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AZD1152-HQPA

Cat. No. M1663

AZD1152-HQPA Structure

Synonym: Barasertib

Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 330 In stock
100mg USD 580 In stock
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Quality Control
Biological Activity

AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM  for Aurora B and Aurora A respectively.Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumor cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis.

Protocol
Cell Experiment
Cell lines HL-60 and U937 cells line
Preparation method Proliferation assay.
To evaluate the growth inhibition effects, the sodium 3′-(1-[(phenylamino)-carbonyl-3,4-tetrazolium])-bis (4-methoxy-6-nitro) benzene sulfonic acid hydrate (XTT) assay was performed according to the manufacturer’s instructions (Roche, Indianapolis, IN, USA) with slight modifications.Roche, Indianapolis, IN, USA) with slight modifications. Cell cycle distribution. Flow cytometric analysis was performed to evaluate the cell cycle distribution. The treated samples were fixed in 80% ethanol, stained with 20 lg ⁄mL propidium iodide (Beckman Coulter, Fullerton, CA, USA), and analyzed using FACSCanto II (BD Bioscience, Franklin Lakes, NJ, USA).
Concentrations 25 nM
Incubation time 0 h, 24 h, 48 h, and 72 h
Animal Experiment
Animal models SW620, Colo205, HCT116 human colorectal tumor xenografts in nude mice
Formulation in Tris buffer pH 9.0
Dosages 150 mg/kg/day
Administration subcutaneous infusion
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 507.56
Formula C26H30FN7O3
CAS Number 722544-51-6
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validation
Source Journal of Hematology & Oncology (2017). Figure 7. AZD1152-HQPA (Abmole Bioscience)
Method CCK8 assay
Cell Lines U251, U87 and U118 cell lines
Concentrations
Incubation Time 48 h
Results Treatment with two other aurora kinase inhibitors, AZD1152 and MLN8237, demonstrated similar results (Fig. 7d).
Rating
Product Citations
References

Aurora kinases in childhood acute leukemia: the promise of Aurora B as therapeutic target.
Hartsink-Segers et al. Leukemia. 2012 Sep 3. PMID: 22940834.

Characterizing tumor response to chemotherapy at various length scales using temporal diffusion spectroscopy.
Xu et al. PLoS One. 2012;7(7):e41714. PMID: 22911846.

Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia.
Dennis et al. Cancer Chemother Pharmacol. 2012 Sep;70(3):461-9. PMID: 22864876.

Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors.
Schwartz et al. Invest New Drugs. 2012 Jun 2. PMID: 22661287.

Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia.
Löwenberg et al. Blood. 2011 Dec 1;118(23):6030-6. PMID: 21976672.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD1152-HQPA, Barasertib supplier, Aurora Kinase, inhibitors

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