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Kobe0065

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产品名称: Kobe0065
产品型号: GOY-Y2391
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-04-27

简单介绍

Kobe0065≥ 23.85mg/mL in DMSO


Kobe0065  的详细介绍

性能参数

产品名称

Kobe0065

规格

1mg

货号

GOY-Y2391

 含量

>98.00%

CAS

Cas No. 436133-68-5

别名

 

 

 

化学名

N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide

分子式

C15H11ClF3N5O4S

分子量

分子量 449.79

溶解度

≥ 23.85mg/mL in DMSO

储存条件

Store at -20°C

General tips

 

用途

仅供科研

价格

电询

详细内容

Kobe0065 is a small-molecule inhibitor of Ras with Ki value of 46 μM for the binding of H-Ras.GTP to c-Raf-1 [1].

Kobe0065 is a compound screened out by an in silico screen method as a potent inhibitor of the Ras–Raf interaction. It showed favorite efficacy to inhibit the binding of M-Ras.GTP and H-Ras.GTP to the Ras-binding domain of c-Raf-1. Kobe0065 also dose-dependently inhibited the binding of H-RasG12V to c-Raf-1 in NIH 3T3 cells with a rough IC50 value of 10 μM. Besides that, 20 μM of Kobe0065 effectively suppressed the phosphorylation of down-stream kinases of Raf, including MEK and ERK. In NIH 3T3 cells transfected with H-rasG12V, Kobe0065 inhibited the colony formation with IC50 value of 0.5 μM. Kobe0065 also showed effect on other cancer cells carrying activated ras oncogenes, such as PANC-1(K-rasG12V), HT1080 (N-rasQ61L) and HCT116 (H-rasG13D). Moreover, in mice bearing SW480 xenografts, administration of Kobe0065 resulted in 40-50% inhibition of the tumor growth at dose of 80 mg/kg. This effect turned to be more distinct when the dose was up to 160 mg/kg [1].

 

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