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

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

Cat. No.: HY-10126 Purity: 99.47%
Handling Instructions

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.

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
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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
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Based on 6 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. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells[1].

IC50 & Target[1]

Aurora B

0.37 nM (IC50)

In Vitro

Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells[1].
Barasertib-hydroxyquinazoline pyrazol anilide (HQPA)] is converted rapidly to the active Barasertib-HQPA in plasma[2].
Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line[3].
Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1].

Cell Line: AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells.
Concentration: 0-100 nM. (Barasertib -HQPA)
Incubation Time: 48 h.
Result: IC50 values ranged from 3 nM to 40 nM.
In Vivo

Barasertib (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors[1].
Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1].
Barasertib (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P < 0.05) in immunodeficient mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.47%

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Keywords:

Barasertib-HQPAAZD2811 INH-34 AZD1152-HQPAAZD 2811AZD-2811INH34INH 34INH-34Aurora KinaseApoptosiscolonbreastlungcancerleukemiaInhibitorinhibitorinhibit

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