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FGFR (Fibroblast growth factor receptor),a kind of glycoproteins with extracellular immunoglobulin (Ig)-like domains, which consists of five members FGFR-1, FGFR-2, FGFR-3, FGFR-4 and FGFR-5 are tyrosine kinase receptors which mediate signaling from their high-affinity ligands, fibroblast growth factors (FGFs). Active FGFRs stimulate tyrosine phosphorylation and activation of a number of signaling molecules: Shc, PI3K, SRC, PLC, Crk, SH2 domain containing phosphatase-2 (SHP-2), p38, STAT1/3 and FGFR substrate2 (FRS2). Phosphorylation of the docking protein FRS2 recruits and activates the Grb2/Sos1 complex, which then interacts with Ras to activate the MAPK pathway.
| Cat.No. | Product Name | Information | Publication | Customer Review |
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| S2183 | BGJ398 (NVP-BGJ398) | BGJ398 (NVP-BGJ398) is a potent and selective inhibitor of FGFR1, FGFR2 and FGFR3 with IC50 of 0.9 nM, 1.4 nM and 1 nM, respectively. |
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| S2801 | AZD4547 | AZD4547 is a novel selective FGFR inhibitor targeting FGFR1, FGFR2, and FGFR3 with IC50 of of 0.2 nM, 2.5 nM, and 1.8 nM, respectively. |
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| S1010 | BIBF1120 (Vargatef) | BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
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| S1264 | PD173074 | PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM. |
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| S1107 | Danusertib (PHA-739358) | Danusertib (PHA-739358) is an Aurora inhibitor for Aurora A/B/C, Bcr-Abl, c-RET and FGFR with IC50 of 13 nM/79 nM/61 nM, 25 nM, 31 nM and 47 nM, respectively. |
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| S1018 | Dovitinib (TKI-258) | Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively. |
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| S1470 | TSU-68 (SU6668) | TSU-68 (SU6668, Orantinib) is a potent inhibitor of Flk-1/KDR, FGFR1 and PDGFRβ with Ki of 2.1 μM, 1.2 μM, and 8 nM, respectively. |
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| S8024 | Tyrphostin AG 1296 (AG 1296) | Tyrphostin AG 1296 (AG 1296) is an inhibitor of PDGFR, FGFR and c-Kit with IC50 of < 1 μM, 12.3 μM and 1.8 μM, respectively. |
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| S2774 | MK-2461 | MK-2461 is a potent inhibitor of c-Met, Ron, Flt1/3, PDGFRβ, Mer and FGFR1/2/3 with IC50 of 2.5 nM, 7 nM, 10 nM/22 nM, 22 nM, 24 nM and 65 nM/39 nM/50 nM, respectively. |
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| S1138 | Brivanib alaninate (BMS-582664) | BMS-582664 is an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1 and FGFR1 with IC50 of 25 nM, 89 nM, 380 nM and 148 nM, respectively. |
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| S1084 | Brivanib (BMS-540215) | Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively. |
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