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Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit , VEGFR-2 and PDGFRβ with IC 50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
In Vitro
Famitinib inhibits the VEGF-induced proliferation, migration and tubule formation of human umbilical vein endothelial cells, and micro-vessel spouting from matrigel-embedded rat aortic rings. Famitinib (1.8 and 3.6 μM; 48 h) inhibits cell proliferation by inducing cell cycle arrest at the G2/M phase and causes cell apoptosis in a dose-dependent manner in gastric cancer cell lines. Famitinib (0.6-20.0 µM; 24-72 h) inhibits gastric cancer cell growth in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Human gastric cancer cells BGC-823 and MGC-803 Concentration: 0, 0.6, 1.25, 2.5, 5.0, 10.0 and 20.0 µM Incubation Time: 24, 48 and 72 hours Result: Inhibited cell growth in a dose-dependent manner with IC 50 values of 3.6 and 3.1 µM for BGC-823 and MGC-803 cells, respectively.
In Vivo
Famitinib exhibits broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines . Famitinib (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenograftsDosage: 50 and 100 mg/kg Administration: Oral gavage; 50 and 100 mg/kg; once daily for 3 weeks Result: Inhibited BGC-823 xenograft growth (tumor volume, 395.2 vs. 2,690.5 mm 3 ), and animal weights were similar between groups (21.6 vs. 18.7 g).
Form:Solid