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)。

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.

Solid

VEGFR-2 4.2 nM (IC50) PDGFRβ 6.6 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Liguang Lou, et al. Abstract 3604: Preclinical antitumor study of famitinib, an orally available multi-targeted kinase inhibitor of VEGFR/PDGFR/c-Kit in phase I clinical trials.
[2]. Sai Ge, et al. Famitinib exerted powerful antitumor activity in human gastric cancer cells and xenografts. Oncol Lett. 2016 Sep;12(3):1763-1768.

In Vitro: DMSO : 4.17 mg/mL (10.16 mM; ultrasonic and warming and heat to 60°C)配制储备液