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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 | Fexagratinib | 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 |