDGFRh,
IC50=65 nM; FGFR1, IC50=69 nM; FGFR2, IC50=37 nM;
FGFR3, IC50=108 nM.
Foretinib
(GSK1363089,
XL880)
A novel Met and VEGFR2/KDR kinase inhibitor. KDR,
IC50=0.8 nM; Met, IC50=0.4 nM; Ron, IC50=3 nM; Flt1,
IC50=6.8 nM; Flt4, IC50=2.8 nM.
Axitinib
A VEGFR2 and VEGFR3 phosphorylation inhibitor.
VEGFR2, IC50=0.2 nM; VEGFR3, IC50=0.1 to 0.3 nM.
S1010
S1111
S1005
S2769
S1003
S1490
Dovitinib
dilactic acid
(TKI258 dilactic acid)
A multitargeted tyrosine kinase inhibitor of Flt3 and
c-Kit. Flt3, IC50=1 nM; c-Kit, IC50=2 nM.
Linifanib
(ABT-869)
A structurally novel, potent RTK, VEGFR and PDGFR
inhibitor. , IC50=2 nM; KDR, IC50=4 nM;
CSF-1R, IC50=7 nM.
Ponatinib
(AP24534)
VEGFR2, IC50=1.5 nM; pan-Bcr-Abl, IC50=0.37 nM;
mutant Bcr-Abl, IC50=2 nM; FGFR1, IC50=2.2 nM;
, IC50=1.1 nM; mutant Flt3 phosphorylation,
IC50=1 nM; Lyn, IC50=0.24 nM; Src, IC50=5.4 nM.
S1119
XL184 free base
(Cabozantinib)
VEGFR2, IC50=0.035 nM; Met, IC50=1.8 nM; Flt3,
IC50=14.4 nM; Tie-2, IC50=14.3 nM; Kit, IC50=4.6 nM;
RET.
S1032
Motesanib
diphosphate
(AMG-706)
A multiple inhibitor of VEGFR1/2/3, PDGFR, Kit and
RET receptors. VEGFR1, IC50=2 nM; VEGFR2,
IC50=3 nM; VEGFR3, IC50=6 nM; PDGFR, IC50=84 nM;
Kit, IC50=8 nM; RET, IC50=59 nM.
S1178
S1207
S1101
S1489
Regorafenib
(BAY 73-4506)
Tivozanib
(AV-951)
Inhibitor
Data from [Nature, 2011, 478(7369), 349-355]
BIBF1120 (Vargatef) purchased from Selleck
immunostaining of insulin and BrdU, in 3 week- and
12 month-old WT islets exposed to PDGF-AA
!"#!"$#%&'
*&'!+
S1363
A multikinase inhibitor. VEGFR2, IC50=40 nM; c-Kit,
IC50=17 nM; B-Raf, IC50=69 nM; VEGFR3; RET;
PDGFR.
An orally bioavailable inhibitor. VEGFR1, IC50=0.21
nM; VEGFR2, IC50=0.16 nM; VEGFR3, IC50=0.24 nM;
c-Kit, IC50=1.63 nM; PDGFR, IC50=1.72 nM.
Vatalanib
dihydrochloride
(PTK787)
A novel VEGFR and c-Kit tyrosine kinase and
angiogenesis inhibitor. c-Kit, IC50=0.73 μM; KDR,
IC50=37 nM; Flt1, IC50=77 nM; Flk, IC50=0.27 μM.
PIK-93
A inhibitor with an IC50 of 19 nM. ,
IC50=16 nM; , IC50=39 nM; , IC50=0.59 μM;
, IC50=0.12 μM.
Vehicle
S1264
Data from [Haematologica, 2011, 96(6), 922-926]
Dovitinib Dilactic acid (TKI258 dilactic acid)
purchased from Selleck
In vitro assays on CUX1-FGFR1-expressing
Ba/F3 cells. c. Western blot analyses of
CUX1-FGFR1-transformed Ba/F3 cells after
treatment with PKC412 and TKI258.
Phosphorylation of CUX1-FGFR1 and its
downstream effectors STAT5 and RPS6K
decreased with increasing inhibitor concentrations.
Expression of total CUX1-FGFR1, STAT5 and
RPS6K remained unaffected.
Data from [Circ Res, 2011, 108(10), 1190-1198]
Vatalanib dihydrochloride (PTK787) purchased
from Selleck
Mechanisms of VEGF-activated Ca2+ entry.
All data were from HUVECs. a, Mean 100 ng/mL
VEGF-evoked Ca2+ entry in the presence of
100 nmol/L sorafenib (n/N=3/40), 10 nmol/L
<>?@%QX&
Y\^@X%%
(n/N=3/24) normalized to their matched controls.
e, Example merged image of a cell labeled
with anti-VEGFR2 antibody (green), anti-Orai1
antibody (red), and the nuclear counter stain,
DAPI (blue).
Terrific Validation, Tech Support & Prompt Delivery
Data independently produced by Dr. Antonino Maria
Sparta, University of Trento
ENMD-2076 purchased from Selleck
Neurospheres were obtained growing CHP-134 cells
in a selective medium (DMEMF12, B27, EGF, bFGF,
L-Glut). The cells were grown in 96-well plates to
confluence and treated with ENMD-2076 for 24 h.
The toxic effect was measured by a WST-1
chromogenic assay. It appears that the bulk cell line
is more sensitive to treatment that the neurospheres.
PD173074
Ki8751
A potent and selective VEGFR2 tyrosine kinase inhibitor with
IC50 of 0.9 nM. c-Kit, IC50=40 nM; , IC50=67 nM;
FGFR2, IC50=170 nM.
S2202
NVP-BHG712
VEGFR2, ED50=4.2 μM; EphB4, ED50=25 nM; c-Raf,
ED50=0.4 μM; c-Src, ED50=1.3 μM; c-Abl, ED50=1.7 μM.
S1557
KRN 633
A cell-permeable, reversible and ATP-competitive VEGFR
kinase inhibitor. VEGFR1, IC50=170 nM; VEGFR2, IC50=160
nM; VEGFR3, IC50=125 nM; , IC50=0.97 μM; c-Kit,
IC50=4.33 μM.
S2201
BMS 794833
A potent ATP-competitive Met/VEGFR2 kinase inhibitor.
It also inhibits Ron, Axl and Flt3 with IC50 of <3 nM.
S1138
Brivanib
alaninate
(BMS-582664)
A multiple inhibitor of VEGFR and FGFR. VEGFR2, IC50 of 25 nM
and Ki of 26 nM; VEGFR1, IC50=380 nM; VEGFR3, IC50=10 nM;
FGFR1, IC50=148 nM; FGFR2, IC50=125 nM; FGFR3, IC50=68 nM.
S2231
Telatinib
(BAY 57-9352)
An orally available, potent multitargeted VEGFR2, VEGFR3,
and c-Kit inhibitor with an IC50 of 19 nM for the
inhibition of VEGFR2 autophosphorylation.
S2200
Raf265
derivative
A derivative of Raf265, which is an oral highly selective Raf
and VEGFR kinase inhibitor with IC50sX&'+j#
the effects of this derivative are not known.
S1035
Pazopanib HCl
A VEGFR inhibitor with IC50s of 10 nM, 30 nM and 47 nM for
VEGFR1, 2 and 3.
S1040
Sorafenib
(Nexavar)
A novel and small molecular inhibitor of several tyrosine
protein kinases (VEGFR and PDGFR) and Raf/MEK/ERK
cascade. Raf-1, IC50=6 nM; wt B-Raf, IC50=22 nM; V599E
mutant B-Raf, IC50=38 nM.
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
FGFR inhibitor
Ki67
Hand2 d/d
Data from [Science, 2011, 331(6019), 912-916]
PD173074 purchased from Selleck
The FGFR-specific inhibitor PD173074 was
administered to one uterine horn of Hand2d/d mice
on day 3 of pregnancy (n = 5). The other horn served
as vehicle-treated control. Uterine horns were
collected on the morning of day 4, and sections were
subjected to IHC to detect p-FRS2, p-ERK1/2, and
Ki-67.
c-Met
p-c-Met
0
0.001 0.01
0.1
1
5
μM
Data independently produced by Dr. Zhang of Tianjin
Medical University
MGCD-265 purchased from Selleck
{''+&'
MGCD265 was added.
