Famitinib 法米替尼; SHR1020|cas:1044040-56-3|西域试剂

Famitinib 法米替尼; SHR1020,98.43%

产品编号：Bellancom-108713| CAS NO：1044040-56-3| 分子式：C₂₃H₂₇FN₄O₂| 分子量：410.48

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-108713		￥6700.00	杭州北京（现货）
Bellancom-108713		￥10700.00	杭州北京（现货）

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Famitinib 法米替尼; SHR1020

产品介绍

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 of c-kit, VEGFR-2 and PDGFRβ with IC₅₀ 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.

体外研究

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.

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

Cell Proliferation Assay

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 IC₅₀ values of 3.6 and 3.1 µM for BGC-823 and MGC-803 cells, 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 .
Famitinib (50 and 100 mg/kg; p.o. once daily for 3 weeks) reduces tumor growth in vivo via inhibition of angiogenesis.

西域 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
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).

体内研究

西域 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
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).

体内研究

西域 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
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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 4.17 mg/mL (10.16 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式