E-7090

Product NameE-7090
CAS1622204-21-0
MFC32H37N5O6
MW587.67
EINECS
MOL File1622204-21-0.mol

Chemical Properties

form	Solid
color	White to off-white

Usage And Synthesis

Uses

E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively[1].

in vivo

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner^[1].
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model^[2].

Animal Model:	Mouse xenograft model of SNU-16 human gastric cancer^[2]
Dosage:	6.25 to 50 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

IC 50

FGFR1: 0.71 nM (IC₅₀); FGFR2: 0.50 nM (IC₅₀); FGFR3: 1.2 nM (IC₅₀); FGFR4: 120 nM (IC₅₀)

References

[1] Saori Watanabe Miyano, et al. E7090: A potent and selective FGFR inhibitor with activity in multiple FGFR-driven cancer models with distinct mechanisms of activation. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
[2] Saori Watanabe Miyano, et al. E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models. Mol Cancer Ther. 2016 Nov;15(11):2630-2639. DOI:10.1158/1535-7163.MCT-16-0261