Sapitinib fumarate  (Synonyms: AZD-8931 fumarate)

Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

706.07

C₃₁H₃₃ClFN₅O₁₁

1196531-39-1

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Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [4]. Wang R, et al. Endothelial Cells Promote Colorectal Cancer Cell Survival by Activating the HER3-AKT Pathway in a Paracrine Fashion. Mol Cancer Res. 2018 Aug 21. pii: molcanres.0341.2018.  [Content Brief]