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Barasertib (AZD1152-HQPA)
Aurora Kinase B inhibitor, Potent and selective

Catalog No.A4112
Size Price Stock Qty
10mM (in 1mL DMSO)
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Evaluation Sample
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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Christine M Field, James F Pelletier, et al. "Disassembly of actin and keratin networks by Aurora B kinase at the midplane of cleaving Xenopus laevis eggs." bioRxiv. 2019 January 06.
2.Shodai Tanaka, Kaori Senda-Murata, et al. "Live cell imaging of anaphase bridge formation and the subsequent cleavage furrow regression induced by the Aurora B kinase inhibitor AZD1152-HQPA." Bioimages.2017.10.05.
3.Hanley ML, Yoo TY, et al. "Chromosomal passenger complex hydrodynamics suggests chaperoning of the inactive state by nucleoplasmin/nucleophosmin." Mol Biol Cell. 2017 Apr 12. pii: mbc.E16-12-0860. PMID:28404751

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Chemical structure

Barasertib (AZD1152-HQPA)

Related Biological Data

Barasertib (AZD1152-HQPA)

Related Biological Data

Barasertib (AZD1152-HQPA)

Related Biological Data

Barasertib (AZD1152-HQPA)

Related Biological Data

Barasertib (AZD1152-HQPA)

Related Biological Data

Barasertib (AZD1152-HQPA)

Biological Activity

Description Barasertib (AZD1152-HQPA) is a highly selective inhibitor of Aurora B with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A.
Targets Aurora B          
IC50 0.37 nM          


Cell experiment: [1]

Cell lines

HL-60 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

25 nM, 72 hours


The cells exhibited increased DNA contents of 4N and 8N, indicative of polyploidy, within 24–48 h of treatment. After 48–72 h, barasertib-HQPA induced apoptotic cell death, as detected by an increased sub-G1 population compared for that of untreated cells. The induction of polyploidy was obvious at 24–48 h, and thereafter, the nuclei showed morphology typical of apoptosis, such as nuclear fragmentation and condensation. These observations were in accordance with the findings of the flow cytometric analysis.

Animal experiment: [2]

Animal models

Female nude mice injected with SW620, Colo205 or HCT116 cells

Dosage form

Subcutaneous injection, 150 mg/kg/day, minipump infusion over 48 h


In SW620, HCT116 and Colo205 xenografts significant tumor growth inhibitions of 79% (P<0.001, day 23), 60% (P<0.001, day 25) and 81% (P<0.05, day 21) were observed, respectively. Colo205 xenografts appeared the most sensitive to treatment with a mean tumor volume (± SEM) on day 21 after cell implantation, of 0.42±0.19 cm3 for the barasertib group compared to 2.24±0.75 cm3 (P<0.05) for the vehicle control animals.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Yamauchi T, Uzui K, Shigemi H, et al. Aurora B inhibitor barasertib and cytarabine exert a greater-than-additive cytotoxicity in acute myeloid leukemia cells. Cancer science, 2013, 104(7): 926-933.

[2] Alferez D G, Goodlad R A, Odedra R, et al. Inhibition of Aurora-B kinase activity confers antitumor efficacy in preclinical mouse models of early and advanced gastrointestinal neoplasia. International journal of oncology, 2012, 41(4): 1475-1485.

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Chemical Properties

Cas No. 722544-51-6 SDF Download SDF
Synonyms AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34
Chemical Name 2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide
Formula C26H30FN7O3 M.Wt 507.56
Solubility ≥25.4 mg/mL in DMSO, <2.27 mg/mL in EtOH, <2.28 mg/mL in H2O Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

3. Aurora B inhibitor barasertib and cytarabine exert a greater-than-additive cytotoxicity in acute myeloid leukemia cells. Cancer Sci. 2013 Jul;104(7):926-33. doi: 10.1111/cas.12164. Epub 2013 May 12.
As an active metabolite of Barasertib, barasertib-HQPA is an inhibitor of aurora B that potently inhibited growth of HL cells by inducing polyploidy and apoptosis. In order to provide a greater-than-additive cyctotoxicity to HL cells, barasertib-HQPA must be applied before or concurrently with ara-C.
4. Effect of the drug transporters ABCG2, Abcg2, ABCB1 and ABCC2 on the disposition, brain accumulation and myelotoxicity of the aurora kinase B inhibitor barasertib and its more active form barasertib-hydroxy-QPA. Invest New Drugs. 2013 Oct;31(5):1125-35. doi: 10.1007/s10637-013-9923-1. Epub 2013 Jan 13.
Both barasertib and barasertib-hQPA could be efficiently transported by BCRP and MDR1, in which significant barasertib resistance has been observed. MRP2 neither transported barasertibe nor affected its cytotoxicity.
5. Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors. Invest New Drugs. 2013 Apr;31(2):370-80. doi: 10.1007/s10637-012-9825-7. Epub 2012 Jun 2.
Barasertib, an Aurora B Kinase inhibitor, was generally well tolerated in patients with advanced solid malignancies with MTDs of 150 mg and 220 mg for 48-h continuous infusion and two 2-h infusion respectively, which caused neutropenia as the DLT and mild to modest adverse side effects of hematologic or gastrointestinal etiology.


Barasertib, previously known as AZD1152-hydroxyquinazoline pyrazol anilide (HQPA), is a potent aurora kinase inhibitor, which is resulted from rapid phosphatase-mediated cleavage of the precursor, AZD1152, in serum following parenteral administration in vivo. It shows inhibitory effects against a broad range of aurora kinases, including aurora A kinase (AKB), aurora B kinase (ABK), and aurora C kinase (ACK) with inhibition constant (Ki) of 1369 nM, 0.36 nM, and 17.0 nM respectively, as well as the FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation. Barasertib has demonstrated anti-tumor activity against a range tumor cell lines including those of leukaemic acute myeloid leukemia (AML) origin.


Martin Grundy, Claire Seedhouse, Nigel H Russell and Monica Pallis. P-glycoprotein and breast cancer resistance protein in acyte myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-Hqpa. BMC Cancer 2011, 11:254

Mike Dennis, Michelle Davies, Stuart Oliver, Roy D’Souza, Laura Pike, and Paul Stockman. Phase I study of the aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia. Cancer Chemother Pharmacol (2012) 70:461-469