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Cat. No. Name Size Price Add Cart
KI0401AZD1152-HQPA10 mg$336

Chemical Characteristic

Product NameAZD1152-HQPA
SynonymsBarasertib
CAS No.722544-51-6
Molecular Weight 507.56
FormulaC26H30FN7O3
Chemical Name2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide
Smiles[nH]1nc(cc1Nc1ncnc2c1ccc(c2)OCCCN(CCO)CC)CC(=O)Nc1cc(ccc1)F
Chemical Structure

Biological activities

AZD1152-HQPA is a specific inhibitor of the enzymatic activity of Aurora kinase. AZD1152-HQPA inhibits Aurora B and A kinases with IC50 values of 0.37 nM and 1.37 μM, respectively. AZD1152-HQPA has even less activity against a panel of greater than 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152-HQPA inhibits Philadelphia chromosome-positive ALL PALL-2, acute monocytic leukemia MOLM13, and biphenotypic leukemia MV4-11 cells with IC50s of approximately 5, 12, and 8 nM, respectively. AZD1152-HQPA also inhibits the clonogenic growth of MOLM13 and MV4-11cells with IC50s of 1 and 2.8 nM, respectively. Besides, AZD1152-HQPA blocks phosphorylation of histone H3 in leukemia cells and increases the population of cells with 4N/8N DNA content. [1] In vitro, addition of AZD1152-HQPA to tumor cells induces chromosome misalignment, prevents cell division, consequently reduces cell viability and induces apoptosis. Meanwhile, exposure of human SW620 colorectal tumor cells to AZD1152-HQPA results in a dose-dependent inhibition of histone H3 phosphorylation on Ser10. [2] AZD1152-HQPA at concentrations as low as 0.01 µM produces a significant decrease in the ability of NB4 cells to proliferate by 48 hours, and the other cell lines (HL-60, NB4R2, K562, KG1 and U937) also show reduced proliferative capacity following treatment with AZD1152-HQPA.[3] AZD1152-HQPA inhibits the phosphorylation of Histone H3 (pHH3) on serine 10 resulting in polyploid cells, apoptosis, and loss of viability in a panel of AML cell lines.[4] In vivo, AZD1152-HQPA (25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors compared with control mice, and none of the mice shows signs of wasting or other toxicity.[1]

Protocols

AZD1152-HQPA is dissolved in 100% DMSO to a stock concentration of 10 mM and stored at -80°C. [1]

References

[1] Yang J, et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007, 110: 2034-2040.
[2] Robert W, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007, 13: 3682-3688.
[3] Elisabeth W, 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.
[4] Martin G, et al. The FLT3 internal tandem duplication mutation is a secondary target of the Aurora B kinase inhibitor AZD1152-HQPA in acute myelogenous leukemia cells. Mol Cancer Ther. 2010, 9: 661-672.

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