WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200298
CAS#: 848942-61-0
Description: Sapitinib, also known as AZD-8931, is an erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. erbB kinase inhibitor AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB. The erbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization.
MedKoo Cat#: 200298
Name: Sapitinib (AZD-8931)
CAS#: 848942-61-0
Chemical Formula: C23H25ClFN5O3
Exact Mass: 473.163
Molecular Weight: 473.93
Elemental Analysis: C, 58.29; H, 5.32; Cl, 7.48; F, 4.01; N, 14.78; O, 10.13
Related CAS #: 1196531-39-1 (difumarate)
Synonym: AZD8931; AZD8931; AZD 8931; Sapitinib
IUPAC/Chemical Name: 2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-N-methylacetamide
InChi Key: DFJSJLGUIXFDJP-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
SMILES Code: O=C(NC)CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1
1: Mu Z, Klinowska T, Dong X, Foster E, Womack C, Fernandez SV, Cristofanilli M. 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. doi: 10.1186/1756-9966-33-47. PubMed PMID: 24886365; PubMed Central PMCID: PMC4061513.
2: Singleton KR, Kim J, Hinz TK, Marek LA, Casás-Selves M, Hatheway C, Tan AC, DeGregori J, Heasley LE. A receptor tyrosine kinase network composed of fibroblast growth factor receptors, epidermal growth factor receptor, v-erb-b2 erythroblastic leukemia viral oncogene homolog 2, and hepatocyte growth factor receptor drives growth and survival of head and neck squamous carcinoma cell lines. Mol Pharmacol. 2013 Apr;83(4):882-93. doi: 10.1124/mol.112.084111. Epub 2013 Jan 31. PubMed PMID: 23371912; PubMed Central PMCID: PMC3608435.
3: Hickinson DM, Klinowska T, Speake G, Vincent J, Trigwell C, Anderton J, Beck S, Marshall G, Davenport S, Callis R, Mills E, Grosios K, Smith P, Barlaam B, Wilkinson RW, Ogilvie D. 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. doi: 10.1158/1078-0432.CCR-09-2353. Epub 2010 Feb 9. PubMed PMID: 20145185.