Sapitinib (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.
Product Specifications
CAS Number
1196531-39-1
Product Name Alternative
AZD-8931 (fumarate)
UNSPSC
12352005
Hazard Statement
H302-H360-H372
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/sapitinib-fumarate.html
Smiles
OC(/C=C/C(O)=O)=O.COC(C(OC1CCN(CC1)CC(NC)=O)=C2)=CC3=C2C(NC4=C(C(Cl)=CC=C4)F)=NC=N3.OC(/C=C/C(O)=O)=O
Molecular Formula
C31H33ClFN5O11
Molecular Weight
706.07
Precautions
P260-P264-P270-P280-P330-P405-P501
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
Scientific Category
Reference compound1
Clinical Information
Phase 2
Frequently Asked Questions
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