[email protected]
EGFR
VEGFR/EGFR
S1042
Sunitinib malate A multitargeted Flt3, PDGFR, VEGFR and Kit kinase inhibitor
(Sutent)
with Kis of 9nM and 8 nM for Flk-1 and PDGFR.
S2406
Chrysophanic acid An EGFR/mTOR pathway inhibitor.
(Chrysophanol)
S1046
Vandetanib
(Zactima)
A VEGFR and EGFR antagonist and a tyrosine kinase inhibitor
with IC50s of 60 nM, 90 nM, 40 nM for HUVEC proliferation,
PC-9 cells and tyrosine kinase activity, respectively.
S1083
XL647
An EGFR and ErbB2 inhibitor with IC50s of 0.3 nM and
16 nM, respectively.
Apatinib
(YN968D1)
A small-molecule selective multitargeted tyrosine kinase
inhibitor with an IC50 of 2.43 nM for the inhibition of VEGFR2.
S2727
PF299804
A potent, orally available, irreversible tyrosine kinase
HER1 (EGFR), HER2 and HER4 inhibitor. EGFR,
IC50=6 nM; ErbB2, IC50=45.7 nM; ErbB4, IC50=73.7 nM.
S2733
AV-412
A second-generation and orally bioavailable dual
EGFR/HER2 tyrosine kinase inhibitor.
S2221
S2475
S1035
Imatinib
(Gleevec)
Pazopanib HCl
EGFR
A number of tyrosine kinase enzymes specific inhibitor.
A novel multitargeted VEGFR1, VEGFR2, VEGFR3, PDGFR,
FGFR, c-Kit and c-Fms inhibitor with IC50s of 10 nM, 30 nM,
47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Data independently produced by Dr. Zhang of
Tianjin Medical University
CYC116 purchased from Selleck
Breast cancer cells line MDA-MB-231 was
treated with the indicated concentrations of
CYC116.
Epidermal Growth Factor Receptor
S2728 NEW AG-1478
(Tyrphostin
AG-1478)
A highly potent and specific EGFR tyrosine kinase
inhibitor with an IC50 of 3 nM.
S1023
Erlotinib HCl
An HER1/EGFR with an IC50 of 2 nM.
S1025
Gefitinib (Iressa)
A novel potent EGFR tyrosine kinase and Akt
phosphorylation inhibitor with IC50s of 37 nM, 26 nM and
57 nM for Tyr1173, Tyr1173 and Tyr992, respectively,
the low and high EGFR expressing cell lines.
EGFR Inhibitors
Data from [Antiviral Res, 2011, 89(1), 64-70]
PD153035 HCl purchased from Selleck
Inhibition of orthopoxvirus replication and spreading
correlates with blocking of EGFR signaling by
PD153035 (PD), Vandetanib (Van) and Gefitinib (Gef).
Western blot of cell lysates obtained from VACV
plaque reduction tests for analysis of EGFR-ERK1/2
signaling and VACV proteins. As an indicative band
for VACV a 30KDa protein was depicted from
detection of total VACV proteins by a polyclonal
antibody in cell lysates of infected Hep2 cells.
EGF
-
+
+
+
+
+
+
0
0
0.001
0.01
0.1
1
10
p-Akt -308
Cat.No.
Product Name
Target and IC50 Value
BIBW2992
(Afatinib)
An irreversible EGFR/HER2 inhibitor with an IC50 of 14
nM for in vitro potency against HER2.
S1170
WZ3146
An irreversiblely inhibitor against EGFR T790M.
S1173
WZ4002
An EGFR T790M inhibitor with an IC50 of <20nM.
S1194
CUDC-101
A potent multitargeted inhibitor. EGFR, IC50=2.4 nM;
HDAC, IC50=4.4 nM; HER2, IC50=15.7 nM.
S1011
S1028
Lapatinib ditosylate An EGFR and HER2 autophosphorylation inhibitor, with
(Tykerb)
IC50 values against purified EGFR and HER2 of 10.2nM
S1046
Vandetanib
(Zactima)
A VEGFR and EGFR antagonist and a tyrosine kinase
inhibitor with IC50s of 60 nM, 90 nM and 40 nM for
HUVEC proliferation, PC-9 cells and tyrosine kinase
activity, respectively.
S2111
Lapatinib
A potent purified EGFR and ErbB2 inhibitor with IC50s of
10.2 nM and 9.8 nM, respectively.
S2205
OSI-420 (Desmethyl
Erlotinib, CP-473420)
An orally active EGFR tyrosin kinase inhibitor with IC50s
of 2 nM and 20 nM for the inhibition of human EGFR
and EGFR autophosphorylation in tumor cells.
S2185
AST-1306
A novel irreversible epidermal growth factor receptor
inhibitor of EGFR and ErbB4 with IC50s of 0.5 nM and
0.8 nM, respectively.
S2755
ARRY334543
A selective and potent kinase ErbB1 and ErbB2
inhibitor with IC50s of 7 nM and 2 nM, respectively.
and 9.8 nM, respectively.
P-EGFR
EGFR
S1392
Pelitinib
(EKB-569)
A 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor
with potential antineoplastic activity.
S1079
PD153035 HCl
An inhibitor of EGFR, competitive with ATP. EGFR,
IC50=25 pM, Ki=6 pM.
S1019
CI-1033
(Canertinib)
A potent tyrosine kinase inhibitor of EGFR and ErbB2
with IC50s of 1.5 nM and 9.0 nM, respectively.
S1486
AEE788
A novel multitargeted HER1/2 and VEGFR1/2 inhibitor.
EGFR, IC50=2 nM; ErbB2, IC50=6 nM; KDR, IC50=77 nM;
Flt1, IC50=59 nM.
S1143
AG-490
A potent EGFR kinase autophosphorylation inhibitor.
EGFR, IC50=100 nM; JAK, IC50=56.8 μM.
S1056
BMS-599626
(AC480)
A highly selective pan-HER kinase inhibitor. HER1,
IC50=20 nM; HER2, IC50=30 nM.
S2192
AZD8931
A novel potent reversible small molecule inhibitor. EGFR,
IC50=4 nM; ErbB2, IC50=3 nM; ErbB3, IC50=4 nM.
S1179
WZ8040
An irreversiblely EGFR T790M inhibitor with an
IC50 of <10 nM.
EGF(100ng/ml)
+
+
+
+
+
-
WZ3146(μM)
0
0.1
1
10
20
0
Data independently produced by Dr. Zhang of Tianjin
Medical University
WZ3146 purchased from Selleck
T47D cells were pretreated with 100ng/ml EGF for
20 min and then treated with the indicated
concentrations of WZ3146 for 24 hours.
Akt
Data independently produced by Dr. Zhang of
Tianjin Medical University
Chrysophanic acid (Chrysophanol) purchased
from Selleck
A549 cells were serum starved for 24 h, pretreated
with the indicated concentrations of Chrysophanic
acid for 3h and then treated with 100 ng/mL EGF
for 15 min.
Data from [J Cell Sci, 2010,123, 3102-3111]
CI-1033(Canertinib) purchased from Selleck
Effect of pan-ErbB inhibitors on NRG-1 action on
human melanocytes and MelanoDerms.
(A) HEM-DP were treated for 9 days with 50 ng/ml
>X"@+&'X@@
%&'<"'$+"#
the average of three independent experiments±s.d.
(B) Dark (from African-American skin)
MelanoDerms were treated for 9 days with 50 ng/ml
NRG-1 in the presence of @+&'X@@
%&'<" (DMSO) alone. L values shown
are the average of three spots measured in the
center of each MelanoDerm.
Terrific Validation, Tech Support & Prompt Delivery
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
[email protected]
PDGFR/Src
PDGFR
PDGFR
Platelet-derived Growth Factor Receptor
S2622
PP-121
PDGFR Inhibitors
Cat.No.
