Cas No.: | 1622204-21-0 |
Chemical Name: | Tasurgratinib |
Synonyms: | E7090|E 7090 |
Formula: | C32H37N5O6 |
M.Wt: | 587.677 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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 TumorsPhase 1 Clinical |