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
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
Preparing Stock Solutions
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, 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.