| Identification | Back Directory | [Name]
5-[[7-[3-[Ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-3-acetamide dihydrochloride | [CAS]
722543-50-2 | [Synonyms]
AZD 1152 (hydrochloride)
5-[[7-[3-[Ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-3-acetamide dihydrochloride | [Molecular Formula]
C26H32ClFN7O6P | [MDL Number]
MFCD16620512 | [MOL File]
722543-50-2.mol | [Molecular Weight]
624.01 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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].
| [storage]
-20°C | [References]
[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 DOI:10.1182/blood-2007-02-073700
[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. DOI:10.1158/0008-5472.CAN-08-3203
[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. DOI:10.1158/1078-0432.CCR-06-2979 |
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