AZD1152(Barasertib)

AZD1152 is a selective inhibitor of Aurora B with Ki of 0.36 nM.

AZD1152(Barasertib) Chemical Structure

AZD1152(Barasertib) Chemical Structure

CAS No. 722543-31-9

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AZD1152(Barasertib) Related Products

Biological Activity

Description AZD1152 is a selective inhibitor of Aurora B with Ki of 0.36 nM.
Features Selectivity for Aurora-B over Aurora-A.
Targets
Aurora B [1]
0.36 nM
In vitro
In vitro AZD1152 is a pro-drug converting to active substance AZD1152-HQPA in human plasma. AZD1152 inhibits Aurora-A, Aurora B-INCENP, and Aurora C-INCENP with Kis of 687 nM, 0.36 nM, and 17.0 nM, indicating a 100-fold selectivity for Aurora-B over Aurora-A. [1] AZD1152 results in a dose-dependent inhibition of histone H3 phosphorylation on Ser10 in SW620 colorectal tumor cell line. [2] AZD1152 induces growth arrest of a variety of types of leukemia cells, with IC50 of 5, 12, and 8 nM for ALL PALL-2, MOLM13, MV4-11 respectively. [3]
Kinase Assay Affinity determination
AZD1152 are incubated with Aurora A or Aurora B-INCENP and the substrate peptide. Twenty microliters of reaction mix (25 mM Tris-HCl, 12.7 mM KCl, 2.5 mM NaF, 0.6 mM dithiothreitol, 6.25 mM MnCl2, 7.5μM ATP for Aurora A assay and 15 μM for Aurora B-INCENP assay, 6.25 μM peptide substrate containing 0.2 μCi [γ33P]ATP) is then added to all test wells to start the reaction (to give a final volume of 50 μL). Plates are incubated at room temperature for 60 min, reactions are stopped by addition of 100 μL of 20% v/v orthophosphoric acid, and peptide substrate is captured on positively charged nitrocellulose P30 filtermat using a 96-well plate harvester and then assayed for incorporation of 33P with a Beta plate counter.
Cell Research Cell lines ALL PALL-2; MOLM13; MV4-11 cells
Concentrations ~100 nM
Incubation Time 48 h
Method Leukemic cells are grown in liquid culture for 2 days in the presence of various concentrations of AZD1152-HQPA (1-100 nM). Growth inhibition is measured by thymidine uptake; the percent inhibition is graphed and the concentration of AZD1152-HQPA that induced 50% growth inhibition (IC50) of leukemia cells is determined.
In Vivo
In vivo AZD1152 (2.5 mg/kg/d) significantly suppresses PhH3 by 69% in SW620 colon tumors. AZD1152 (10-150 mg/kg/d) inhibits growth in a panel of human tumor xenografts including Colo205 , A549, and HL-60 with inhibition rate ranging from 55% to 100%. Additional results show cells exposed to AZD1152 end up apoptosis.[2] AZD1152 (25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors in MOLM13 xenografts. [3]
Animal Research Animal Models Male nude mice bearing SW620, Colo205, A549, and HL-60 human tumor xenografts.
Dosages 2.5-150 mg/kg
Administration i.v. i.p. s.c.

Chemical Information & Solubility

Molecular Weight 587.54 Formula

C26H31FN7O6P

CAS No. 722543-31-9 SDF --
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (170.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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