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AZD1152-HQPA

Cat. No. M1663
AZD1152-HQPA Structure
Synonym:

Barasertib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 48  USD48 In stock
10mg USD 70  USD70 In stock
50mg USD 270  USD270 In stock
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Quality Control & Documentation
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.

Product Citations
Customer Product Validations & Biological Datas
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).
Protocol (for reference only)
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
Chemical Information
Molecular Weight 507.56
Formula C26H30FN7O3
CAS Number 722544-51-6
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Hartsink-Segers et al. Leukemia. Aurora kinases in childhood acute leukemia: the promise of Aurora B as therapeutic target.

[2] Xu et al. PLoS One. Characterizing tumor response to chemotherapy at various length scales using temporal diffusion spectroscopy.

[3] Dennis et al. Cancer Chemother Pharmacol. Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia.

[4] Schwartz et al. Invest New Drugs. Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors.

[5] Löwenberg et al. Blood. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia.

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  Catalog
Abmole Inhibitor Catalog




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


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