Famitinib(Synonyms: 法米替尼; SHR1020)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Famitinib (Synonyms: 法米替尼; SHR1020)

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(Synonyms: 法米替尼; SHR1020)

Famitinib Chemical Structure

CAS No. : 1044040-56-3

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生物活性

Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively[1]. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis[2].

IC50 & Target[2]

VEGFR-2

4.2 nM (IC50)

PDGFRβ

6.6 nM (IC50)

c-kit

2.3 nM (IC50)

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 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) inhibits gastric cancer cell growth in a dose-dependent manner[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

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. The IC50 values in BGC-823 and MGC-803 cells were 3.6 and 3.1 µM, respectively.

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 significantly slows tumor growth in vivo via inhibition of angiogenesis in BGC-823 xenograft models. Famitinib (50 and 100 mg/kg;gavage) reduces xenograft growth in vivo via inhibition of angiogenesis[2].

Shanghai Jinpan Biotech Co Ltd 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 xenografts[4]
Dosage: 50 and 100 mg/kg
Administration: Gavage, once daily for 3 weeks
Result: Both doses exerted a similar inhibitory power, but greater toxicity was observed.
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).

分子量

410.48

Formula

C23H27FN4O2
CAS 号

1044040-56-3
中文名称

法米替尼
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.
参考文献

  • [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.

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