计算溶液所需的质量、体积或浓度。
概述
FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC 50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research
In Vivo
FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high C max , low clearance, the C max 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:FGFR4 6.5 nM (IC 50 ) FGFR2 505 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
FGFR4-IN-5
生化机理
FGFR4-IN-5 是一种强效的选择性共价 FGFR4 抑制剂，IC50 为 6.5 nM。FGFR4-IN-5 在体内具有很强的抗肿瘤活性，可用于肝癌研究。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
520.37
高级数据
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溶液计算器
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