Tasurgratinib (E7090) | FGFR inhibitor | Probechem Biochemicals

Chemical Structure : E7090

CAS No.: 1622204-21-0

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E7090 (Tasurgratinib, E-7090)

货号: PC-35144Not For Human Use, Lab Use Only.

E7090 (Tasurgratinib) is a potent, selective, orally available inhibitor of FGFR1, -2, and -3 with IC50 of 0.71, 0.50 and 1.2 nM, weakly inhibits FGFR4 (IC50=120 nM).

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生物&药学活性

E7090 (Tasurgratinib) is a potent, selective, orally available inhibitor of FGFR1, -2, and -3 with IC50 of 0.71, 0.50 and 1.2 nM, weakly inhibits FGFR4 (IC50=120 nM).
E7090 inhibits only 3 tyrosine kinases (RET, DDR2, and FLT1) with IC50 lower than 10 nM among the 93 kinases, also potently inhibits mutant FGFR3 (K650E and K650M, IC50=3.1 and 16 nM).
E7090 inhibits FGFR phosphorylation and cell proliferation of SNU-16 cells with IC50 of 1.2 and 5.7 nM, respectively.
E7090 shows selective antiproliferative activity against cancer cell lines harboring FGFR abnormalities.
E7090 exhibits antitumor activity and inhibits FGFR signaling in a mouse xenograft model of SNU-16 human gastric cancer.

物理化学性质&存储条件

分子量	587.677
分子式	C32H37N5O6
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamido)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide

参考文献

1. Watanabe Miyano S, et al. Mol Cancer Ther. 2016 Nov;15(11):2630-2639.

E7090 (Tasurgratinib, E-7090)

生物&药学活性

物理化学性质&存储条件

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E7090 (Tasurgratinib, E-7090)

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