KRAS G12C inhibitor 11 ( —— )

产品货号. M13445 CAS No. 2158297-63-1

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

KRAS G12C inhibitor 11
注意事项

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
产品简述

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。
产品描述

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.
体外实验

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.
体内实验

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同义词

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通路

MAPK/ERK Signaling
靶点

Ras
受体

Ras
研究领域

——
适应症

——

CAS Number

2158297-63-1
分子量

551.695
分子式

C32H37N7O2
纯度

>98% (HPLC)
溶解度

——
SMILES

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

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

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

计算器

产品手册

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1-AM

一种有效、选择性、共价 KRAS G12C 抑制剂，可在亚微摩尔浓度下选择性抑制 KRAS G12C 依赖性信号传导和癌细胞生长。
K-Ras G12C-IN-3

突变型 K-ras G12C 的新型不可逆抑制剂。