AZD1152(Barasertib)

Catalog No.S1051 Batch:S105102

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Technical Data

Formula

C26H31FN7O6P
Molecular Weight 587.54 CAS No. 722543-31-9
Solubility (25°C)* In vitro DMSO 118 mg/mL (200.83 mM)
Water 118 mg/mL (200.83 mM)
Ethanol 3 mg/mL (5.1 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
saline
118.000mg/ml (200.84mM) Taking the 1 mL working solution as an example, add 118 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description AZD1152 is a selective inhibitor of Aurora B with Ki of 0.36 nM.
Targets
Aurora B [1]
0.36 nM
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]
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]
Features Selectivity for Aurora-B over Aurora-A.

Protocol (from reference)

Kinase Assay:[4]
  • 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 Assay:[3]
  • 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.
Animal Study:[2]
  • 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.

Selleck's AZD1152(Barasertib) has been cited by 7 publications

Vitamins C and K3: A Powerful Redox System for Sensitizing Leukemia Lymphocytes to Everolimus and Barasertib [Ivanova D, et al. Anticancer Res, 2018, 38(3):1407-1414] PubMed: 29491065
Aurora Kinases as Druggable Targets in Pediatric Leukemia: Heterogeneity in Target Modulation Activities and Cytotoxicity by Diverse Novel Therapeutic Agents [Jayanthan A, et al. PLoS One, 2014, 9(7):e102741] PubMed: 25048812
Dual inhibition of SRC and Aurora kinases induces postmitotic attachment defects and cell death. [Ratushny V, et al. Oncogene, 2012, 31(10):1217-27] PubMed: 21785464
Aurora B is regulated by the mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK) signaling pathway and is a valuable potential target in melanoma cells. [Bonet C, et al. J Biol Chem, 2012, 287(35):29887-98] PubMed: 22767597
Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families [Glaser KB, et al. J Pharmacol Exp Ther, 2012, 343(3):617-27] PubMed: 22935731
Preclinical Characterization of ABT-348, a Kinase Inhibitor Targeting the Aurora, Vascular Endothelial Growth Factor Receptor/Platelet-Derived Growth Factor … [Glaser KB, et al. J Pharmacol Exp Ther, 2012, 343(3):617-27] PubMed: 22935731
Aurora A and Aurora B jointly coordinate chromosome segregation and anaphase microtubule dynamics. [H間arat N, et al. J Cell Biol, 2011, 195(7):1103-13] PubMed: 22184196

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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