ChemicalBook CAS DataBase List 1879965-80-6

1879965-80-6

Name	E7090 succinate
CAS	1879965-80-6
Molecular Formula	C36H43N5O10
Molecular Weight	705.77
MOL File	1879965-80-6.mol

Chemical Properties

storage temp.	Store at -20°C
form	Solid
color	White to off-white

Hazard Information

Uses

E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively[1].

in vivo

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner. Overall, the in vitro and in vivo studies confirm that E7090 is a potent and selective FGFRs inhibitor, showing promising antitumor activities with wider therapeutic windows in preclinical cancer models harboring FGFRs gene abnormalities^[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)

storage

Store at -20°C

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

Supplier

Send Inquriy