Sapitinib
Product Specifications
Product Name Alternative
AZD-8931
UNSPSC Description
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
Target Antigen
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Sapitinib.html
Purity
99.93
Solubility
DMSO : ≥ 33 mg/mL
Smiles
O=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC
Molecular Weight
473.93
References & Citations
[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-13050/Sapitinib-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-13050/Sapitinib-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
848942-61-0
Available Sizes
Curated Selection
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