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Angiogenesis FGFR

FGFR

The fibroblast growth factor receptors (FGFR) are, as their name implies, receptors that bind to members of the fibroblast growth factor (FGF) family of proteins. Some of these receptors are involved in pathological conditions. For example, a point mutation in FGFR3 can lead to achondroplasia.The fibroblast growth factor receptors consist of an extracellular ligand domain composed of three immunoglobulin-like domains, a single transmembrane helix domain, and an intracellular domain with tyrosine kinase activity. These receptors bind fibroblast growth factors, members of the largest family of growth factor ligands, comprising 22 members.
Cat No. product name
T0093 Sorafenib tosylateHOT Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
T0374 Sunitinib MalateHOT Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
T0520 Lenvatinib Lenvatinib is a Kinase Inhibitor. The mechanism of action of lenvatinib is as a Receptor Tyrosine Kinase Inhibitor.
T1338 Sucralfate Sucralfate is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers.
T1639 Amlexanox Amlexanox is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mas...
T1886 TAK632 TAK-632 is a potent pan-Raf inhibitor.
T1895 SKLB 610 SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2, and PDGFR at a rate of 97%, 65%, and 55%, respectively, ...
T1948 AZD4547HOT AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).
T1975 InfigratinibHOT Infigratinib (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9/1.4/1 nM for FGFR1/2/3), >40-fold selective for FGFR versus FGFR4 and VEGFR2.
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may...
T2215 Ferulic Acid Ferulic Acid is a highly abundant phenolic phytochemical and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.It can be ab...
T7499 TAK-779 TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
T2347 BLU9931 BLU9931 is the first selective small molecule inhibitor of FGFR4.
T2361 LY-2874455 LY2874455 has been used in trials studying the treatment of Advanced Cancer.
T2372 PonatinibHOT Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
T2446 KI8751 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2576 Brivanib Alaninate Brivanib Alaninate is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib ...
T2608 CHIR-98014 CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
T2642 PD173074 PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold fo...
T3274 S49076 S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.
T3456 BLU-554 BLU-554 is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).
T3466 FIIN-3 FIIN-3 is an irreversible inhibitor of FGFR.
T3492 PD-166866 PD166866 is a selective FGFR tyrosine kinase inhibitor.
T3512 S49076 HCl S49076 is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstrea...
T3714 SUN 11602 SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and preven...
T3726 Erdafitinib Erdafitinib is a quinoxaline derivative compound, acts on FGFR1/2/3/4.
T4075 Sulfatinib Sulfatinib may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity. It also is a hERG inhibitor.
T4235 Roblitinib FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and in...
T6024 CH5183284 CH5183284 is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), res...
T6036 Brivanib Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3...
T6082 SSR128129E SSR128129E is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.
T6124 Mubritinib Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T6128 PHA-665752 PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
T6154 SU11274 SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.
T6184 Orantinib TSU-68,a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little ef...
T6193 Dovitinib Dilactic Acid Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with...
T6289 Dovitinib Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V ...
T6479 Dovitinib Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also p...
T6711 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
T6836 FIIN-2 FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
T6930 Pazopanib HCl Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, ...
T6932 PD168393 PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
T6996 SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
T4318 ACTB-1003 ACTB-1003 is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).
T5122 Alofanib Alofanib is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10...
T5044 TAS120 TAS-120 is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.
T5001 Nintedanib Ethanesulfonate Salt BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β
T1777 NintedanibHOT Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).
T5473 ASP-5878 ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.
T7104 Dovitinib lactate Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
Sorafenib tosylate HOT
T0093CAS 475207-59-1
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
Sunitinib Malate HOT
T0374CAS 341031-54-7
Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
Lenvatinib
T0520CAS 417716-92-8
Lenvatinib is a Kinase Inhibitor. The mechanism of action of lenvatinib is as a Receptor Tyrosine Kinase Inhibitor.
Sucralfate
T1338CAS 54182-58-0
Sucralfate is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers.
