AZD1152_722543-31-9_DataSheet_MedChemExpress

Product Name:

AZD1152CAS No.:

722543-31-9

Product Data Sheet

Cat. No.:

HY-10127MWt:

587.54Formula:

C26H31FN7O6P Purity :

>98%

Solubility:Mechanisms:

Biological Activity:

Pathways:Cell Cycle/DNA Damage; Target:Aurora Kinase

DMSO > 80 mg/ml Water

g y 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 References:

[1]. Ron J. Keizer, Anthe S. Zandvliet,Jos H. Beijnen et al. Two-stage model-based design of cancer phase I dose escalation trials: evaluation using the phase I program of barasertib (AZD1152).Invest

New Drugs. 2012 August; 30(4): 1519-1530.[2]. Bob L?wenberg, Petra Muus , Gert Ossenkoppele et al. Phase 1/2 study to assess the safety,p y gp p p y p

sensitive to barasertib-hQPA induced pHH3 inhibition (p = <0.001) than samples without these transporters. IC50inhibition of pHH3 by barasertib-h...

[]g pp y y efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid

leukemia .Blood December 1, 2011 vol. 118 no. 23 6030-6036[3]. Martin Grundy, Claire Seedhouse , Nigel H Russell et al.P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the Aurora-B Kinase Inhibitor

barasertib-hQPA. BMC Cancer 2011, 11:254[4]. Gary K. Schwartz & Richard D. Carvajal et al. Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients ...

Caution: Not fully tested. For research purposes only

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