产品
编 号：F746319
分子式：C23H23Cl2N5O5
分子量：520.37
分子式：C23H23Cl2N5O5
分子量：520.37
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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结构图
CAS No: 1628793-01-0
产品详情
生物活性：
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.
体内研究：
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.FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model.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.Animal Model:Hep3B cell bearing mice model
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; twice daily; 28 days
Result:Resulted in tumor regression and sustained growth inhibition.
Animal Model:Sorafenib-resistant tumors established to mice bearing Huh7 tumors
Dosage:10, 30, and 100 mg/kg
Administration:Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result:Resulted in dose-dependent growth inhibition of resistant tumors.
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.
体内研究：
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.FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model.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.Animal Model:Hep3B cell bearing mice model
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; twice daily; 28 days
Result:Resulted in tumor regression and sustained growth inhibition.
Animal Model:Sorafenib-resistant tumors established to mice bearing Huh7 tumors
Dosage:10, 30, and 100 mg/kg
Administration:Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result:Resulted in dose-dependent growth inhibition of resistant tumors.
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