| Hazard Information | Back Directory | [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 |
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