Barasertib dihydrochloride  (Synonyms: AZD1152 dihydrochloride)

Barasertib (AZD1152 dihydrochloride), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib (AZD1152 dihydrochloride) induces growth arrest and apoptosis in cancer cells^[1].

IC50: 0.37 nM (Aurora B)

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 induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Barasertib (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152 dihydrochloride-treated tumors^[1].
Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts^[1].
Barasertib (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 < 0.05) in immunodeficient mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

660.46

C₂₆H₃₃Cl₂FN₇O₆P

722543-50-2

O=C(CC1=NNC(NC2=C3C=CC(OCCCN(CCOP(O)(O)=O)CC)=CC3=NC=N2)=C1)NC4=CC(F)=CC=C4.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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 Sep  [Content Brief]

  [2]. 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]

  [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.  [Content Brief]