Product Name
Target and IC50 Value
Inhibitor
S1010
BIBF1120
(Vargatef)
An inhibitor of VEGFR, PDGFR and FGFR. VEGFR,
IC50=13-34 nM; PDGFRa, IC50=59 nM; PDGFRh,
IC50=65 nM; FGFR1, IC50=69 nM; FGFR2, IC50=37 nM;
FGFR3, IC50=108 nM.
Ponatinib
(AP24534)
VEGFR2, IC50=1.5 nM; pan-Bcr-Abl, IC50=0.37 nM;
mutant Bcr-Abl, IC50=2 nM; FGFR1, IC50=2.2 nM;
, IC50=1.1 nM; mutant Flt3 phosphorylation,
IC50=1 nM; Lyn, IC50=0.24 nM; Src, IC50=5.4 nM.
S1026
Imatinib mesylate
A multitargeted c-Kit, PDGFR and c-Abl inhibitor with
IC50@+&'%+&'""
proliferation stimulated by DCs and PHA.
S2769
A multitargeted tyrosine kinase inhibitor of Flt3 and
Dovitinib
dilactic acid
c-Kit. Flt3, IC50=1 nM; c-Kit, IC50=2 nM.
(TKI258 dilactic acid)
S1032
Motesanib
diphosphate
(AMG-706)
A multiple inhibitor of VEGFR1/2/3, PDGFR, Kit and
RET receptors. VEGFR1, IC50=2 nM; VEGFR2, IC50=3 nM;
VEGFR3, IC50=6 nM; PDGFR, IC50=84 nM; Kit, IC50=8 nM;
RET, IC50=59 nM.
S1064
Masitinib
A tyrosine kinase c-Kit, PDGFR, FGFR3 and FAK
inhibitor with IC50 of 150 ± 80 nM, 200 ± 40 nM for Kit
tyrosine phosphorylation and the recombinant human
wild-type Kit.
S1207
Tivozanib
(AV-951)
An orally bioavailable inhibitor. VEGFR1, IC50=0.21 nM;
VEGFR2, IC50=0.16 nM; VEGFR3, IC50=0.24 nM; c-Kit,
IC50=1.63 nM; PDGFR, IC50=1.72 nM.
S1490
S1005
Axitinib
A VEGFR2 and VEGFR3 phosphorylation inhibitor.
VEGFR2, IC50=0.2 nM; VEGFR3, IC50=0.1 to 0.3 nM.
S1003
Linifanib
(ABT-869)
A structurally novel, potent RTK, VEGFR and PDGFR
inhibitor. , IC50=2 nM; KDR, IC50=4 nM;
CSF-1R, IC50=7 nM.
S1244
MP-470
A multi-targeted tyrosine kinase inhibitor with potent activity
against mutant c-Met, c-Kit, , Flt3 and c-RET.
S1470
TSU-68
(SU6668)
S1363
S1557
S2231
Data from [Nature, 2011, 478, 349-355]
BIBF1120(Vargatef) purchased from Selleck
Real-time RT-PCR analyses of mRNAs encoding
Ezh2 and Ezh1 from 3 week-old WT islets 2 days
after exposure to PDGF-AA alone, or PDGF-AA
plus RTK inhibitors Sunitinib or Vargatef at the
indicated concentrations.
Data from [Br J Cancer, 2011, 104(1), 75-82]
Dovitinib Dilactic acid (TKI258 dilactic acid)
purchased from Selleck
RT112 cells were exposed to PD173074 (PD)
(500 nM) for 0-24 h, TKI-258 (TK) (500 nM) or
SU5402 (SU) (5 mM) for 1 h. Cells were lysed,
FGFR3 was immunoprecipitated
(immunoprecipitated, IP) and blots (immunoblot, IB)
were probed for phospho-tyrosine and reprobed for
FGFR3 or probed for phospho-ERK and reprobed
for total ERK.
A multitargeted dual receptor tyrosine kinase inhibitor.
mTOR, IC50=10 nM; , IC50=52 nM; , IC50=1.4
μM; , IC50=0.15 μM; , IC50=1.1 μM; DNA-PK,
IC50=60 nM; PDGFR, IC50=2 nM; Abl, IC50=18 nM; Hck,
IC50=8 nM; Src, IC50=14 nM; Src (T338I), IC50=0.22 μM;
VEGFR2, IC50=12 nM; EGFR, IC50=0.26 μM; EphB4,
IC50=0.19 μM.
S2730
Crenolanib
(CP-868569)
A highly selective and potent inhibitor with IC50s
of 0.9 nM and 1.8 nM against and ,
respectively.
S1035
Pazopanib HCl
A VEGFR inhibitor with IC50s of 10 nM, 30 nM and 47 nM
for VEGFR1, 2 and 3.
S1040
Sorafenib
(Nexavar)
A novel, small molecular inhibitor of several tyrosine
protein kinases (VEGFR and PDGFR) and Raf/MEK/ERK
cascade. Raf-1, IC50=6 nM; wt BRAF, IC50=22 nM; V599E
mutant B-Raf, IC50=38 nM.
S1042
Sunitinib malate
(Sutent)
A multitargeted Flt3, PDGFR, VEGFR and Kit kinase
inhibitor with Kis of 9 nM and 8 nM for Flk-1 and PDGFR.
S2774
MK-2461
A potent inhibitor of c-Met, Ron, Flt1, Flt3, , and
Mer with IC50s of 2.5 nM, 7 nM, 10 nM, 22 nM, 22 nM and
24 nM, respectively.
S2475
Imatinib
A multi-target inhibitor of v-Abl, c-Kit and PDGFR
with IC50+&'+X&'+X&'<+
Src
Proto-oncogene Tyrosine-protein Kinase Src
Src Inhibitors
Cat.No. Product Name
Target and IC50 Value
S1006
Saracatinib
(AZD0530)
An orally available, dual-specific Src/Abl kinase
inhibitor. c-Src, IC50=2.7 nM; Abl kinase, IC50=30 nM.
S1014
Bosutinib
(SKI-606)
An Src family kinase inhibitor. Inhibited migration of
breast cancer cell lines with IC50s of 0.1 to 0.3 μM.
A novel multiple receptor tyrosine kinase inhibitor.
VEGFR1, IC50=2.1 μM; , IC50=8 nM; FGFR1,
IC50=1.2 μM.
S1107
Danusertib
(PHA-739358)
A pyrrolo-pyrazole and small molecule Aurora kinase
and Bcr-Abl kinase inhibitor. Aurora A, IC50=13 nM;
Aurora B, IC50=79 nM; Aurora C, IC50=61 nM.
Ki8751
A potent, selective VEGFR2 tyrosine kinase inhibitor with
IC50 of 0.9 nM. c-Kit, IC50=40 nM; , IC50=67 nM;
FGFR2, IC50=170 nM.
S2202
NVP-BHG712
c-Src, ED50=1.3 μM; EphB4, ED50=25 nM; c-Raf, ED50=0.4
μM; c-Abl, ED50=1.7 μM; VEGFR2, ED50=4.2 μM.
KRN 633
A cell-permeable, reversible, ATP-competitive VEGFR
kinase inhibitor. VEGFR1, IC50=170 nM; VEGFR2,
IC50=160 nM; VEGFR3, IC50=125 nM; ,
IC50=0.97 μM; c-Kit, IC50=4.33 μM.
S2391
Quercetin
(Sophoretin)
A PI3K and PKC inhibitor with IC50s@+&'
49.6 μM.
S2680
PCI-32765
A high potent irreversible BTK inhibitor with an IC50 of
0.46 nM.
Telatinib
(BAY 57-9352)
Data independently produced by Dr. Zhang of
Tianjin Medical University
Linifanib (ABT-869) purchased from Selleck
T47D breast cancer cells were pretreated with
indicated concentrations of ABT-869.
An orally available, potent multitargeted VEGFR2, VEGFR3,
and c-Kit inhibitor with an IC50 of 19 nM for the
inhibition of VEGFR2 autophosphorylation.
