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Barasertib-HQPA

Catalog No. T2602   CAS 722544-51-6
Synonyms: 1H-Pyrazole-3-acetamide, Barasertib, AZD1152-HQPA, AZD2811, AZD1152-HQPA|AZD2811

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Barasertib-HQPA Chemical Structure
Barasertib-HQPA, CAS 722544-51-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 61.00
25 mg In stock $ 118.00
50 mg In stock $ 233.00
100 mg In stock $ 432.00
500 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.29%
Purity: 98.46%
Purity: 98.43%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.
Targets&IC50 Aurora B:0.37 nM (cell free)
In vitro AZD1152 inhibited the proliferation of AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells with an IC50 ranging from 3 nM to 40 nM [1]. AZD1152-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of AZD1152-HQPA decreased expression of AR [2].
In vivo AZD1152 inhibited the proliferation of AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells with an IC50 ranging from 3 nM to 40 nM [1]. AZD1152-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of AZD1152-HQPA decreased expression of AR [2]. AZD1152 potently inhibited the growth of human colon, lung, and hematologic tumor xenografts in immunodeficient mice. In colorectal SW620 tumor-bearing athymic rats treated i.v. with AZD1152, transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells [3].
Cell Research LNCaP cells were cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum, in 5 % CO2 at 37 °C. The cells were treated with 5, 10, 50, 100, and 500 nM of AZD1152-HQPA for 48 h. After 48-h treatment with AZD1152-HQPA, cells were further incubated with 100 μl of MTT (0.5 mg/ml) at 37 °C for 2 h. Precipitated formazan was solubilized with 100 μl of DMSO, and the optical densitometry was measured at a wavelength of570 nm. Cell treated with 0.1 % DMSO was defined as the control group [2].
Animal Research Female immune-deficient BALB/c nude mice at 4 weeks of age were maintained in pathogen-free conditions with irradiated chow. Animals were bilaterally, subcutaneously injected with 2 × 10^6 MOLM13 cells/tumor in 0.1 mL Matrigel. When MOLM13 cells formed palpable tumors, mice were divided randomly into control (n=5) and treatment groups (n=5), and treatment was begun. AZD1152 (5 or 25 mg/kg) with or without vincristine (0.2 mg/kg) was given to mice by intraperitoneal injection 4 times a week or every another day, respectively. Daunorubicin (1 mg/kg) was given to mice by intraperitoneal injection 6 times during 2 weeks of treatment either alone or in combination with AZD1152 (5 mg/kg). The dose of these agents was determined by our preliminary studies (data not shown). Control diluent was given to the untreated control mice. Body weight and tumors were measured twice a week. Tumor sizes were calculated by the formula: a × b × c, where "a" is the length, "b" is the width, and "c" is the height in millimeters. At the end of the experiment, animals were killed by CO2 asphyxiation and tumor weights were measured after their careful resection. Tumor tissue was collected for analysis [1].
Synonyms 1H-Pyrazole-3-acetamide, Barasertib, AZD1152-HQPA, AZD2811, AZD1152-HQPA|AZD2811
Molecular Weight 507.56
Formula C26H30FN7O3
CAS No. 722544-51-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3 mg/mL (5.91 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 94 mg/mL (185.2 mM)

TargetMolReferences and Literature

1. Yang, Jing., 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 Sep 15;110(6):2034-40. 2. Zekri A, et al. AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Tumour Biol. 2015 Feb;36(2):623-32. 3. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. 5. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin[J]. European Journal of Pharmaceutical Sciences. 2021: 105786.

TargetMolCitations

1. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin. European Journal of Pharmaceutical Sciences. 2021: 105786. 2. Qi J, Gao X, Zhong X, et al. Selective inhibition of Aurora A and B kinases effectively induces cell cycle arrest in t(8;21) acute myeloid leukemia. Biomedicine & Pharmacotherapy. 2019, 117: 109113. 3. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Kinase Inhibitor Library Epigenetics Compound Library ReFRAME Related Library Bioactive Compounds Library Max Fluorochemical Library Preclinical Compound Library

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Keywords

Barasertib-HQPA 722544-51-6 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase colon Inhibitor 1H-Pyrazole-3-acetamide Barasertib BarasertibHQPA AZD 2811 AZD1152-HQPA cancer INH 34 AZD1152-HQPA|AZD 2811 leukemia breast inhibit AZD1152-HQPA|AZD-2811 AZD2811 lung INH-34 AZD1152-HQPA|AZD2811 AZD-2811 INH34 Barasertib HQPA inhibitor

 

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