WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 575209
CAS#: 1196531-39-1 (fumurate)
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#: 575209
Name: Sapitinib fumurate
CAS#: 1196531-39-1 (fumurate)
Chemical Formula: C31H33ClFN5O11
Exact Mass: 705.1849
Molecular Weight: 706.08
Elemental Analysis: C, 52.73; H, 4.71; Cl, 5.02; F, 2.69; N, 9.92; O, 24.92
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Synonym: Sapitinib fumurate; Sapitinib difumurate; AZD8931; AZD8931; AZD 8931; Sapitinib;
IUPAC/Chemical Name: 1-Piperidineacetamide, 4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxy-6-quinazolinyl)oxy)-N-methyl-, (2E)-2-butenedioate (1:2)
InChi Key: LSXKPHWAKWZIKV-LVEZLNDCSA-N
InChi Code: InChI=1S/C23H25ClFN5O3.2C4H4O4/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;2*5-3(6)1-2-4(7)8/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29);2*1-2H,(H,5,6)(H,7,8)/b;2*2-1+
SMILES Code: CNC(=O)CN1CCC(CC1)Oc2cc3c(Nc4cccc(Cl)c4F)ncnc3cc2OC.OC(=O)\C=C\C(=O)O.OC(=O)\C=C\C(=O)O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 706.08 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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, CasÃ¡s-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.