2018-2019 AdooQ 最新目录册 点击此处下载

FGFR

Inhibitory Selectivity
Catalog No.Inhibitor Name FGFRFGFR1FGFR2FGFR3FGFR4Other
A10080Ponatinib
****
Abl,PDGFRα,VEGFR2
A11159BGJ398
****
****
****
**
VEGFR2,Lyn,Kit
A10137Nintedanib
**
**
**
*
VEGFR3,VEGFR2,LCK
A10703PD173074
**
VEGFR2,c-Src
A11411Dovitinib
***
***
FLT3,c-Kit,VEGFR3/FLT4
A11075AZD4547
****
****
****
*
KDR,IGFR
A10715Danusertib
**
Aurora A,Abl,TrkA
A10953Orantinib
*
PDGFRβ,Flk1
A10254Brivanib
*
VEGFR2,Flk1,VEGFR1
A10198Dovitinib Dilactic Acid
***
***
FLT3,c-Kit,VEGFR3/FLT4
A11753MK-2461
**
**
**
A10162Brivanib Alaninate
*
VEGFR2,Flk1,VEGFR1
A13211SSR128129E
*
VEGFR2,PDGFRβ
A11558SU5402
**
A15534BLU9931
*
*
*
****
A12357FIIN-2
****
***
**
**
FLT3,c-Kit,VEGFR3/FLT4
A14415CH5183284
***
***
***
*
VEGFR2
A11244LY2874455
****
****
***
***
A15957Erdafitinib
A10508KW-2449
**
FLT3, Bcr-Abl, Aurora A, PDGFRβ, IGF-1R, EGFR
A10699Pazopanib HCl
*
VEGFR1, VEGFR2, VEGFR3, PDGFR, c-Kit, c-Fms
A11518Pazopanib
*
VEGFR1, VEGFR2, VEGFR3, PDGFR, c-Kit, c-Fms
A13111R 1530
*
Chk2, KDR, FGFR, Aurora A, Cdk2, VEGFR-2, PDGFRβ
A15073E-3810
***
**
VEGFR1, VEGFR2, VEGFR3
A15848FIIN-3
***
**
**
**
A15957Alofanib (RPT835)

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



31 个项目

每页

设置升序顺序
Catalog No. Product Name Application Product Information
A11411 SALE

Dovitinib (TKI-258)

RTK 抑制剂
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
A13069 SALE

XL-228

IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13111 SALE

R1530

Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂
R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
A13211

SSR128129E

FGFR1 抑制剂
SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM
A14415

Debio-1347 (CH5183284)

FGFR1/2/3 抑制剂
Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity.
A14431 SALE

ACTB-1003

FGFR1 抑制剂
ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase).
A15073

E-3810

VEGFR/FGFR 抑制剂
E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
A15194

NVP-BGJ398 phosphate

FGFR 抑制剂
NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
A15534 SALE

BLU9931

FGFR 抑制剂
BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM),
A12357 SALE

FIIN-2

FGFR 抑制剂
FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
A15848

FIIN-3

Irreversible FGFR 抑制剂
FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
A15946

Alofanib (RPT835)

FGFR2 抑制剂
Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity.
A15957

Erdafitinib (JNJ-42756493)

FGFR 抑制剂
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity.
A16197

Nintedanib esylate

RTK 抑制剂
Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).
A11558 SALE

SU-5402

VVEGFR/FGFR/EGFR 抑制剂?€?
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).
A11244 SALE

LY 2874455

FGFR/VEGFR2 抑制剂
LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
A11518 SALE

Pazopanib (GW-786034)

VEGFR 抑制剂
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
A10080 SALE

AP24534 (Ponatinib)

BCR-ABL 抑制剂
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
A10715 SALE

Danusertib (PHA-739358)

Aurora 抑制剂
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
A10137 SALE

Bibf1120 (Vargatef)

VEGFR 抑制剂
BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.
A10703 SALE

PD173074

FGFR1/VEGFR2 抑制剂
PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.
A10953 SALE

TSU-68 (Orantinib, SU6668)

PDFGR?? 抑制剂
Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
A10254 SALE

Brivanib (BMS-540215)

VEGFR-2 抑制剂
Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
A10162

Brivanib alaninate (BMS-582664)

VEGFR 抑制剂
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling.
A10508 SALE

KW-2449

FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
A11075 SALE

AZD4547

FGFR 抑制剂
AZD4547 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.
A11159 SALE

BGJ398 (NVP-BGJ398)

FGFR 抑制剂
BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively).
A10699 SALE

Pazopanib HCl (GW786034)

VEGFR/PDGFR/FGFR 抑制剂
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
A10198 SALE

Dovitinib Dilactic acid (TKI258 Dilactic acid)

RTK 抑制剂
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
A11753

MK-2461

c-Met 抑制剂
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
A16251

FGFR4-IN-1

FGFR4 抑制剂
FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.

31 个项目

每页

设置升序顺序