KRAS G12C inhibitor 11

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KRAS G12C 抑制剂 11 是一种有效的、选择性的、共价的、不可逆的 KRAS G12C 抑制剂。

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; demonstrates super proportional dose ascending oral exposure in mice with 3h target coverage at the 30 mg/kg dose; shows rapid growth inhibition and durable efficacy even after dosing was stopped, orally active.

Kirsten Rat Sarcoma 2 Viral Oncogene Homolog (KRas) is a small GTPase and a member of the Ras family of oncogenes. KRas serves a molecular switch cycling between inactive (GDP -bound) and active (GTP -bound) states to transduce upstream cellular signals received from multiple tyrosine kinases to downstream effectors to regulate a wide variety of processes, including cellular proliferation.

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MAPK/ERK Signaling

Ras

Ras

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2158297-63-1

551.695

C32H37N7O2

>98% (HPLC)

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CN1CCCC1COC2=NC3=C(CCN(C3)C4=CC=CC5=CC=CC=C54)C(=N2)N6CCN(C(C6)CC#N)C(=O)C=C

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

(-20℃)

With Ice Pack

≥ 2 years