pan-HER-IN-1 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

pan-HER-IN-1

pan-HER-IN-1 (Compound C5) 是一种不可逆的、具有口服活性的广谱 HER 抑制剂。对 EGFR、HER4、EGFR^T790M/L858R 和 HER2 的 IC₅₀ 分别为 0.38、1.6、2.2 和 3.5 nM。pan-HER-IN-1 诱导细胞凋亡 (apoptosis)，表现出抗肿瘤活性。

pan-HER-IN-1 Chemical Structure

CAS No. : 1639040-94-0

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生物活性

pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC₅₀ values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR^T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities^[1].

IC₅₀ & Target

EGFR

0.38 nM (IC₅₀)

HER4

1.6 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

2.2 nM (IC₅₀)

HER2

3.5 nM (IC₅₀)

分子量

408.25

Formula

C₁₉H₁₄BrN₅O

CAS 号

1639040-94-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Tang Q, et al. Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. Eur J Med Chem. 2022 Apr 5;233:114249.

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