Sapitinib (AZD-8931) [CAS 848942-61-0] - ChemeGen-活性小分子-抑制剂-激动剂

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Sapitinib (AZD-8931) [CAS 848942-61-0]

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产品详情

Cat. No.：	C100301	Chinese Name：	沙普替尼
CAS：	848942-61-0	Formula：	C23H25ClFN5O3
MWt：	473.93	Purity：	≥98%
Solubility：	DMSO	Storage：	Powder -20°C 3 years; 4°C 2 years In solvent -80°C 6 months;-20°C 1 month
Research Area：	Cancer	Target：	IC50: 14 nM (HER2), 12 nM (EGFR)[3]
Description：	Sapitinib is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3, exhibiting inhibitory activity against HER2 and EGFR with IC50 14 and 12 nM, respectively.

[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.

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