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Infigratinib(BGJ-398;NVP-BGJ398)对FGFR家族具有强效抑制作用,对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为0.9 nM、1.4 nM、1 nM和60 nM。
Nintedanib(BIBF 1120)是一种强效的三重血管激酶抑制剂,对VEGFR1/2/3、FGFR1/2/3和PDGFRα/β的IC50值分别为34 nM、13 nM、13 nM、69 nM、37 nM、108 nM、59 nM和65 nM。
AZD-4547(Fexagratinib ; ADSK091) 是一种有效的FGFR家族抑制剂,对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为0.2 nM、2.5 nM、1.8 nM和165 nM。
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.
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.
FGFR-IN-1 is a potent and highly selective FGFR inhibitor, used for antitumor treatment.
ASP5878 是一种口服活性的 FGFR 1、2、3 和 4 的抑制剂,IC50 值分别为 0.47 nM、0.6 nM、0.74 nM 和 3.5 nM,具有潜在的抗肿瘤活性。
Derazantinib is a fibroblast growth factor receptor (FGFR) inhibitor that has antitumor activity.
Nintedanib esylate (BIBF 1120 esylate) (BIBF 1120 esylate) 是一种有效的三重血管激酶抑制剂,对VEGFR1/2/3、FGFR1/2/3和PDGFRα/β的IC50值分别为34 nM/13 nM/13 nM、69 nM/37 nM/108 nM和59 nM/65 nM。
PRN1371 is an irreversible covalent FGFR inhibitor used for the treatment of solid tumor.
BLU9931 is an inhibitor of FGFR4 with IC50 of 3 nM and is less potent for FGFR1/2/3 (IC50 > 150 nM).
FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
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.
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.
BO-264 is a highly TACC3 inhibitor with IC50 value of 188nM. It significantly decreased centrosomal TACC3 during both mitosis and interphase, as well as displayed potent anti-proliferative activity (~90% have less than 1μM GI50 value) in the NCI-60 cell line panel compromising nine different cancer types.
Dovitinib is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.
MK-2461 is a potent and multi-targeted inhibitor for c-Met with IC50 of 0.4-2.5 nM, also inhibits FGFR1/2/3, KDR, TrkA/B, and Flt4 with IC50 of 65/39/50 nM, 44 nM, 46/61 nM, and 78 nM respectively.
FIIN-3 is an irreversible inhibitor of FGFR1-4 with IC50s of 13, 21, 31, and 35 nM, respectively.
S49076 is a potent inhibitor of MET, AXL/MER, and FGFRs.
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Tags: FGFR3 | FGFR | FGFR3 相关产品 | FGFR3 基因表达
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