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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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