FGFR4-IN-5 |
| Katalog-Nr.GC62602 |
FGFR4-IN-5 ist ein potenter und selektiver kovalenter FGFR4-Inhibitor mit einem IC50 von 6,5 nM. FGFR4-IN-5 weist in vivo eine starke AntitumoraktivitÄt auf und kann fÜr die hepatozellulÄre Karzinomforschung verwendet werden.
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Cas No.: 1628793-01-0
Sample solution is provided at 25 µL, 10mM.
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FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research[1].
FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively[1].FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model[1].FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %δT/δC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo[1].
[1]. Haibo Liu, et al. Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma. ACS Med Chem Lett. 2020 Mar 6;11(10):1899-1904.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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