Barasertib (AZD1152-HQPA)

Catalog No.S1147 Batch:S114709

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Technical Data

Formula

C26H30FN7O3
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)
Clear solution
5% DMSO 95% corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

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.
Targets
Aurora B [1]
(Cell-free assay)
0.37 nM
In vitro

Barasertib (AZD1152-HQPA), a highly selective Aurora B inhibitor, causes polyploidy and apoptosis in many cancer cell lines.[1]
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]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    NCI-H82 cells, SCLC and NSCLC cell lines

  • Concentrations

    --

  • Incubation Time

    --

  • Method

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Customer Product Validation

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]

Selleck's Barasertib (AZD1152-HQPA) has been cited by 156 publications

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
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
Molecular landscape and functional characterization of centrosome amplification in ovarian cancer [ Nat Commun, 2023, 14(1):6505] PubMed: 37845213
Single cell analysis in head and neck cancer reveals potential immune evasion mechanisms during early metastasis [ Nat Commun, 2023, 14(1):1680] PubMed: 36973261
Stage-specific dual function: EZH2 regulates human erythropoiesis by eliciting histone and non-histone methylation [ Haematologica, 2023, 108(9):2487-2502] PubMed: 37021526
Stage-specific dual function: EZH2 regulates human erythropoiesis by eliciting histone and non-histone methylation [ Haematologica, 2023, 108(9):2487-2502] PubMed: 37021526
Mitotic perturbation is a key mechanism of action of decitabine in myeloid tumor treatment [ Cell Rep, 2023, 42(9):113098] PubMed: 37714156

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

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