Amlexanox
T1639CAS 68302-57-8
Amlexanox is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mas...
TAK632
T1886CAS 1228591-30-7
TAK-632 is a potent pan-Raf inhibitor.
SKLB 610
T1895CAS 1125780-41-7
SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2, and PDGFR at a rate of 97%, 65%, and 55%, respectively, ...
AZD4547 HOT
T1948CAS 1035270-39-3
AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays).
Infigratinib HOT
T1975CAS 872511-34-7
Infigratinib (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9/1.4/1 nM for FGFR1/2/3), >40-fold selective for FGFR versus FGFR4 and VEGFR2.
Danusertib
T2094CAS 827318-97-8
Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may...
Ferulic Acid
T2215CAS 1135-24-6
Ferulic Acid is a highly abundant phenolic phytochemical and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.It can be ab...
TAK-779
T7499CAS 229005-80-5
TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
BLU9931
T2347CAS 1538604-68-0
BLU9931 is the first selective small molecule inhibitor of FGFR4.
LY-2874455
T2361CAS 1254473-64-7
LY2874455 has been used in trials studying the treatment of Advanced Cancer.
Ponatinib HOT
T2372CAS 943319-70-8
Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
KI8751
T2446CAS 228559-41-9
KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
Brivanib Alaninate
T2576CAS 649735-63-7
Brivanib Alaninate is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib ...
CHIR-98014
T2608CAS 252935-94-7
CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
PD173074
T2642CAS 219580-11-7
PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold fo...
S49076
T3274CAS 1265965-22-7
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.
BLU-554
T3456CAS 1707289-21-1
BLU-554 is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4).
FIIN-3
T3466CAS 1637735-84-2
FIIN-3 is an irreversible inhibitor of FGFR.
PD-166866
T3492CAS 192705-79-6
PD166866 is a selective FGFR tyrosine kinase inhibitor.
S49076 HCl
T3512CAS 1265966-31-1
S49076 is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstrea...
SUN 11602
T3714CAS 704869-38-5
SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and preven...
Erdafitinib
T3726CAS 1346242-81-6
Erdafitinib is a quinoxaline derivative compound, acts on FGFR1/2/3/4.
Sulfatinib
T4075CAS 1816307-67-1
Sulfatinib may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity. It also is a hERG inhibitor.
Roblitinib
T4235CAS 1708971-55-4
FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and in...
CH5183284
T6024CAS 1265229-25-1
CH5183284 is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), res...
Brivanib
T6036CAS 649735-46-6
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3...
SSR128129E
T6082CAS 848318-25-2
SSR128129E is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.
Mubritinib
T6124CAS 366017-09-6
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
PHA-665752
T6128CAS 477575-56-7
PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
SU11274
T6154CAS 658084-23-2
SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.
Orantinib
T6184CAS 252916-29-3
TSU-68,a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little ef...
Dovitinib Dilactic Acid
T6193CAS 852433-84-2
Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with...
Dovitinib
T6289CAS 405169-16-6
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V ...
Dovitinib Lactate
T6479CAS 915769-50-5
Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also p...
Tyrphostin AG 1296
T6711CAS 146535-11-7
Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
FIIN-2
T6836CAS 1633044-56-0
FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
Pazopanib HCl
T6930CAS 635702-64-6
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, ...
PD168393
T6932CAS 194423-15-9
PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
SU5402
T6996CAS 215543-92-3
SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
ACTB-1003
T4318CAS 939805-30-8
ACTB-1003 is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).
Alofanib
T5122CAS 1612888-66-0
Alofanib is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10...
TAS120
T5044CAS 1448169-71-8
TAS-120 is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.
Nintedanib Ethanesulfonate Salt
T5001CAS 656247-18-6
BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β
Nintedanib HOT
T1777CAS 656247-17-5
Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).
ASP-5878
T5473CAS 1453208-66-6
ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.
Dovitinib lactate
T7104CAS 692737-80-7
Dovitinib lactate(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).