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Formula | C26H30FN7O3 |
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Molecular Weight | 507.56 | CAS No. | 722544-51-6 | ||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (197.02 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1. | ||
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Targets |
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In vitro | Barasertib (AZD1152-HQPA), a highly selective Aurora B inhibitor, causes polyploidy and apoptosis in many cancer cell lines.[1] |
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In vivo | Barasertib (AZD1152-HQPA) is an aurora B kinase inhibitor, and has efficacy against RB1 / SCLC cell line xenografts, RB1 / SCLC PDXs, and autochthonous Rb1 / neuroendocrine tumors.[1] |
Cell Assay: |
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Data from [Data independently produced by Nature, 2014, 508(7494), 118-22]
Data from [Data independently produced by J Exp Med, 2014, 10.1084/jem.20141123]
Data from [Oncogene, 2014, 33, 3550-60]
Data from [Oncogene, 2012, 31, 1217–1227]
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] | PubMed: 38262581 |
Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041] | PubMed: 38310113 |
Repurposed AT9283 triggers anti-tumoral effects by targeting MKK3 oncogenic functions in Colorectal Cancer [ J Exp Clin Cancer Res, 2024, 43(1):234] | PubMed: 39164711 |
Inhibition of Aurora B kinase (AURKB) enhances the effectiveness of 5-fluorouracil chemotherapy against colorectal cancer cells [ Br J Cancer, 2024, 10.1038/s41416-024-02584-z] | PubMed: 38287178 |
Chromosomal passenger complex condensates generate parallel microtubule bundles in vitro [ J Biol Chem, 2024, S0021-9258(24)00045-0] | PubMed: 38272221 |
Inhibition of epigenetic and cell cycle-related targets in glioblastoma cell lines reveals that onametostat reduces proliferation and viability in both normoxic and hypoxic conditions [ Sci Rep, 2024, 14(1):4303] | PubMed: 38383756 |
The effects of Aurora Kinase inhibition on thyroid cancer growth and sensitivity to MAPK-directed therapies [ Cancer Biol Ther, 2024, 25(1):2332000] | PubMed: 38521968 |
The effects of Aurora Kinase inhibition on thyroid cancer growth and sensitivity to MAPK-directed therapies [ Cancer Biol Ther, 2024, 25(1):2332000] | PubMed: 38521968 |
Visualization strategies to aid interpretation of high-dimensional genotoxicity data [ Environ Mol Mutagen, 2024, 10.1002/em.22604] | PubMed: 38757760 |
Role of AURKB Inhibition in Reducing Proliferation and Enhancing Effects of Radiotherapy in Triple-Negative Breast Cancer [ Breast Cancer (Dove Med Press), 2024, 16:341-346] | PubMed: 39006183 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.