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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-ASP2453
ASP2453

Chemical Structure : ASP2453

CAS No.: 2241719-73-1

ASP2453 (ASP-2453)

货号: PC-72958Not For Human Use, Lab Use Only.

ASP2453 (ASP-2453) is a novel potent, selective and covalent KRAS G12C inhibitor, inhibits SOS-mediated interaction between KRAS G12C and Raf with IC50 of 40 nM.

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

生物&药学活性

ASP2453 (ASP-2453) is a novel potent, selective and covalent KRAS G12C inhibitor, inhibits SOS-mediated interaction between KRAS G12C and Raf with IC50 of 40 nM.
ASP2453 potently and selectively inhibited KRAS G12C-mediated growth, KRAS activation and downstream signalling in vitro and in vivo, and improved the anti-tumour effects of targeted agents and immune checkpoint inhibitors.
ASP2453 had more rapid binding kinetics to KRAS G12C protein and showed more potent inhibitory effects on KRAS activation and cell proliferation after washout than AMG 510.
ASP2453 also induced tumour regression in an AMG 510-resistant xenograft model.

物理化学性质&存储条件

分子量 747.864
分子式 C40H48F3N7O4
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-(6-cyclopropyl-2-((1-(3-methoxypropyl)piperidin-4-yl)oxy)-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)quinazolin-4-yl)-2,7-diazaspiro[3.5]nonan-2-yl)prop-2-en-1-one

参考文献

1. Nakayama A, et al. Br J Cancer. 2022 Mar;126(5):744-753.

2. Sayama H, et al. CPT Pharmacometrics Syst Pharmacol. 2021 Aug;10(8):864-877.

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