1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. Barasertib-HQPA

Barasertib-HQPA (Synonyms: AZD2811; INH-34; AZD1152-HQPA)

Cat. No.: HY-10126 Purity: 99.64%
Handling Instructions

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay, and shows 3700-fold selectivity for Aurora B over Aurora A.

For research use only. We do not sell to patients.

Barasertib-HQPA Chemical Structure

Barasertib-HQPA Chemical Structure

CAS No. : 722544-51-6

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10 mM * 1 mL in DMSO USD 56 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 70 In-stock
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50 mg USD 290 In-stock
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100 mg USD 520 In-stock
Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

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Description

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay, and shows 3700-fold selectivity for Aurora B over Aurora A.

IC50 & Target[1]

Aurora B

0.37 nM (IC50)

In Vitro

Barasertib-HQPA (AZD2811) displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM.Barasertib-HQPA (AZD2811) has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. Barasertib-HQPA (AZD2811) 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. Barasertib-HQPA (AZD2811) 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. Barasertib-HQPA (AZD2811) induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[2]. Barasertib-HQPA (AZD2811) 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
Molecular Weight

507.56

Formula

C₂₆H₃₀FN₇O₃

CAS No.

722544-51-6

SMILES

O=C(CC1=NNC(NC2=C3C=CC(OCCCN(CCO)CC)=CC3=NC=N2)=C1)NC4=CC=CC(F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 22 mg/mL (43.34 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.93 mM); Precipitated solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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
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Barasertib-HQPA
Cat. No.:
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