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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]
High-throughput screening identifies Aurora kinase B as a critical therapeutic target for Merkel cell carcinoma [ Nat Commun, 2025, 16(1):1583] | PubMed: 39939315 |
Unraveling AURKB as a potential therapeutic target in pulmonary hypertension using integrated transcriptomic analysis and pre-clinical studies [ Cell Rep Med, 2025, 6(2):101964] | PubMed: 39933527 |
Identification of chemical inhibitors targeting long noncoding RNA through gene signature-based high throughput screening [ Int J Biol Macromol, 2025, 292:139119] | PubMed: 39722392 |
Oversized cells activate global proteasome-mediated protein degradation to maintain cell size homeostasis [ Elife, 2025, 14e75393] | PubMed: 39791360 |
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 |
WEE1 confers resistance to KRASG12C inhibitors in non-small cell lung cancer [ Cancer Lett, 2024, 611:217414] | PubMed: 39725152 |
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 |
New Fusarochromanone Derivatives from the Marine Fungus Fusarium equiseti UBOCC-A-117302 [ Mar Drugs, 2024, 22(10)444] | PubMed: 39452852 |
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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.