Synonym
AZD0530 Difumarate; AZD 0530 Difumarate; AZD-0530 Difumarate; Saracatinib difumarate
IUPAC/Chemical Name
4-Quinazolinamine, N-(5-chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methyl-1- piperazinyl)ethoxy)-5-((tetrahydro-2H-pyran-4-yl)oxy)-, (2E)-2-butenedioate (1:2)
InChi Key
OQXMMAQEMJUIQM-LVEZLNDCSA-N
InChi Code
InChI=1S/C27H32ClN5O5.2C4H4O4/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22;2*5-3(6)1-2-4(7)8/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31);2*1-2H,(H,5,6)(H,7,8)/b;2*2-1+
SMILES Code
CN1CCN(CCOc2cc(OC3CCOCC3)c4c(Nc5c(Cl)ccc6OCOc56)ncnc4c2)CC1.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
774.18
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: Huang RY, Wong MK, Tan TZ, Kuay KT, Ng AH, Chung VY, Chu YS, Matsumura N, Lai HC, Lee YF, Sim WJ, Chai C, Pietschmann E, Mori S, Low JJ, Choolani M, Thiery JP. An EMT spectrum defines an anoikis-resistant and spheroidogenic intermediate mesenchymal state that is sensitive to e-cadherin restoration by a src-kinase inhibitor, saracatinib (AZD0530). Cell Death Dis. 2013 Nov 7;4:e915. doi: 10.1038/cddis.2013.442. PubMed PMID: 24201814; PubMed Central PMCID: PMC3847320.
2: de Wispelaere M, LaCroix AJ, Yang PL. The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J Virol. 2013 Jul;87(13):7367-81. doi: 10.1128/JVI.00632-13. Epub 2013 Apr 24. PubMed PMID: 23616652; PubMed Central PMCID: PMC3700292.
3: Gangadhar TC, Clark JI, Karrison T, Gajewski TF. Phase II study of the Src kinase inhibitor saracatinib (AZD0530) in metastatic melanoma. Invest New Drugs. 2013 Jun;31(3):769-73. doi: 10.1007/s10637-012-9897-4. Epub 2012 Nov 15. PubMed PMID: 23151808; PubMed Central PMCID: PMC3600382.
