Chemical Structure : KRAS G12C inhibitor compound 8
CAS No.:
3023465-19-9
KRAS G12C inhibitor compound 8
货号: PC-25991Not For Human Use, Lab Use Only.
KRAS G12C inhibitor compound 8 is a potent, specific KRAS G12C dual inhibitor with IC50 of 10 nM (GDP Exchange Inhibition) and 133 nM (RAS/RAF Disruption), covalently modifies both KRAS G12C inactive and active states.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
KRAS G12C inhibitor compound 8 is a potent, specific KRAS G12C dual inhibitor with IC50 of 10 nM (GDP Exchange Inhibition) and 133 nM (RAS/RAF Disruption), covalently modifies both KRAS G12C inactive and active states.
Compound 8 is a rapid inhibitor of both the GDP-bound inactive state KRAS G12C (kinact/KI >79,000 M-1s-1) and GMPPNP-bound active state KRAS G12C (kinact/KI >8,000 M-1s-1).
Compound 8 shows comparable pERK potency (IC50: 0.4 nM) to divarasib (IC50: 0.3 nM).
Compound 8 inhibits cellular proliferation in MIA PaCa-2, a KRAS G12C mutant cell line, with IC50 of 1.6 nM.
Compound 8 shows robust and potent activity in a panel of KRAS G12C mutant cell lines with cell line sensitivity profile similar to KRAS G12C inactive state-selective inhibitor divarasib.
Compound 8 showsselectivity for the Cys12 of KRAS G12C over the majority of other peptides identified, including Cys 80 of KRAS and NRAS.
(150 mg/kg twice daily (BID)) demonstated tumor growth inhibition of 88% in KRASG12C-mutant NSCLC patient derived xenograft (PDX) model.
物理化学性质&存储条件
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分子量
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689.74
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分子式
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C39H34F3N7O2
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(Z)-1-(4-(7-(8-ethynylnaphthalen-1-yl)-8-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)pyrido[4,3-d]pyrimidin-4-yl)piperazin-1-yl)-2-fluoro-3-(pyridin-2-yl)prop-2-en-1-one
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参考文献
1. Condakes ML, et al. Nat Commun. 2026 Jan 31. doi: 10.1038/s41467-026-69003-0.