Terrific Validation, Tech Support & Prompt Delivery
Data independently produced by Dr. Cheri Pasch of
UW Madison
Axitinib purchased from Selleck
Axitinib treatment blocks VEGFR2 phosphorylation.
HUVECs were starved O/N in EBM-2 basal medium
with 1% FBS and antibiotic. Cells were pre-treated
with Axitinib at 0.1, 1 and 10 nM concentrations.
VEGF stimulation was 50 ng/mL for 10 min before
cells were collected and protein isolated for
immunoprecipitation with VEGFR2 followed by
immunoblotting with VEGFR-2 and phospho-VEGFR-2.
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
Data from [Mol Endocrinol, 2010 , 24(6),
1151-1164]
Saracatinib (AZD0530) purchased from Selleck
Effect of a c-Src inhibitor on tyrosine
phosphorylation of VDR in the plasma membrane.
Primary human hepatocytes were treated with Veh,
X%%@
YX&
"$"@&
for 6 h. Cell extract (10%) was set aside as input.
[email protected]
Src/Bcr-Abl
c-Met
S2700
KX2-391
An orally bioavailable, small molecule and non-ATP competitive Src inhibitor with an
average IC50 of 72 nM.
c-Met
S1021
Dasatinib
(BMS-354825)
This ATP-competitive, dual Src/Abl inhibitor inhibits all members of the Src family,
including c-Src, Lck, Fyn and Yes (IC50<1.1 nM).
c-Met Inhibitors
S1213
Nelarabine
(Arranon)
It performes growth inhibitory activity (IC50=1.61 μM) against MOLT-4 cells.
S1225
Etoposide (VP-16)
A topoisomerase II inhibitor (IC50?+%&'+
Hepatocyte Growth Factor Receptor
Cat.No.
Product Name
S1068
PF-2341066
(Crizotinib)
An inhibitor of the c-Met kinase and the
NPM-ALK. It inhibited cell proliferation in
ALK-positive ALCL cells with an IC50 of 30 nM.
Foretinib
(GSK1363089, XL880)
A novel Met and VEGFR2/KDR kinase inhibitor.
KDR, IC50=0.8 nM; Met, IC50=0.4 nM; Ron,
IC50=3 nM; Flt1, IC50=6.8 nM; Flt4, IC50=2.8 nM.
S1111
Bcr-Abl
Target and IC50 Value
Bcr-Abl Inhibitors
S1112
SGX-523
An ATP-competitive Met inhibitor with an IC50 of
4 nM for the inhibition of HGFR.
S1119
XL184 free base
(Cabozantinib)
VEGFR2, IC50=0.035 nM; Met, IC50=1.8 nM;
Flt3, IC50=14.4 nM; Tie-2, IC50=14.3 nM; Kit,
IC50=4.6 nM; RET.
Product Name
Target and IC50 Value
S1006
Saracatinib
(AZD0530)
An orally available, dual-specific Src/Abl kinase
inhibitor. c-Src, IC50=2.7 nM; Abl kinase, IC50=30 nM.
S1107
Danusertib
(PHA-739358)
A pyrrolo-pyrazole and small molecule Aurora kinase
and Bcr-Abl kinase inhibitor. Aurora A, IC50=13 nM;
Aurora B, IC50=79 nM; Aurora C, IC50=61 nM.
S1114
JNJ-38877605
A c-Met inhibitor with an IC50 of 4 nM.
S1094
PF-04217903
An Met inhibitor with IC50s from 3.1 to142 nM.
Ponatinib
(AP24534)
Pan-Bcr-Abl, IC50=0.37 nM; mutant Bcr-Abl, IC50=2 nM;
VEGFR2, IC50=1.5 nM; FGFR1, IC50=2.2 nM; PDGFR
, IC50=1.1 nM; mutant Flt3 phosphorylation,
IC50=1 nM; Lyn, IC50=0.24 nM; Src, IC50=5.4 nM.
S1244
MP-470
A multi-targeted tyrosine kinase inhibitor with
potent activity against mutant c-Met, c-Kit,
, Flt3 and c-RET.
S1361
MGCD-265
AT9283
A multi-targeted c-Abl, JAK2, Aurora A and B inhibitor.
Bcr-Abl (T3151), IC50=4 nM; JAK2, IC50=1.2 nM; JAK3,
IC50=1.1 nM; Aurora A and B, IC50s of approximate 3 nM.
A multi-targeted kinase inhibitor, which targets
the c-Met, VEGFR1, VEGFR2, VEGFR3, Tie-2
and Ron.
S1561
BMS 777607
A small-molecule Met kinase Inhibitor with an
IC50+X&'+
S2243
WP1130
A novel selective small molecular deubiquitinase
inhibitor and a Bcr/Abl destruction pathway activator
with an IC50X+&'%+
Data from [Mol Endocrinol, 2010 , 24(6),1151-1164]
Saracatinib (AZD0530) purchased from Selleck
Q-RT PCR assay of the effects of a c-Src inhibitor on
CYP7A1 (left panel) and CYP24A1 (right panel)
mRNA expression in primary human hepatocytes
from different liver donors (HH1479, HH1483, and
HH1493). Primary human hepatocytes were treated
!"*"X%2-D3
YX&
m) &
X "+ $
significant difference (P < 0.05; n = 3), AZD-treated
<+ <" X%2-D3 (50
nm) or Y X &
<+ X
%%@ Y X &
+
Statistically significant difference (P < 0.05; n = 3), 1
%2-D3
YX&
vs. vehicle control.
S1316
AMG-208
A potent small molecular c-Met inhibitor with an
IC50 of 9.3 nM.
S2201
BMS 794833
A potent ATP-competitive Met/VEGFR2 kinase
inhibitor. It also inhibits Ron, Axl and Flt3 with
IC50s of <3 nM.
KW 2449
A multi-kinase inhibitor of Flt3 (IC50 at 6.6 pM), Abl
(IC50 at 14 pM), Abl-T315I and Aurora kinase.
S1369
Bafetinib
(INNO-406)
An orally available, dual Abl/Lyn kinase inhibitor (cell
IC50s of 11 ~ 22 nM).
S1070
PHA-665752
A c-Met inhibitor with an IC50 of 9 nM and a Ki of 4 nM.
S2202
NVP-BHG712
C-Src, ED50=1.3 μM; c-Abl, ED50=1.7 μM; VEGFR2,
ED50=4.2 μM; EphB4, ED50=25 nM; c-Raf, ED50=0.4 μM.
S2747 NEW
AMG458
S2634
DCC-2036
An Abl switch control inhibitor. u-Abl1 native,
IC50=0.8 nM; p-Abl1 native, IC50=2 nM.
A potent selective c-Met inhibitor of human c-Met
and mouse c-Met with Kis of 1.2 nM and 2 nM,
respectively.
S2774
MK-2461
S1021
Dasatinib
(BMS-354825)
The ATP-competitive, dual Src/Abl inhibitor inhibits all
members of the Src family, including c-Src, Lck, Fyn
and Yes (IC50<1.1 nM).
A potent inhibitor of c-Met, Ron, Flt1, Flt3,
, and Mer with IC50s of 2.5 nM, 7 nM,
10 nM, 22 nM, 22 nM and 24 nM, respectively.
S2753
ARQ 197
A novel and selective human c-Met receptor
tyrosine kinase inhibitor with a minimum IC50 of
+X&'+
S2761
NVP-BVU972
A selective and potent inhibitor of Met kinase
with an IC50 of 14 nM.
S1033
Nilotinib (AMN-107)
An inhibitor of Bcr-Abl with IC50 of <30 nM.
S5002
FTY720
(Fingolimod)
An Src-Bcr-Abl Inhibitor and S1P receptor agonist
with IC50s of 0.137 nM, 10.98 nM for (S)- and
(R)- FTY720-phosphate.
S1026
Imatinib mesylate
A mesylate salt of Imatinib which is a multi-target
inhibitor of v-Abl, c-Kit and PDGFR with IC50s of
+&'+X&'+X&'<+
Data independently produced by Dr. Claude Haan
and Catherine Rolvering of Universite du
Luxembourg
AT9283 purchased from Selleck
HEL cells were treated for 3 h with the indicated
concentrations of AT9283. AT9283 inhibited
Jak2-V617F mediated signal transduction at
submicromolar concentrations in intact cells.
