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E7090 succinate

Chemical Structure : E7090 succinate

CAS No.: 1879965-80-6

E7090 succinate

Catalog No.: PC-35145Not For Human Use, Lab Use Only.

E7090 (E 7090) 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

E7090 (E 7090) 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); 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); inhibits FGFR phosphorylation and cell proliferation of SNU-16 cells with IC50 of 1.2 and 5.7 nM, respectively; shows selective antiproliferative activity against cancer cell lines harboring FGFR abnormalities, exhibits antitumor activity and inhibits FGFR signaling in a mouse xenograft model of SNU-16 human gastric cancer.

Solid Tumors

Phase 1 Clinical

Physicochemical Properties

M.Wt 705.765
Formula C36H43N5O10
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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 succinate

References

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

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