Saracatinib, also known as AZD0530, is an orally available dual-specific inhibitor of Src and Abl with anti-invasive and anti-tumor activities. Src and Abl are protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. Saracatinib binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival.
Chemical Formula: C27H32ClN5O5
Exact Mass: 541.2092
Molecular Weight: 542.03
Elemental Analysis: C, 59.83; H, 5.95; Cl, 6.54; N, 12.92; O, 14.76
Chemical Name: N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
InChi Code: InChI=1S/C27H32ClN5O5/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/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)
Appearance: white 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, not in water
Shelf Life: >2 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
Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM)
Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats).
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.
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.
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.
Nam HJ, Im SA, Oh DY, Elvin P, Kim HP, Yoon YK, Min A, Song SH, Han SW, Kim TY, Bang YJ. Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer. Mol Cancer Ther. 2013 Jan;12(1):16-26. doi: 10.1158/1535-7163.MCT-12-0109. Epub 2012 Nov 9. PubMed PMID: 23144237.
Liu KJ, He JH, Su XD, Sim HM, Xie JD, Chen XG, Wang F, Liang YJ, Singh S, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Wu HY, Fu LW. Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. Int J Cancer. 2013 Jan 1;132(1):224-35. doi: 10.1002/ijc.27649. Epub 2012 Jun 13. PubMed PMID: 22623106; PubMed Central PMCID: PMC3459133.
Products are for research use only. Not for human use.