Terrific Validation, Tech Support & Prompt Delivery
Data independently produced by Dr. Zhang of
Tianjin Medical University
SU11274 purchased from Selleck
Western blot analysis of c-Met, MAPK and Akt.
%&'$\XX^%Q!+
FGF
BMS777607 (μM) 0
+
+
+
+ +
0 0.001 0.01 0.1 1
+ +
10 100
ERK1/2
p-ERK1/2
Data independently produced by Dr. Zhang of
Tianjin Medical University
BMS 777607 purchased from Selleck
T47D cells were serum starved for 24 h,
pretreated with the indicated concentrations of
BMS 777607 for 3 h, and then treated with
100 ng/mL EGF for 20 min.
p-c-Met
S2158
MAPK
P-Akt
A c-Met inhibitor with an IC50 of 12 nM.
Cat.No.
S1134
cMET
p-MAPK
Akt
SU11274
S1080
S1490
Breast Cancer Cell line MDA-MB-231
p-cMET
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
c-Met
HGF (100 ng/mL) +
+
+
+
+
-
PHA665752 (nM) 0
12.5
25
50
100
0
Data independently produced by Dr. Zhang of
Tianjin Medical University
PHA-665752 purchased from Selleck
Western blot analysis of p-c-Met and c-Met.
X&'^%!+
[email protected]
ALK/HER2
ALK
IGF-1R
IGF-1R
Anaplastic Lymphoma Kinase, CD246
ALK Inhibitors
Cat.No.
IGF-1R Inhibitors
Product Name
Target and IC50 Value
S1068
PF-2341066
(Crizotinib)
An inhibitor of the c-Met kinase and the NPM-ALK.
ALK. It
inhibited cell proliferation in ALK-positive ALCL cells
with an IC50 of 30 nM.
S1108
TAE684
(NVP-TAE684)
An ALK inhibitor with IC50s between 2 nM and 10 nM.
S2703
GSK1838705A
ALK, IC50=0.5 nM; the insulin receptor, IC50=1.6
1.6 nM;
IGF-IR, IC50=2.0 nM.
S2762
CH5424802
A potent and selective ALK inhibitor with an IC
C50 of
1.9 nM.
HER2
Cat.No.
We give free samples and
rewards to people who would
like to provide us useful scientific
data (western blot, etc.)
Human Epidermal Growth Factor Receptor 2
HER2 Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S1011
BIBW2992
(Afatinib)
An irreversible EGFR/HER2 inhibitor with an IC50
of 14 nM for in vitro potency against HER2.
S1019
CI-1033
(Canertinib)
A potent tyrosine kinase inhibitor of EGFR and
ErbB2 with IC50s of 1.5 nM and 9.0 nM,
respectively.
S1167
CP-724714
An orally available, small molecule, potent HER2
tyrosine kinase inhibitor. It inhibits HER2-chimera
phosphorylation with an IC50 of 32 nM,
S2150
Neratinib
(HKI-272)
An orally available, irreversible tyrosine kinase
inhibitor. HER2, IC50=59 nM; EGFR, IC50=92 nM.
S1194
CUDC-101
A potent multitargeted inhibitor. HER2, IC50=15.7 nM;
EGFR, IC50=2.4 nM; HDAC, IC50=4.4 nM.
S1056
BMS-599626
(AC480)
A highly selective pan-HER kinase inhibitor. HER1,
IC50=20 nM; HER2, IC50=30 nM.
S2192
AZD8931
A novel potent reversible small molecule inhibitor.
EGFR, IC50=4 nM; ErbB2, IC50=3 nM; ErbB3,
IC50=4 nM.
S2733 NEW
AV-412
A second-generation, orally bioavailable dual
EGFR/HER2 tyrosine kinase inhibitor.
S2752 NEW
Arry-380
An orally bioavailable, potent, selective,
small-molecule tyrosine kinase HER2 inhibitor with
an IC50 of 8 nM.
S1028
Lapatinib ditosylate
(Tykerb)
An EGFR and HER2 autophosphorylation inhibitor,
with IC50 values against purified EGFR and HER2
of 10.2 and 9.8 nM, respectively.
S2216
Mubritinib
A potent inhibitor of ErbB2 with an IC50 of 6 nM.
Insulin-like Growth Factor 1 Receptor
Product Name
Target and IC50 Value
S1093
GSK1904529A
An inhibitor of IGF-1R (IC50=27 nM) and IR (IC50=25 nM).
S1012
BMS-536924
A small molecule ATP-competitive IGF-1R kinase
inhibitor with an IC50 of 80 nM.
S1034
NVP-AEW541
An IGF-1R inhibitor with a median IC50@+&'+
S1088
NVP-ADW742
An IGF-1R inhibitor with an IC50+X+%&'+
S1091
OSI-906
An IGF-1R inhibitor (EC50<400 nM).
S2703
GSK1838705A
IGF-1R, IC50=2.0 nM; the insulin receptor, IC50=1.6 nM;
ALK, IC50=0.5 nM.
S1086
BMS-554417
IGF-1R, IC50=67.9 nM; IR, IC50=50.6 nM.
S1124
BMS-754807
An IGF-1R inhibitor with an IC50 of 13 nM.
S1234
AG-1024
(Tyrphostin)
A selective inhibitor of IGF-1R and IR with IC50s of
+Q&'+X&'#+
Data independently produced by Xuejun Jiang from
Memorial Sloan-Kettering Cancer Center
GSK1904529A purchased from Selleck
Immortalized wild-type mouse embryonic fibroblasts
were serum starved for 4 h, then stimulate with 100 ng/mL
IGF-1 for 5 min. Inhibitor was added for the last 1 h
of serum starvation.
Data from [Carcinogenesis, 2010 , 31(11),
1948-1955]
CI-1033 (Canertinib) purchased from Selleck
LNCaP-AI cells were starved in 1% stripped
medium for 24 h. The cells were then treated with
Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib
(20 μM), CI-1033 (8 μM), LY294002 (20 μM) and
Bortezomib (20 μM) for 24 h. Cell culture medium
was collected from each sample and subjected to
ELISA for sPLA2-IIa. The condition medium
samples were diluted 10 times for ELISA.
Data independently produced by Dr. Xiangbing
Meng of University of Iowa
CUDC-101 purchased from Selleck
Effect of CUDC-101 on the viability was detected
by WST-1 method after 3 days treatment in
endometrial cancer cell line Hec50 and lshikawa
and ovarian cancer cell line SKOV3, Caov and
PA-1.
Terrific Validation, Tech Support & Prompt Delivery
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
[email protected]
c-Kit
c-Kit
c-Kit
Proto-oncogene c-Kit, CD117
c-Kit Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S1018
Dovitinib
(TKI258)
VEGFR1, IC50=10 nM; VEGFR2, IC50=13 nM; VEGFR3,
IC50=8 nM; Flt3, IC50=1 nM; c-Kit, IC50=2 nM; ,
IC50=27 nM; CSF-1R, IC50=36 nM; FGFR3, IC50=9 nM.
S1119
XL184 Free Base
(Cabozantinib)
VEGFR2, IC50=0.035 nM; Met, IC50=1.8 nM; Flt3,
IC50=14.4 nM; Tie-2, IC50=14.3 nM; Kit, IC50=4.6 nM;
RET.
S1032
Motesanib
diphosphate
(AMG-706)
A multiple inhibitor of VEGFR1/2/3, PDGFR, Kit and
RET receptors. VEGFR1, IC50=2 nM; VEGFR2, IC50=3 nM;
VEGFR3, IC50=6 nM; PDGFR, IC50=84 nM; Kit, IC50=8 nM;
RET, IC50=59 nM.
S1064
Masitinib
A tyrosine kinase c-Kit, PDGFR, FGFR3 and FAK
inhibitor with IC50 of 150 ± 80 nM, 200 ± 40 nM for Kit
tyrosine phosphorylation and the recombinant human
wild-type Kit.
