Famitinib (SHR1020) malate 是一种有效的，具有口服活性的多靶点激酶抑制剂，抑制c-kit，VEGFR-2和PDGFRβ的活性，IC50值分别为 2.3 nM、4.7 nM 和 6.6 nM。Famitinib malate 诱导细胞凋亡 (apoptosis)。Famitinib malate 具有抗肿瘤活性，可用于癌症的研究。
| 生物活性 | Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity ofc-kit,VEGFR-2andPDGFRβwithIC50values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cellapoptosis. Famitinib malate exerts powerful antitumor activity in human gastriccancercells and xenografts, it can be used for the research ofcancer[1][2]. |
| IC50& Target | VEGFR2 4.2 nM (IC50) | PDGFRβ 6.6 nM (IC50) | c-kit 2.3 nM (IC50) |
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体外研究
(In Vitro) | Famitinib malate 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[1].
Famitinib malate (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[2].
Famitinib malate (0.6-20.0 μM; 24-72 h) inhibits gastric cancer cell growth in a dose-dependent manner[2].
Cell Proliferation Assay[2] | Cell 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 IC50values of 3.6 and 3.1 μM for BGC-823 and MGC-803 cells, respectively. |
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体内研究
(In Vivo) | Famitinib malate exhibits broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines[1].
Famitinib malate (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis[2].
| Animal Model: | 18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenografts[2] | | Dosage: | 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 mm3), and animal weights were similar between groups (21.6 vs. 18.7 g). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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