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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-D3S-001
D3S-001

Chemical Structure : D3S-001

CAS No.: 2914919-85-8

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D3S-001 (Elisrasib)

货号: PC-24126Not For Human Use, Lab Use Only.

Elisrasib (D3S-001) is a potent, selective, CNS-penetrable, covalent inhibitor of GDP-bound KRAS G12C inhibitor, decreases cellular active KRAS proteins in a dose-dependent manner (IC50=0.6 nM) in NCI-H358 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Elisrasib (D3S-001) is a potent, selective, CNS-penetrable, covalent inhibitor of GDP-bound KRAS G12C inhibitor, decreases cellular active KRAS proteins in a dose-dependent manner (IC50=0.6 nM) in NCI-H358 cells.
D3S-001 is 58- and 130-fold more potent than sotorasib and adagrasib, respectively.
D3S-001 exhibits irreversible binding to GDP-bound KRAS G12C protein and limited or no binding to GTP-bound KRAS G12C protein.
D3S-001 demonstrates IC50 values of 0.5 and 0.3 nmol/L in NCI-H358 and MIA PaCa2 cells, respectively, which is a 38 to 86-fold increase in potency when compared with sotorasib or adagrasib.
D3S-001 inhibits cell growth with a median IC50 of 4.35 nmol/L in KRAS G12C-mutant cell lines, and a median IC50 > 10 μmol/L in cell lines without KRAS G12C mutation, D3S-001 exhibits high KRAS G12C allele-selective activity with markedly higher potency and selectivity compared with sotorasib and adagrasib.
D3S-001 (3, 10, 30, and 100 mg/kg, QD) inhibited KRAS signaling and tumor growth in NCI-H358 xenograft models, inhibited the phosphorylation of ERK1/2 and RSK.

物理化学性质&存储条件

分子量 679.67
分子式 C32H35F6N7O3
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

2-((S)-4-((S)-7-(3-amino-2-fluoro-5-methyl-6-(trifluoromethyl)phenyl)-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile

参考文献

1. Jing Zhang, et al. Cancer Discov. 2024 Sep 4;14(9):1675-1698.

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