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FGFR

FGFR

Cat. No. Product Name CAS No. Information
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.
CSN18656 Sulfatinib   1308672-74-3 Sulfatinib is an inhbitor of KDR and FGFR1 with IC50 values of 0.021 M and 0.053 M respectively. It also shows inhibition of hERG (IC50 6.8 M).
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, PDGFR, VEGFR2 (Flk-1KDR), FGFR1 activity in vitro (IC50 0.01, 0.1, 3.9, and 3.8 M, respectively) and PDGFVEGFbFGF-mediated angiogenesis and tumor development. Although initially characterized as an RTK inhibitor, SU6668 is now also known to target serthr kinases Aurora A, Aurora B, TBK1 (NAKT2K), and AMPK (IC50 0.85, 0.047, 1.4, and 1.8 M, respectively), as well as non-receptor TKs Lyn and Yes (IC50 4.3 and 5.8 M, 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
CSN22605 3-((3-((4-(Morpholinomethyl)-1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)methyl)thiazolidine-2,4-dione hydrochloride 1265966-31-1 S49076 hydrochloride is a potent, ATP-competitive tyrosine kinase inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 <20 nM.
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 524 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 28 nM 26 nM 64 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 12 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 31 43 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 07 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 11 nM has potential antineoplastic activity
CSN17720 Erdafitinib 1346242-81-6 Erdafitinib inhibits FGFR1 pIC50 9 FGFR2 pIC50 85 FGFR3 pIC50 85 and FGFR4 pIC50 825 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 45 18 and 45 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 Fexagratinib   1035270-39-3 AZD4547 is a selective FGFR inhibitor targeting FGFR123 with IC50 of 02 nM25 nM18 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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