Tasurgratinib(E7090)

  Cat. No.:  DC22085   Featured
Chemical Structure
1622204-21-0
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Field of application
E7090 (E 7090) is a highly potent and selective orally bioavailable inhibitor targeting FGFR1, FGFR2, and FGFR3, with IC50 values of 0.71 nM, 0.50 nM, and 1.2 nM, respectively. It exhibits significantly weaker inhibition of FGFR4, with an IC50 of 120 nM. This distinct selectivity profile positions E7090 as a promising therapeutic candidate for diseases driven by aberrant FGFR1-3 signaling, offering a targeted approach to inhibit these receptors while minimizing off-target effects on FGFR4. Its oral availability further enhances its potential as a convenient and effective treatment option for patients with FGFR-dependent conditions.
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
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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