S1178
Regorafenib
(BAY 73-4506)
A multikinase inhibitor. VEGFR2, IC50=40 nM; c-Kit,
IC50=17 nM; B-Raf, IC50=69 nM; VEGFR3; RET;
PDGFR.
S1207
Tivozanib
(AV-951)
An orally bioavailable inhibitor. VEGFR1, IC50=0.21 nM;
VEGFR2, IC50=0.16 nM; VEGFR3, IC50=0.24 nM; c-Kit,
IC50=1.63 nM; PDGFR, IC50=1.72 nM.
S1101
Vatalanib
dihydrochloride
(PTK787)
A novel VEGFR and c-Kit tyrosine kinase and
angiogenesis inhibitor. c-Kit, IC50=0.73 μM; KDR,
IC50=37 nM; Flt1, IC50=77 nM; Flk, IC50=0.27 μM.
S1244
MP-470
A multi-targeted tyrosine kinase inhibitor with potent
activity against mutant c-Met, c-Kit, , Flt3
and c-RET.
S1220
OSI-930
An inhibitor of c-Kit (IC50=9.5 nM) and VEGFR2
(IC50=10.1 nM).
S1363
Ki8751
A potent, selective VEGFR2 tyrosine kinase inhibitor
with IC50 of 0.9 nM. c-Kit, IC50=40 nM; ,
IC50=67 nM; FGFR2, IC50=170 nM.
S2231
Telatinib
(BAY 57-9352)
An orally available, potent multitargeted VEGFR2,
VEGFR3, and c-Kit inhibitor with an IC50 of
19 nM for the inhibition of VEGFR2
autophosphorylation.
S1005
Axitinib
A VEGFR2 and VEGFR3 phosphorylation inhibitor.
VEGFR2, IC50=0.2 nM; VEGFR3, IC50=0.1 to 0.3 nM.
S1021
Dasatinib
(BMS-354825)
The ATP-competitive, dual Src/Abl inhibitor inhibits all
members of the Src family, including c-Src, Lck, Fyn
and Yes (IC50<1.1 nM).
S1026
Imatinib mesylate
A multitargeted c-Kit, PDGFR and c-Abl inhibitor with
IC50@+&'%+&'""
proliferation stimulated by DCs and PHA.
Terrific Validation, Tech Support & Prompt Delivery
Inhibitor
S1035
Pazopanib HCl
A VEGFR inhibitor with IC50s of 10 nM, 30 nM and 47 nM for VEGFR1, 2 and 3.
S1042
Sunitinib malate
(Sutent)
A multitargeted Flt3, PDGFR, VEGFR and Kit kinase inhibitor with Kis of 9 nM and 8 nM
for Flk-1 and PDGFR.
S2769
Dovitinib dilactic
acid
A multitargeted tyrosine kinase inhibitor of Flt3 and c-Kit with IC50s of 1 nM and 2 nM,
respectively.
Data from [AACR, 2011]
Dovitinib (TKI258 ) purchased from Selleck
Ba/F3 cell lines expressing the recombinant
TEL/kinase domain fusion protein for FGFR1-4
.Cells were grown in RPMI 1640 containing 10%
FBS and 500 ng/mL puromycin. The parental Ba/F3
cell line transduced with an empty vector was
grown in 10 ng/mL IL-3 (R&D systems). Cell viability
was assessed at 72 h using the Cell Titer 96
Aqueous One Solution (Promega).
Data from [Circ Res, 2011, 108(10), 1190-1198]
Vatalanib dihydrochloride (PTK787) purchased
from Selleck
Mechanisms of VEGF-activated Ca2+ entry. All
data were from HUVECs. b and c, eYFP-STIM1
(green) before (control) (b) and after exposure to
100 ng/mL VEGF (c). d, Summary data for 100
ng/mL VEGF-evoked transient and sustained
Ca2+ signals after transfection with STIM1.si or
sc.si (n/N=3/64).Scale bar =10 μM.
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
[email protected]
Flt
Flt
Flt/FGFR
Fms-like Tyrosine Kinase
Flt Inhibitors
Cat.No.
S1017
S1490
S1119
S1043
Product Name
Target and IC50 Value
Cediranib
(AZD2171)
A VEGFR2 inhibitor. It inhibited VEGF-stimulated
proliferation and KDR phosphorylation with IC50s of
0.4 nM and 0.5 nM, respectively.
Ponatinib
(AP24534)
Mutant Flt3 phosphorylation, IC50=1 nM; VEGFR2,
IC50=1.5 nM; pan-Bcr-Abl, IC50=0.37 nM; mutant
Bcr-Abl, IC50=2 nM; FGFR1, IC50=2.2 nM; ,
IC50=1.1 nM; Lyn, IC50=0.24 nM; Src, IC50=5.4 nM.
XL184 free base
(Cabozantinib)
Flt3, IC50=14.4 nM; VEGFR2, IC50=0.035 nM; Met,
IC50=1.8 nM; Tie-2, IC50=14.3 nM; Kit, IC50=4.6 nM; RET.
Tandutinib
(MLN518)
An Flt3, PDGFR and Kit inhibitor with IC50 values
of 95-122 ng/mL.
AC220
(Quizartinib)
A uniquely potent and selective Flt3 inhibitor with IC50s
of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375,
respectively.
S1101
Vatalanib
(PTK787)
A novel VEGFR and c-Kit tyrosine kinase and
angiogenesis inhibitor. Flt1, IC50=77 nM; c-Kit,
IC50=0.73 μM; KDR, IC50=37 nM; Flk, IC50=0.27 μM.
S1181
ENMD-2076
An antiangiogenic and Aurora kinase inhibitor. Flt3,
IC50=3 nM; VEGFR2, IC50=93 nM; KDR, IC50=40 nM;
AurA, IC50=13 nM; AurB, IC50=0.35 μM; Src, IC50=23
nM; FGFR1, IC50=0.12 μM.
S1486
AEE788
A novel multitargeted HER 1/2 and VEGFR1/2 inhibitor.
Flt1, IC50=59 nM; EGFR, IC50= 2 nM; ErbB2, IC50=6 nM;
KDR, IC50=77 nM.
S1244
MP-470
A multi-targeted tyrosine kinase inhibitor with potent
activity against mutant c-Met, c-Kit, , Flt3,
and c-RET.
S2769
Dovitinib dilactic
acid
A multitargeted tyrosine kinase inhibitor of Flt3 and
c-Kit with IC50s of 1 nM and 2 nM, respectively.
S2158
KW 2449
A multi-kinase inhibitor of Flt3 (IC50 at 6.6 pM), Abl
(IC50 at 14 pM), Abl-T315I and Aurora kinase.
S2692
S1042
S1018
TG101209
A potent and small molecule JAK2-selective kinase
inhibitor. Flt3, IC50=25 nM; JAK2, IC50=6 nM; RET,
IC50=17 nM; JAK3, IC50=169 nM.
Sunitinib malate
(Sutent)
A multitargeted Flt3, PDGFR, VEGFR and Kit kinase
inhibitor with Kis of 9 nM and 8 nM for Flk-1 and
PDGFR.
Dovitinib Dilactic
acid (TKI258
Dilactic acid)
VEGFR1, IC50=10 nM; VEGFR2, IC50=13 nM; VEGFR3,
IC50=8 nM; Flt3, IC50=1 nM; c-Kit, IC50=2 nM; ,
IC50=27 nM; CSF-1R, IC50=36 nM; FGFR3, IC50=9 nM.
R406
A potent and orally available spleen tyrosine kinase (Syk) inhibitor with an EC50 and a Ki of
56 nM and 30 nM, respectively.
S2725
PF-03814735
A novel, potent, orally bioavailable, reversible small-molecule Aurora kinase inhibitor. Aurora 1,
IC50=0.8 nM; Aurora 2, IC50=5 nM; Flt1, IC50=10 nM; FAK, IC50=22 nM.
Inhibitor
FGFR
Fibroblast Growth Factor Receptor
FGFR Inhibitors
Data independently produced by Dr. Antonino Maria
Sparta, University of Trento
ENMD-2076 purchased from Selleck
SDS-PAGE of CHP-134 cells extracts after 24 h
exposure to the indicated drug and concentration.
