產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
ARS-853 | 1mg 5mg 10mg 25mg 50mg | 1629268-00-3 | EY-Y0165159 |
Cas No.1629268-00-3
別名 N/A
化學(xué)名 N/A
分子式 C22H29ClN4O3
分子量 432.94
溶解度 DMSO : ≥ 71 mg/mL (164.00 mM)
儲存條件 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：
ARS-853 is a selective, covalent KRASG12C inhibitor with an IC50 of 2.5 uM.
ARS853 is designed to bind KRASG12C with high affinity. Treatment of KRASG12C-mutant lung cancer cells with ARS853 reduces the level of GTP-bound KRAS by more than 95% (10 uM). ARS853 inhibits proliferation with an inhibitory concentration 50% (IC50) of 2.5 uM, which is similar to its IC50 for target inhibition. ARS853 (10 uM) inhibits effector signaling and cell proliferation to varying degrees in six KRASG12C mutant lung cancer cell lines, but not in non-KRASG12C models. Similarly, it completely suppresses the effects of exogenous KRASG12C expression on KRAS-GTP levels, KRAS-BRAF interaction, and ERK signaling. ARS-853 treatment also induces apoptosis in four KRASG12C mutant cell lines. ARS853 selectively reduces KRAS-GTP levels and RAS-effector signaling in KRASG12C-mutant cells, while inhibiting their proliferation and inducing cell death[1]. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation[2].
References:
[1]. Lito P, et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism. Science. 2016 Feb 5;351(6273):604-8.
[2]. Patricelli MP, et al. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State. Cancer Discov. 2016 Mar;6(3):316-29.
關(guān)鍵字： 1629268-00-3;C22H29ClN4O3;ARS-853;
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，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。
公司具有對普通貨物、冷藏及冷凍倉庫的存儲、包裝及運輸能力。
公司將始終堅持信譽立業(yè)、以人為本、質(zhì)量保證、誠信服務(wù)的宗旨，不斷拼搏，開拓進取，與各界朋友攜手共創(chuàng)美好未來。