Famitinib (SHR1020) 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具有抗肿瘤活性。且诱导细胞凋亡 (apoptosis)。
| 生物活性 | Famitinib (SHR1020), 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[1]. Famitinib exerts powerful antitumor activity in human gastriccancercells and xenografts. Famitinib triggersapoptosis[2]. |
| IC50& Target[2] | VEGFR-2 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 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 (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 (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 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 (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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 4.17 mg/mL(10.16 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.4362 mL | 12.1809 mL | 24.3617 mL | | 5 mM | 0.4872 mL | 2.4362 mL | 4.8723 mL | | 10 mM | 0.2436 mL | 1.2181 mL | 2.4362 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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