>
<!<#
used as house-keeping protein. Aurora A blockade
seems to diminish N-myc expression or stability.
KW2449(μM)
S1526
S2194
0
0.001
0.01
0.1
1
Cat.No.
Product Name
Target and IC50 Value
S1010
BIBF1120
(Vargatef)
An inhibitor of FGFR, VEGFR and PDGFR. FGFR1,
IC50=69 nM; FGFR2, IC50=37 nM; FGFR3, IC50=108 nM;
VEGFR, IC50=13-34 nM; PDGFRa, IC50=59 nM;
PDGFRh, IC50=65 nM.
S1107
Danusertib
(PHA-739358)
A pyrrolo-pyrazole and small molecule Aurora kinases
and Bcr-Abl kinase inhibitor. Aurora A, IC50=13 nM;
Aurora B, IC50=79 nM; Aurora C, IC50=61 nM.
S1490
Ponatinib
(AP24534)
FGFR1, IC50=2.2 nM; VEGFR2, IC50=1.5 nM;
pan-Bcr-Abl, IC50=0.37 nM; mutant Bcr-Abl, IC50=2 nM;
, IC50=1.1 nM; mutant Flt3 phosphorylation,
IC50=1 nM; Lyn, IC50=0.24 nM; Src, IC50=5.4 nM.
S1064
Masitinib
A tyrosine kinase c-Kit, PDGFR, FGFR3 and FAK
inhibitor with IC50 of 150 ± 80 nM, 200 ± 40 nM for Kit
tyrosine phosphorylation and the recombinant human
wild-type Kit.
S1084
Brivanib
(BMS-540215)
A VEGFR2 inhibitor with an IC50 of 25 nM and Ki of
26 nM. FGFR1, IC50=148 nM; FGFR2, IC50=125 nM;
FGFR3, IC50=68 nM; VEGFR1, IC50=0.38 μM;
VEGFR3, IC50=10 nM.
S1470
TSU-68 (SU6668)
A novel multiple receptor tyrosine kinase inhibitor.
FGFR1, IC50=1.2 μM; VEGFR1, IC50=2.1 μM; ,
IC50=8 nM.
S1264
PD173074
A potent ATP-competitive, reversible FGFR and
VEGFR inhibitor. FGFR3, IC50=5 nM; FGFR1,
IC50=21.5 nM; VEGFR2, IC50 , ~100 nM; PDGFR,
IC50=17.6 μM; c-Src, IC50=19.8 μM.
p-Histone
Histone
Data independently produced by Dr. Zhang of
Tianjin Medical University
KW 2449 purchased from Selleck
Western blot analysis of p-histone and histone.
X&'{%QQ!+
Data independently produced by Dr. Yong-Weon Yi
from Georgetown University Medical Center
MP-470 purchased from Selleck
For MTT assays, cells (2,000~5,000 cells/well) were
subcultured into 96-well plates according to their
growth properties. Cell proliferation was assayed at
^%"
'Q^%&Y
Y'#X&Y!"
#
+
After incubating for 3-4 h at 37°C, the media were
removed and 150 μL/well of MTT solvent (either
absolute DMSO or isopropanol containing 4 mM HCl
and 0.1% Nonidet-40) was added to dissolve the
formazan.
DAPI
Hypoxyprobe
Overlay
Large
Colony
(Cont)
S1138
Brivanib alaninate
(BMS-582664)
A multiple inhibitor of VEGFR and FGFR. VEGFR2,
IC50 of 25 nM and Ki of 26 nM; VEGFR1, IC50=0.38 μM;
VEGFR3, IC50=10 nM; FGFR1, IC50=148 nM; FGFR2,
IC50=125 nM; FGFR3, IC50=68 nM.
S2774
MK-2461
A potent inhibitor of c-Met, Ron, Flt1, Flt3, ,
and Mer with IC50s of 2.5 nM, 7 nM, 10 nM, 22 nM,
22 nM and 24 nM, respectively.
S2183
BGJ398
A potent and selective FGFR family inhibitor for FGFR1,
FGFR2, FGFR3 and FGFR4 with IC50s of 0.9 nM, 1.4 nM,
1 nM and 60 nM, respectively.
S2769
Dovitinib dilactic
acid
A multitargeted tyrosine kinase inhibitor of Flt3 and
c-Kit with IC50s of 1 nM and 2 nM, respectively.
Small
Colony
(Cont)
Large
Colony
(1μM)
Data from [Biochem Bioph Res Co, 2010, 398,
205-211]
Sunitinib malate (Sutent) purchased from Selleck
Sunitinib limits the colonial growth of HT-29 by
downregulating HIF-1a. HIF-1a expression and
hypoxia within HT-29 colony. After colonies grew for
4 weeks, HIF-1a and hypoxia were visualized by
immunofluoroscence staining. Bar = 20 μm.
Terrific Validation, Tech Support & Prompt Delivery
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
Data from [Nature, 2011, 478(7369), 349-355]
BIBF1120(Vargatef) purchased from Selleck
#
all insulin+ cells with BrdU incorporation.
Data from [Science, 2011, 331(6019), 912-916]
PD173074 purchased from Selleck
'#X#
Hand2d/d mice treated with PD173074.
[email protected]
HIF/VDA/Syk/Tie-2
HIF
FAK/c-RET
FAK
Hypoxia-inducible Factor
FAK Inhibitors
HIF Inhibitor
Cat.No.
Product Name
Target and IC50 Value
S1233
2-Methoxyestradiol
A natural metabolite of estrogen that is known to
o inhibit
"
HIF-1 alpha with an IC50+^X+XX&'"
inhibition of BPAEC migration.
VDA
We give free samples and
rewards to people who would
like to provide us useful scientific
data (western blot, etc.)
Cat.No.
Product Name
Target and IC50 Value
S1064
Masitinib
A tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50s of 150 ± 80 nM,
200 ± 40 nM for Kit tyrosine phosphorylation and the recombinant human wild-type Kit.
S2672
PF-562271
A potent ATP-competitive FAK and Pyk2 inhibitor with potential antineoplastic and antiangiogenic
activities.
S2725
PF-03814735
A novel, orally bioavailable, reversible small-molecule Aurora kinase inhibitor. Aurora 1, IC50=0.8 nM;
Aurora 2, IC50=5 nM; Flt1, IC50=10 nM; FAK, IC50=22 nM.
Vascular Disrupting Agent
VDAs
c-RET
Cat.No.
Product Name
Target and IC50 Value
S1537
DMXAA (ASA404)
A tumor-VDA with an IC50 of 9.46 ± 1.7 nM.
M.
S1176
NPI-2358 (Plinabulin)
A novel VDA with an IC50 of 15 nM against
st
HT-29 cells.
Syk
Focal Adhesion Kinase
We give free samples and
rewards to people who would
like to provide us useful scientific
data (western blot, etc.)
RET Proto-oncogene
c-RET Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S1046
Vandetanib
A tyrosine kinase c-Kit, PDGFR, FGFR3 and FAK inhibitor with IC50 of 150 ± 80 nM,
200 ± 40 nM for Kit tyrosine phosphorylation and the recombinant human wild-type
Kit.
S1244
Amuvatinib
A potent and multi-targeted tyrosine kinase inhibitor of c-Kit and , as well
as their mutants, with IC50
X'@X&'+
S2692
TG101209
A potent and small molecule JAK2-selective kinase inhibitor. JAK2, IC50=6 nM;
Flt3, IC50=25 nM; RET, IC50=17 nM; JAK3, IC50=169 nM.
S1107
Danusertib
An aurora kinase inhibitor of Aurora A, B and C with IC50s of 13 nM, 79 nM and
61 nM, respectively.
Spleen Tyrosine Kinase
Syk Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S2194
R406
An orally available Syk inhibitor with an IC50 of 41 nM.
S1533
R406 free base
An orally available Syk inhibitor with a Ki of 30 nM.
