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Famitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Famitinib图片
CAS NO:1044040-56-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
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-2PDGFRβ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)

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.
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).
Clinical Trial
分子量

410.48

性状

Solid

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
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4362 mL12.1809 mL24.3617 mL
5 mM0.4872 mL2.4362 mL4.8723 mL
10 mM0.2436 mL1.2181 mL2.4362 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。