產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
K-Ras(G12C) inhibitor 9 | 5mg 25mg | 1469337-91-4 | EY-Y0164538 |
Cas No.1469337-91-4
別名
化學(xué)名 N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide
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
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)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.
關(guān)鍵字： 1469337-91-4;C16H21ClIN3O4S;K-Ras(G12C) inhibito;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來(lái)，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運(yùn)用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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