S2206
R935788 (Fostamatinib
disodium)
A selective Syk inhibitor with an IC50 of 41 nM.
S2625
R788 (Fostamatinib)
An important Syk inhibitor and a free base of R788.
Tie-2
Angiopoietin Receptor
Tie-2 Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S1119
XL184 free base
(Cabozantinib)
VEGFR2, IC50=0.035 nM; Met, IC50=1.8 nM; Flt3, IC50=14.4 nM; Tie-2,
IC50=14.3 nM; Kit, IC50=4.6 nM; RET.
S1361
MGCD-265
A multi-targeted kinase inhibitor, which targets the c-Met, VEGFR1, VEGFR2,
VEGFR3, Tie-2 and Ron.
S1577
Tie-2 kinase inhibitor
A potent, reversible, and ATP-binding site-targeting Tie-2 inhibitor with an IC50 of
250 nM.
Terrific Validation, Tech Support & Prompt Delivery
Toll Free:(877)796-6397
---USA and Canada only---
Phone:+1-832-582-8158
www.selleckchem.com
[email protected]
JAK
Headquarters
JAK
Tel:
+1-832-582-8158
Fax: +1-832-582-8590
E-mail: [email protected]
Janus Kinase
JAK Inhibitors
Cat.No.
Product Name
Target and IC50 Value
S5001
Tofacitinib citrate
(CP-690550)
A potent JAK kinase inhibitor of IL-2-mediated human
T cell blast proliferation and IL-15-induced CD69
expression with IC50s of 11 nM and 48 nM, respectively.
S2162
S1134
S1143
S2179
S2219
AZD1480
AT9283
AG-490
A potent EGFR kinase autophosphorylation inhibitor.
EGFR, IC50=100 nM; JAK, IC50=56.8 μM.
LY2784544
A small molecule selective mutant JAK2 kinase
inhibitor with an IC50 of 68 nM.
Cyt387
AZ 960
A novel JAK2 kinase inhibitor. IC50=3 mM; Ki=0.45 nM.
S2736
TG-101348
A potent, highly selective and ATP- competitive JAK2
inhibitor. JAK2, IC50=3 nM; Flt3, IC50=15 nM;
RET, IC50=48 nM.
S2686
S1378
TG101209
A potent small molecule JAK2-selective kinase
inhibitor. JAK2, IC50=6 nM; Flt3, IC50=25 nM; Ret,
IC50=17 nM; JAK3, IC50=169 nM.
NVP-BSK805
A selective quinoxaline JAK2 inhibitor. JAK2 JH1,
IC50=0.48 nM; FL JAK V617F, IC50=0.56 nM;
FL JAK2 wt, IC50=0.58 nM.
INCB018424
(Ruxolitinib)
An orally bioavailable JAK inhibitor. JAK1, IC50=3 nM;
JAK2, IC50=5 nM; JAK3, IC50=332 nM.
Australia
France
Japan
Spain
Life Research Pty Ltd
EUROMEDEX
Tel:
+33 (3) 88 18 07 22
Email: [email protected]
COSMO BIO CO., LTD
DELTACLON S.L.
Tel:
+81 3 5632 9610
Email: [email protected]
Tel:
+34 917645364
Email: [email protected]
Tel: +61 398030045
Email: [email protected]
Data from [Int Immunol, 2011, 23(11), 701-712]
Tofacitinib citrate (CP-690550) purchased from
Selleck
STAT3 inhibition antagonizes arthritis effects in
vivo. Whole-cell lysates were made from ankle
joint tissues of CIA mice treated with or without
CP690,550 for 2 weeks. Phosphorylated STAT3
was then analyzed by western blot (upper panel)
and ELISA (lower panel).
An ATP-competitive small molecule JAK1/JAK2 inhibitor.
JAK1, IC50=11 nM; JAK2, IC50=18 nM.
S2214
S2692
Worldwide Distributors
A novel pyrazol pyrimidine ATP-competitive JAK1 and
JAK2 inhibitor with IC50s of 1.3 nM and <0.4 nM,
respectively.
A multi-targeted c-Abl, JAK2, Aurora A and B
inhibitor. JAK2, IC50=1.2 nM; JAK3, IC50=1.1 nM;
Bcr-Abl (T3151), IC50=4 nM; Aurora A and B, IC50 of
approximate 3 nM.
Tel:
+49-89-46148500
Fax:
+49-89-461485022
E-mail: [email protected]
Data from [Leukemia, 2012, 26(4), 708-715]
AZD1480 purchased from Selleck
Mutations in the JAK2V617F kinase domain confer
resistance to JAK2 tyrosine kinase inhibitors.
Growth of BaF3.EpoR cells expressing
JAK2V617F and the additional mutations was
determined in response to AZD1480 at various
concentrations, as indicated (n=4).
Web: www.liferesearch.com
Web: www.euromedex.com
Web: www.cosmobio.co.jp
Web: www.deltaclon.com
Australia
Germany
Korea
Sweden
Stratech Scientific APAC
+61 (0)2 9973 2421
Tel:
Email: [email protected]
Absource Diagnostics GmbH
Kim & Friends, Inc.
Tel:
+49 89 8296 9377
Email: [email protected]
Tel:
+82 226476611
Email: kim and [email protected]
SMS-gruppen
Tel: +46 42120240
Email: [email protected]
Web: www.stratechscientific.com.au
Web: www.absource.net
Web: [email protected]
Web: www.sms-gruppen.dk
Austria
Germany
Netherlands
Switzerland
eubio
ICS International Clinical Service GmbH
Bio-Connect Diagnostics BV
LuBioScience GmbH
Tel:
+43 18950145
Email: [email protected]
Tel:
+49 (0)89917551
Email: [email protected]
Tel:
Tel: +41 414170280
Email: [email protected]
Web: www.eubio.at
Web: www.ics-gmbh.de
Web: www.bio-connectdiagnostics.nl
Web: www.lubio.ch
Israel
Poland
Taiwan
Cedarlane
Tel:
+1 289 288 0001
Email: [email protected]
Da-Ta Biotech Ltd.
Tel:
+972 8 9100 575
Email: [email protected]
STI
Tel:
+48 61 64717759
Email: [email protected]
Lumtec
Tel: +88 636663188
Email: [email protected]
Web: www.cedarlanelabs.com
Web: www.databiotech.co.il
Web: www.sti.biz.pl
Web: www.lumtec.com.tw
China
Italy
Russia
UK
BinXin Bio, Co Ltd
Aurogene
Tel:
+39 06 9818 5510
Email: [email protected]
COPRAS
Stratech Scientific Ltd.
Tel:
+86 22 23915166
Email: [email protected]
+74 953331163
Tel:
Email: [email protected]
Tel:
+44 (0)1638782600
Email: [email protected]
Web: [email protected]
Web: www.aurogene.eu
Web: www.copras.ch
Web: www.stratech.co.uk
China
Japan
Russia
USA
Selleck Life Sciences Shanghai
NAMIKI SHOJI CO., LTD.
RUSCHEMBIO
Tel:
400-168-1698
Email: [email protected]
Tel:
+81 3 3354 4026
Email: [email protected]
Tel:
+74 952760067
Email: [email protected]
ThermoFisher
Tel: +1 800 766 7000
Email: [email protected]
Web: www.selleck.cn
Web: www.namiki-s.co.jp
Web: www.ruschembio.ru
Web: www.thermofisher.com
Denmark
Japan
Singapore
USA
SMS-gruppen
Wako Pure Chemical Industries, Ltd.
PRECISION TECHNOLOGIES PTE LTD
VWR International LLC
Tel:
Tel:
Tel:
Tel:
+45 45864400
+81 1 20052099
+65 62734573
+1 800 932 5000
Email: [email protected]
Email: [email protected]
Email: [email protected]
Email: [email protected]
Web:
Web:
Web:
Web: www.vwr.com
www.sms-gruppen.dk
www.wako-chem.co.jp
For detailed product information, please visit us online:
www.selleckchem.com
Terrific Validation, Tech Support & Prompt Delivery
Email: [email protected]
Canada
Selleck Chemicals
+31
www.pretech.com.sg