Toggle Nav

Barasertib (AZD1152-HQPA)

In stock
Catalog No.
A4112
Aurora Kinase B inhibitor, Potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$85.00
In stock
10mg
$145.00
In stock
50mg
$470.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Reference

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

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt507.56
Cas No.722544-51-6
FormulaC26H30FN7O3
SynonymsAZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34
Solubility≥25.4 mg/mL in DMSO, <2.27 mg/mL in EtOH, <2.28 mg/mL in H2O
Chemical Name2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide
SDFDownload SDF
Canonical SMILESCCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Protocol

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

Applications

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

Applications

In SW620, HCT116 and Colo205 xenografts significant tumor growth inhibitions of 79% (P

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.

References:

[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.

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          

Quality Control

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)