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Barasertib-HQPA

MCE China：Barasertib-HQPA

Brand：MedChemExpress (MCE)

Cat. No.HY-10126

CAS：722544-51-6

Synonyms：AZD2811; INH-34; AZD1152-HQPA

Purity：99.47%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.

In Vitro：Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells[1]. Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is converted rapidly to the active Barasertib-HQPA in plasma[2]. Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line[3]. Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis[4].

In Vivo：Barasertib-HQPA (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors[1]. Barasertib-HQPA (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1]. Barasertib-HQPA (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P [2].

IC50 & Target：Aurora B 0.37 nM (IC50)

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References：

[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.  [Content Brief]

[2]. 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.  [Content Brief]

[3]. 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.  [Content Brief]

[4]. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8.  [Content Brief]