1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

AZD1152-HQPA (Synonyms: Barasertib; AZD1152)

Cat. No.: HY-10126 Purity: 99.59%
Data Sheet SDS Handling Instructions

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

For research use only. We do not sell to patients.
AZD1152-HQPA Chemical Structure

AZD1152-HQPA Chemical Structure

CAS No. : 722544-51-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $67 In-stock
5 mg $60 In-stock
10 mg $80 In-stock
50 mg $320 In-stock
100 mg $590 In-stock
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500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

IC50 & Target

IC50: 0.37 nM (Aurora B)

In Vitro

AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[2]. AZD1152-HQPA treatment induces defective cell survival, polyploidy, and cell death in LNCaP cell line. AZD1152-HQPA also decreases expression of AR[3].

In Vivo

AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[1]. Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[2]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00530699 AstraZeneca Acute Myeloid Leukaemia November 2007 Phase 1
NCT01354392 Oxford University Hospitals NHS Trust|The Christie NHS Foundation Trust|University of Manchester|Early Phase Cancer Research Hub, Oxford Lymphoma September 2011 Phase 1|Phase 2
NCT00338182 AstraZeneca Tumors May 23, 2006 Phase 1
NCT00497991 AstraZeneca Myeloid Leukemia May 2006 Phase 1
NCT00926731 AstraZeneca Acute Myeloid Leukemia June 2009 Phase 1
NCT01019161 AstraZeneca Acute Myeloid Leukaemia November 2009 Phase 1
NCT00952588 AstraZeneca Acute Myeloid Leukemia July 2009 Phase 2|Phase 3
NCT00497679 AstraZeneca Solid Tumours August 2006 Phase 1
NCT00497731 AstraZeneca Solid Tumors May 2005 Phase 1
NCT00530699 AstraZeneca Acute Myeloid Leukaemia November 2007 Phase 1
NCT01354392 Oxford University Hospitals NHS Trust|The Christie NHS Foundation Trust|University of Manchester|Early Phase Cancer Research Hub, Oxford Lymphoma September 2011 Phase 1|Phase 2
NCT00338182 AstraZeneca Tumors May 23, 2006 Phase 1
NCT00497991 AstraZeneca Myeloid Leukemia May 2006 Phase 1
NCT00926731 AstraZeneca Acute Myeloid Leukemia June 2009 Phase 1
NCT01019161 AstraZeneca Acute Myeloid Leukaemia November 2009 Phase 1
NCT00952588 AstraZeneca Acute Myeloid Leukemia July 2009 Phase 2|Phase 3
NCT00497679 AstraZeneca Solid Tumours August 2006 Phase 1
NCT00497731 AstraZeneca Solid Tumors May 2005 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9702 mL 9.8511 mL 19.7021 mL
5 mM 0.3940 mL 1.9702 mL 3.9404 mL
10 mM 0.1970 mL 0.9851 mL 1.9702 mL
Cell Assay
[2]

Cells are exposed to various concentrations of AZD1152 for 24 or 48 hours. Cell proliferation is measured by 3H-thymidine uptake (isotope added 6 hours before harvest), and the concentration that induced 50% growth inhibition (IC50) is calculated from dose-response curves. Cell cycle analysis is performed by flow cytometry. Cell apoptosis is measured by annexin V–FITC apoptosis detection kit. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Human tumor xenografts are established by s.c. injecting 100 to 200 μL tumor cells (between 1×106 and 1×107 cells mixed 50:50 with Matrigel) on the flank. Animals are randomized into treatment groups (n=8-11 per group) when tumors reach a defined palpable size (0.2-0.3 cm3 and 0.5-1 cm3 for mice and rats, respectively). AZD1152 is prepared in Tris buffer (pH 9) and administered either as a bolus injection (i.v. or i.p.) or as a continuous 48-h infusion via s.c. implanted osmotic mini-pumps (two 24-h pumps implanted sequentially) in accordance with the manufacturer's instructions. Tumors are measured up to three times weekly with calipers, tumor volumes are calculated, and the data are plotted using the geometric mean for each group versus time. Tumor volume and tumor growth inhibition are calculated. Statistical analysis of any change in tumor volume is carried out using a Student's one-tailed t test (P value of <0.05 is considered to be statistically significant). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

507.56

Formula

C₂₆H₃₀FN₇O₃

CAS No.

722544-51-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.59%

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AZD1152-HQPA
Cat. No.:
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