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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-ARS-1620
ARS-1620

Chemical Structure : ARS-1620

CAS No.: 1698055-85-4

ARS-1620 (ARS1620)

货号: PC-62494Not For Human Use, Lab Use Only.

ARS-1620 is a potent, specific and covalent KRAS G12C inhibitor with an observed rate of 1,100±200 M-1S-1, shows >10-fold improved potency over the initial ARS-853.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ARS-1620 (ARS1620) is a potent, specific and covalent KRAS G12C inhibitor with an observed rate of 1,100±200 M-1S-1, shows >10-fold improved potency over the initial ARS-853.
ARS-1620 inhibits RAS signaling with IC50 of 120 nM, exhibits a half maximal G12C target engagement (TE50) at 0.3 uM and near complete engagement at 3.0 uM across a panel of cell lines harboring the mutant allele.
ARS-1620 achieves rapid and sustained in vivo target occupancy to induce tumor regression, and is a novel generation of KRASG12C-specific inhibitor with promising therapeutic potential.

物理化学性质&存储条件

分子量 430.84
分子式 C21H17ClF2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(4-(6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)quinazolin-4-yl)piperazin-1-yl)prop-2-en-1-one

参考文献

1. Janes MR, et al. Cell. 2018 Jan 25;172(3):578-589.e17.

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