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Sapitinib

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Chemical Structure| 848942-61-0 同义名 : 沙匹替尼 ;AZD8931
CAS号 : 848942-61-0
货号 : A258461
分子式 : C23H25ClFN5O3
纯度 : 99%+
分子量 : 473.928
MDL号 : MFCD18385011
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(73.85 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 5 mg/mL suspension

生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:4 nM

  • ErbB3

    ErbB3, IC50:4 nM

  • HER2/ErbB2

    ErbB2, IC50:3 nM

  • HER2

    ErbB2, IC50:3 nM
描述 AZD8931 exhibits potent inhibitory activity against erbB2 in the ligand-independent MCF-7 cl24 cells, with an IC50 of 59 nM [1]. AZD8931 (1 μM) does not notably alter EGFR expression levels but markedly suppresses Akt phosphorylation in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. Furthermore, AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells [2]. At the cellular level, AZD8931 suppresses EGF-induced phosphorylation of EGFR in the KB cell line (IC50: 4 nM) and heregulin-induced phosphorylation of HER2 (IC50: 3 nM) and HER3 (IC50: 4 nM) in the MCF-7 cell line. However, AZD8931 does not inhibit CYP P450 enzymes (IC50 > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4) [3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human KB cells Function assay Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells, IC50=4 nM 24900741
human MCF7 cells Function assay Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells, IC50=3 nM 24900741
human MCF7 cells Function assay Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells, IC50=4 nM 24900741
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.55mL

2.11mL

1.06mL

21.10mL

4.22mL

2.11mL
参考文献

[1]Hickinson DM, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010 Feb 15;16(4):1159-69.

[2]Mu Z, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor (EGFR), HER2, and HER3: preclinical activity in HER2 non-amplified inflammatory breast cancer models. J Exp Clin Cancer Res. 2014 May 30;33:47.

[3]Barlaam B, et al. Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. ACS Med Chem Lett. 2013 May 31;4(8):742-6.