ARS-853

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Chemical Structure| 1629268-00-3 同义名 : -
CAS号 : 1629268-00-3
货号 : A502082
分子式 : C22H29ClN4O3
纯度 : 99%+
分子量 : 432.94
MDL号 : MFCD30532658
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(57.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 ARS-853 is a selective, covalent inhibitor of KRAS G12C, featuring an IC50 of 2.5 μM. By attaching to the GDP-bound form of the mutant KRAS oncoprotein, ARS-853 blocks its activation, thereby inhibiting KRAS-driven signaling pathways[1].[2].
作用机制 ARS-853 covalently inhibits KRAS G12C and targets the GDP-bound, inactives state and prevents subsequent activation.[1][2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.55mL

2.31mL

1.15mL

23.10mL

4.62mL

2.31mL
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.