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K-Ras(G12C)inhibitor 9
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。
K-Ras(G12C)inhibitor 9图片
CAS NO:1469337-91-4
包装与价格：
包装价格(元)
5mg电议
25mg电议

产品介绍
K-Ras (G12C) inhibitor 9 是 K-Ras (G12C) 的变构抑制剂。
Cas No.1469337-91-4
化学名N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide
Canonical SMILESC=CS(NC1CCN(C(CNC2=C(OC)C=C(Cl)C(I)=C2)=O)CC1)(=O)=O
分子式C16H21ClIN3O4S
分子量513.78
溶解度DMF: 14 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 12 mg/ml
储存条件Store at -20℃
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

Target: K-Ras(G12C)

IC50: N/A

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C) [1]. Ras proteins belong to the large family of GTPase enzymes which are essential to transduce extracellular signals into diverse cellular responses including proliferation, differentiation, and apoptosis. About 30% of all human cancers contain activating Ras mutations, making them one of the most common known genetic molecular drivers of cancer [2]. Therefore, K-Ras signaling have potential therapeutic advantages in cancer. K-Ras(G12C) is present in roughly 10–20% of Ras-driven cancers and in an estimated 50% of Ras-mutated lung adenocarcinomas [3].

In vitro: K-Ras(G12C) inhibitor 9 belongs to a series of small molecules, which irreversibly compete with GTP and GDP for binding to a common oncogenic K-Ras(G12C) mutant and blocked the association of B-Raf and C-Raf with K-Ras(G12C). K-Ras(G12C) inhibitor 9 (10 μM) decreased viability and increased apoptosis of G12C mutations-containing lung cancer cell lines (H1792, Calu-1, H358, and H23) [1].

In vivo: N/A

References:
1.  Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013;503(7477):548-51.
2.  Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, et al. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014;111(24):8895-900.
3.  Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014;53(1):199-204.