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.
|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).
|Incubation time||0 h, 24 h, 48 h, and 72 h|
|Animal models||SW620, Colo205, HCT116 human colorectal tumor xenografts in nude mice|
|Formulation||in Tris buffer pH 9.0|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Source||Journal of Hematology & Oncology (2017). Figure 7. AZD1152-HQPA (Abmole Bioscience)|
|Cell Lines||U251, U87 and U118 cell lines|
|Incubation Time||48 h|
|Results||Treatment with two other aurora kinase inhibitors, AZD1152 and MLN8237, demonstrated similar results (Fig. 7d).|
J Hematol Oncol. 2017 Jun 8;10(1):115.
SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B.
AZD1152-HQPA purchased from AbMole
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.
|Related Aurora Kinase Products|
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity.
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1.
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