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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 |
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