| 溶解性 | DMSO > 80 mg/ml Water |
| 存贮条件 | 储存温度-20°C |
| 生化机理 | AZD1152 (barasertib) is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML). The MTDs （the maximum-tolerated dose ） were 150 mg as a 48-h continuous infusion and 220 mg administered as two 2-h infusions (110 mg/day, days 1, 2, 15 and 16), with neutropenia the dose-limiting toxicity (DLT) of each schedule. Common Terminology Criteria of Adverse Events The pharmacokinetic (PK), metabolic and excretion profiles of barasertib and barasertib-hQPA were characterized in this open-label Phase I study. Pgp and BCRP positive primary samples were less sensitive to barasertib-hQPA induced pHH3 inhibition (p = <0.001) than samples without these transporters. IC50inhibition of pHH3 by barasertib-hQPA was achieved in 94.6% of these samples after 1 hour drug treatment, in contrast to the resistance of the cell lines. Common Terminology Criteria of Adverse Events (CTCAE) grade?≥?3 neutropenia (with or without fever) occurred in 34 % of patients overall. Barasertib-hQPA was extensively distributed to tissues, with a slow rate of total clearance (CL = 31.4 L/h). Overall, 72-82 % of radioactivity was recovered, with approximately double the amount recovered in feces (mean = 51 %) compared with urine (mean = 27 %). |
AZD1152
AZD1152 （订货以英文为准）
编号：A126951
CAS号：722543-31-9
分子式：C26H31FN7O6P
分子量：587.54
| 产品名称 | AZD1152 |
| 中文名称 | AZD1152 |
| CAS号 | 722543-31-9 |
| 分子式（M.F.） | C26H31FN7O6P |
| 分子量（M.W.） | 587.54 |
| 储存条件 | -20°C储存 |
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