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kobe2602
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。
kobe2602图片
CAS NO:454453-49-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议

产品介绍
Kobe2602 是一种 Ras-Raf 相互作用抑制剂。 Kobe2602 抑制 H-Ras.GTP 与 c-Raf-1 RBD 的结合，Ki 为 149 μM。 Kobe2602 具有抗肿瘤活性。
Cas No.454453-49-7
化学名2-(2,6-dinitro-4-(trifluoromethyl)phenyl)-N-(4-fluorophenyl)hydrazinecarbothioamide
Canonical SMILESFC1=CC=C(NC(NNC2=C([N+]([O-])=O)C=C(C(F)(F)F)C=C2[N+]([O-])=O)=S)C=C1
分子式C14H9F4N5O4S
分子量419.31
溶解度≥ 17mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Kobe2602 is a small-molecule inhibitor of Ras with Ki value of 149 μM [1].

Kobe2602 is a compound screened out by a computer-assisted search of about 160,000 compounds. It dose-dependently inhibited the binding of H-RasG12V to c-Raf-1 in NIH 3T3 cells with a rough IC50 value of 10 μM. 20 μM of Kobe2602 effectively suppressed the phosphorylation of down-stream kinases of Raf, including MEK and ERK. Besides that, in NIH 3T3 cells transfected with H-rasG12V, Kobe2602 inhibited the colony formation with IC50 value of 1.4 μM. Kobe2602 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 Kobe2602 resulted in 40-50% inhibition of the tumor growth at dose of 80 mg/kg [1].

References:
[1] Shima F, Yoshikawa Y, Ye M, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras–effector interaction. Proceedings of the National Academy of Sciences, 2013, 110(20): 8182-8187.