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
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Famitinib
CAS number：1044040-56-3 molecular formula：C23H27FN4O2
overview
compound introduction
Specs
| Chinese alias | 法米替尼 | ||
| English alias | - | ||
| CAS number | 1044040-56-3 | molecular formula | C23H27FN4O2 |
| molecular weight | 410.48 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
