|1-(3-(4-(2-((4-氯-2-羟基-5-(1-甲基环丙基)苯基)氨基)乙酰基)-1-哌嗪基)-1-氮杂环丁基)-2-丙烯-1-酮|CsnPharm

CAS No.: 1629268-00-3

ARS-853 is an inhibitor of KRAS G12C with IC50 of 2.5 μM.

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400-920-2911

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描述ARS-853 is a mutant-specific and covalent KRAS^G12C inhibitor with IC50 value of 1.6μM for H358 cellular engagement. ARS-853 is covalently attached to C12 and extends into the Switch II pocket region located between the central beta-sheet of KRAS and the α 2 and α 3 helices, thus triggering interference with GTP binding, stabilization of bound Mg 2+ /GDP, and/or blocking activator and/or effector binding in the Switch II region. Treatment with ARS-853 at concentration<10μM for 24h dose-dependently disrupted the critical interaction of active KRAS with its effector protein CRAF in H358 cells but A549 cells, accompanied with inhibition of the downstream signaling through both MAPK (including pMEK, pERK, and pRSK) and PI3K signaling (pAKT) pathways, G 1 cell-cycle arrest, loss of Cyclin D1 and Rb expression, and an increase in the cell-cycle inhibitor p27 KIP1. Cell lines with KRAS^G12C were robustly inhibited by ARS-853 in soft-agar colony formation assays with an average IC50 value of ∼ 2 μM.
作用机制ARS-853 covalently inhibits KRAS G12C and targets the GDP-bound, inactives state and prevents subsequent activation.^[1]^[2]
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实验方案

技术信息

CAS号

1629268-00-3

储存条件

分子式

C22H29ClN4O3

运输

蓝冰

分子量

432.94

别名

溶解度

DMSO	78.0 mg/mL (180.2 mM)
Water	insoluble

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