FGFR4-IN-5 是一种有效的选择性共价 FGFR4 抑制剂，IC₅₀ 为 6.5 nM。FGFR4-IN-5 具有较强的抗肿瘤活性，可用于肝癌研究。

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.

Solid

FGFR4 6.5 nM (IC50) FGFR2 505 nM (IC5

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.
has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[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.

In Vitro: DMSO : 100 mg/mL (192.17 mM; Need ultrasonic)配制储备液