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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-KRAS G12C inhibitor 11
KRAS G12C inhibitor 11

Chemical Structure : KRAS G12C inhibitor 11

CAS No.: 2158297-63-1

KRAS G12C inhibitor 11

货号: PC-35953Not For Human Use, Lab Use Only.

KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM.

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

    生物&药学活性

    KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM.
    KRAS G12C inhibitor 11 demonstrates super proportional dose ascending oral exposure in mice with 3h target coverage at the 30 mg/kg dose.
    KRAS G12C inhibitor 11 shows rapid growth inhibition and durable efficacy even after dosing was stopped, orally active.

    物理化学性质&存储条件

    分子量 551.695
    分子式 C32H37N7O2
    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)-1-acryloyl-4-(2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-7-(naphthalen-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile

    参考文献

    1. U.S. Pat. Appl. Publ. (2018), US 20180072723 A1 20180315.

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