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AZD1152-HQPA
- AZD 2811 - Defosbarasertib - Barasertib-HQPA
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C26H30FN7O3
- MW: 507.56
Description
AZD1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases. The dihydrogen phosphate prodrug, AZD1152 (Barasertib), is converted rapidly to active AZD1152-HQPA in plasma.
More Information
| Parent CAS No. | 722544-51-6 |
|---|---|
| Chemical Name | 2-[5-(7-{3-[Ethyl-(2-hydroxy-ethyl)-amino]-propoxy}-quinazolin-4-ylamino)-1H-pyrazol-3-yl]-N-(3-fluoro-phenyl)-acetamide |
| SMILES | OCCN(CC)CCCOC1C=C2N=CN=C(NC3NN=C(C=3)CC(=O)NC3=CC=CC(F)=C3)C2=CC=1 |
| MFCD | MFCD10687152 |
| InChi | InChI=1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33) |
| InChiKey | QYZOGCMHVIGURT-UHFFFAOYSA-N |
| CID | 16007391 |
| Short Description | Aurora B inhibitor |
References
- RW Wilkinson et al. AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis. Clin. Cancer Res. 2007 13(12), 3682-3688.
- E Walsby et al. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica 2008, 93(5), 662-669.
- Y Tao et al. Enhancement of radiation response in p53-deficient cancer cells by the Aurora-B kinase inhibitor AZD1152. Oncogene 2008, 27, 3244-3255.
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