1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Epertinib

Epertinib (Synonyms: S-22611)

目录号: HY-107367
产品使用指南

Epertinib (S-22261) 是一种有效,可口服,可逆的,选择性的 EGFRHER2HER4 抑制剂,IC50 值分别为 1.48 nM,7.15 nM 和 2.49 nM。Epertinib 具有高效的抗肿瘤活性。

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Epertinib Chemical Structure

Epertinib Chemical Structure

CAS No. : 908305-13-5

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1 mg ¥2200
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Epertinib 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity[1].

IC50 & Target[1]

EGFR

1.48 nM (IC50)

HER2

2.49 nM (IC50)

HER4

7.15 nM (IC50)

体外研究
(In Vitro)

Epertinib (S-22261) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively, and shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells, with IC50s of 4.5 and 1.6 nM, respectively.
Furthermore, Epertinib exhibits inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2, with IC50s of 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))[1].
Epertinib also inhibits MDA-MB-361 cell growth, with an IC50 of 26.5 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Epertinib shows antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days, with an ED50 of 10.2 mg/kg. Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice[1].
Epertinib (50 mg/kg, p.o.) markedly reduces the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model (IVM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

560.02

Formula

C30H27ClFN5O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献

纯度: ≥98.0%

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