ARS-853

    
98%

ARS-853

源叶(MedMol)
S81384 一键复制产品信息
1629268-00-3
C22H29ClN4O3
432.9437
货号 规格 价格 上海 北京 武汉 南京 购买数量
S81384-1mg 98% ¥188.00 4 - - -
S81384-5mg 98% ¥560.00 4 - - -
S81384-10mg 98% ¥840.00 4 - - -
S81384-25mg 98% ¥1430.00 7 - - -
S81384-50mg 98% ¥2250.00 货期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation

产品描述: ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation
靶点: KRAS(G12C):2.5 μM (IC50);Apoptosis; Raf; Ras
体外研究: 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 μM). ARS853 inhibits proliferation with an inhibitory concentration 50% (IC50) of 2.5 μM, which is similar to its IC50 for target inhibition. ARS853 (10 μM) 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. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
参考文献: 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.
溶解性: soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.31 ml 11.549 ml 23.098 ml
5 mM 0.462 ml 2.31 ml 4.62 ml
10 mM 0.231 ml 1.155 ml 2.31 ml
50 mM 0.046 ml 0.231 ml 0.462 ml
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参考文献

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