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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-ASP6918
ASP6918

Chemical Structure : ASP6918

CAS No.: 2242418-18-2

ASP6918 (ASP 6918, ASP-6918)

货号: PC-21640Not For Human Use, Lab Use Only.

ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.
ASP6918 potently inhibits cell growth of NCI-H1373 cell line with IC50 of 6.1 nM.
ASP6918 induces significant suppression of ERK phosphorylation at doses of 40 and 60 mg/kg in an NCI-H1373 xenograft mouse model.
ASP6918 (10-60 mg/ kg, p.o.) exhibits antitumor growth inhibition and regression in an NCI-H1373 xenograft mouse model.

物理化学性质&存储条件

分子量 621.79
分子式 C36H43N7O3
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

(+)-1-(7-{8-ethoxy-7-(5-methyl-1H-indazol-4-yl)-2-[(1-methylpiperidin-4-yl)oxy]-6-vinylquinazolin-4-yl}-2,7-diazaspiro[3.5]non-2-yl)prop-2-en-1-one

参考文献

1. Tomoyoshi Imaizumi, et al. Bioorg Med Chem. 2023 Dec 27:98:117581.

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