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AZD0530 difumarate
- Saracatinib difumarate
- Parent CAS: 379231-04-6
- Soluble in DMSO
- MF: C27H32ClN5O5.2C4H4O4
- MW: 774.17
Description
AZD0530 difumarate (Saracatinib difumarate) is an orally active SRC-family and ABL tyrosine kinase inhibitor that suppresses signaling involved in proliferation, adhesion and invasion. It is the preferred fumarate salt of AZD0530 (Axon 3284).
Saracatinib is used to investigate SRC-dependent oncogenic signaling, bone remodeling and resistance to receptor-targeted therapies. The compound also inhibits ABL kinases, which should be considered when interpreting cellular responses.
Key Features
- SRC-family and ABL kinase inhibitor
- Orally active small-molecule tyrosine kinase inhibitor
- Reduces SRC-dependent migration and invasion signaling
- Useful for pathway-resistance and combination studies
Applications
- SRC and ABL kinase assays
- Cancer-cell migration and invasion models
- Bone remodeling and osteoclast signaling studies
- Resistance to receptor tyrosine kinase inhibitors
More Information
| Parent CAS No. | 379231-04-6 |
|---|---|
| Chemical Name | (5-Chloro-benzo[1,3]dioxol-4-yl)-[7-[2-(4-methyl-piperazin-1-yl)-ethoxy]-5-(tetrahydro-pyran-4-yloxy)-quinazolin-4-yl]-amine (2E)-2-butenedioate (1:2) |
| SMILES | C1C(OC2CCOCC2)=C2C(NC3C4OCOC=4C=CC=3Cl)=NC=NC2=CC=1OCCN1CCN(C)CC1.C(/C(O)=O)=CC(O)=O.C(/C(O)=O)=CC(O)=O |
| MFCD | MFCD12546336 |
| InChi | 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+ |
| InChiKey | OQXMMAQEMJUIQM-LVEZLNDCSA-N |
| CID | 44195703 |
| Short Description | Src-Abl inhibitor |
References
- H Laurent et al. N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J. Med. Chem. 2006, 49, 6465.
- YM Chang et al. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene 2008, 1–11.
- PM Gwanmesia et al. The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines. BMC Cancer 2009, 9, 53.
- TP Green et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Molecular Oncology 2009, 3(3), 248-261.
- C Dulsat et al. Saracatinib. Drugs Fut. 2009, 34(2), 106.
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