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 小时）显着降低新鲜分离的白血病细胞中组蛋白 H3 磷酸化形式的表达^[1]。
Barasertib-羟基喹唑啉吡唑苯胺 (HQPA)] 在血浆中快速转化为活性 Barasertib-HQPA^[2]。
Barasertib-HQPA 会诱导显着的抗增殖作用，并伴有多倍体群体的出现，这在大多数情况下会导致细胞凋亡^[3]。

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

Barasertib（AZD1152，25 mg/kg）显着抑制 AZD1152 二盐酸盐治疗的肿瘤的生长和重量^[1]。
Barasertib（AZD1152，5 mg/kg）增强长春新碱或柔红霉素抑制人 MOLM13 白血病异种移植物增殖的能力^[1]。
Barasertib（AZD1152，10-150 mg/kg/d）有效抑制免疫缺陷小鼠中人结肠、肺和血液肿瘤异种移植物的生长（平均肿瘤生长抑制范围，55% 至 z100%；P < 0.05）^[2]。

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

660.46

C₂₆H₃₃Cl₂FN₇O₆P

722543-50-2

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]