Barasertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、高选择性的 Aurora B 抑制剂，IC50 为 0.37 nM；显示出比 Aurora B 激酶高 1,000 倍的选择性。

A potent, highly selective Aurora B inhibitor with IC50 of 0.37 nM; displays >1,000-fold selectivity over Aurora B kinase; induces growth arrest and apoptosis in human acute leukemia cells in vitro and in vivo.Blood Cancer Phase 2 Discontinued.

Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells.Barasertib-hydroxyquinazoline pyrazol anilide (HQPA)] is converted rapidly to the active Barasertib-HQPA in plasma.Barasertib-HQPA is used for the in vitro experiments.Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis.

Barasertib (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors.Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts.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. Animal Model:Female immune-deficient BALB/c nude mice (MOLM13 cells injected).Dosage:5 or 25 mg/kg.Administration:Intraperitoneal injection 4 times a week or every another day.Result:Inhibited the growth of human MOLM13 cells growing as xenografts using an immunodeficient murine model.

AZD-1152 | AZD1152

Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

Cancer

Blood cancer

722543-31-9

587.5398

C26H31FN7O6P

>98% (HPLC)

DMSO: ≥ 33 mg/mL

O=P(O)(OCCN(CC)CCCOC1=CC2=NC=NC(NC3=NNC(CC(NC4=CC=CC(F)=C4)=O)=C3)=C2C=C1)O

1H-Pyrazole-3-acetamide, 5-[[7-[3-[ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years