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FGFR

FGFR

货号 产品名 CAS号 信息
CSN21277 Tyrosine kinase-IN-1 705946-27-6 Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
CSN33144 E7090 1622204-21-0 Tasurgratinib is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity.
CSN22070 SUN11602 704869-38-5 SUN11602 is a mimic of basic fibroblast growth factor (bFGF) which can prevent glutamate-induced neuronal death and increase the levels of CALB1 gene expression in cerebrocortical neurons.
CSN18656 Sulfatinib 1308672-74-3 Sulfatinib is an inhbitor of KDR and FGFR1 with IC50 values of 0.021 μM and 0.053 μM respectively. It also shows inhibition of hERG (IC50 = 6.8 μM).
CSN20031 (Z)-Orantinib 210644-62-5 SU6668 is a cell-permeable indolinone compound that acts as a potent ATP-competitive inhibitor against RTKs (receptor tyrosine kinases) Kit, PDGFRβ, VEGFR2 (Flk-1/KDR), FGFR1 activity in vitro (IC50 = 0.01, 0.1, 3.9, and 3.8 µM, respectively) and PDGF/VEGF/bFGF-mediated angiogenesis and tumor development. Although initially characterized as an RTK inhibitor, SU6668 is now also known to target ser/thr kinases Aurora A, Aurora B, TBK1 (NAK/T2K), and AMPK (IC50 = 0.85, 0.047, 1.4, and 1.8 µM, respectively), as well as non-receptor TKs Lyn and Yes (IC50 = 4.3 and 5.8 µM, respectively).
CSN15810 SSR128129E 848318-25-2 SSR128129E is an allosteric modulator of FGFR by binding to the extracellular FGFR domain.
CSN18466 SSR128129E free acid 848463-13-8 SSR128129E free acid is a multi-FGFR blocker with allosteric properties and inhibits FGFR signaling by binding to the extracellular FGFR domain without affecting orthosteric FGF binding.
CSN26937 Rogaratinib 1443530-05-9 Rogaratinib is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor.
CSN20388 PRN1371 1802929-43-6 PRN1371 is an irreversible covalent FGFR inhibitor used for the treatment of solid tumor.
CSN21067 Ponatinib hydrochloride 1114544-31-8 Ponatinib is a multi-targeted kinase inhibitor with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src respectively.
CSN26440 Pemigatinib 1513857-77-6 Pemigatinib, also known as INCB054828, is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types 1, 2, and 3 (FGFR1/2/3), with potential antineoplastic activity. FGFR inhibitor INCB054828 binds to and inhibits FGFR1/2/3, which may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells.
CSN12916 PD173074 219580-11-7 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src.
CSN13927 PD-166866 192705-79-6 PD 166866 is a selective FGFR tyrosine kinase inhibitor with an IC50 of 52.4 nM.
CSN23025 PD0166285 dihydrochloride 212391-63-4 PD 166285 inhibited Src nonreceptor tyrosine kinase, fibroblast growth factor receptor-1, epidermal growth factor receptor and platelet-derived growth factor receptor beta subunit (PDGFR-beta), tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 8.4 +/- 2.3 nM (n = 6), 39.3 +/- 2.8 nM (n = 16), 87.5 +/- 13.7 nM (n = 6) and 98.3 +/- 7.9 nM (n = 16), respectively.
CSN23024 PD-161570 192705-80-9 PD 161570 is a selective FGFR inhibitor with IC50 of 40 nM.
CSN25230 ODM-203 1430723-35-5 ODM-203 is a selective inhibitor of FGFR and VEGFR with IC50 values of 11, 16, 6, 35nM for recombinant FGFR1-4 and 26, 9, 5nM for VEGFR1-3, respectively.
CSN22060 MRX-2843 1429882-07-4 MRX-2843 is an orally available small-molecule inhibitor of both MERTK and FLT3.
CSN16111 LY2874455 1254473-64-7 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM.
CSN18841 H3B-6527 1702259-66-2 H3B-6527 acts as a selective FGFR4 inhibitor (IC50 <1.2 nM) over FGFR1-3.
CSN13938 FIIN-3 1637735-84-2 FIIN-3 is an irreversible inhibitor of FGFR1-4 with IC50s of 13, 21, 31, and 35 nM, respectively.
CSN13937 FIIN-2 1633044-56-0 FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
CSN22818 N-(3-((3-(2,6-Dichloro-3,5-dimethoxyphenyl)-7-(4-(diethylamino)butylamino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide hydrochloride 1779796-29-0 FIIN 1 HCl is a potent, irreversible FGFR inhibitor with Kds of 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively.
CSN18853 FGFR4-IN-1 1708971-72-5 FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
CSN20012 FGFR4 Inhibitor C(-)-11 2020395-38-2 FGFR4 inhibitor C(-)-11 is a highly potent FGFR4 inhibitor with selectivity over FGFR1 with good stability and CYP inhibition.
CSN19155 Futibatinib 1448169-71-8 FGFR-IN-1 is a potent and highly selective FGFR inhibitor, used for antitumor treatment.
CSN19757 Roblitinib 1708971-55-4 FGF401, an inhibitor of human fibroblast growth factor receptor 4 (FGFR4, IC50 = 1.1 nM), has potential antineoplastic activity.
CSN17720 Erdafitinib 1346242-81-6 Erdafitinib inhibits FGFR1 (pIC50 = 9), FGFR2 (pIC50 = 8.5), FGFR3 (pIC50 = 8.5) and FGFR4 (pIC50 = 8.25) and it is a quinoxaline derivative compound.
CSN20555 Derazantinib 1234356-69-4 Derazantinib is a fibroblast growth factor receptor (FGFR) inhibitor that has antitumor activity.
CSN21245 ARQ-087 2HCl 1821329-75-2 Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
CSN12423 Danusertib 827318-97-8 Danusertib is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively. It is modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc.
CSN17224 Zoligratinib 1265229-25-1 CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
CSN13925 BLU9931 1538604-68-0 BLU9931 is an inhibitor of FGFR4 with IC50 of 3 nM and is less potent for FGFR1/2/3 (IC50 > 150 nM).
CSN18780 Fisogatinib 1707289-21-1 BLU-554 is a selective inhibitor of FGFR4 with the IC50 of 5 nM.
CSN17679 Infigratinib phosphate 1310746-10-1 BGJ398 Phosphate is a selective and potent inhibitor of FGFRs with IC50 values of 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM for FGFR3-K650E mutant.
CSN16144 Infigratinib 872511-34-7 BGJ-398 is a selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively and > 40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
CSN12890 AZD4547 1035270-39-3 AZD4547 is a selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM with weaker activity against FGFR4, VEGFR2 (KDR), and little activity observed against IGFR, CDK2, and p38.
CSN19705 ASP5878 1453208-66-6 ASP5878 is a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance.
CSN26650 ARQ 069 1314021-57-2 and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner[1].
CSN22608 Alofanib 1612888-66-0 Alofanib is a selective and allosteric inhibitor of FGFR2 with potential antitumor activity.
CSN12169 Tyrphostin AG1296 146535-11-7 AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. It also inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells.
CSN18610 EOC317 939805-30-8 ACTB-1003 is a potent inhibitor of FGFR1 with IC50 < 10 nM in FGFR-1 biochemical assay.
CSN26199 SKLB 610 1125780-41-7
CSN33244 Methyl 7-chloro-4-(4-methoxybenzyl)-2-methyl-5-oxo-4,5-dihydro-2H-pyrazolo[4,3-b]pyridine-6-carboxylate 2338863-43-5
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