Bioactivity | 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]. |
Target | IC50: 0.37 nM (Aurora B) |
Invitro | 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. 0 --> Barasertib dihydrochloride 相关抗体: |
In Vivo | 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 [2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 722543-50-2 |
Formula | C26H33Cl2FN7O6P |
Molar Mass | 660.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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 [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. [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. |