Barasertib-HQPA
Based on 9 publication(s) in Google Scholar
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.
- Purity: 98.90%
- CAS No.: 722544-51-6
- Formula: C26H30FN7O3
- Molecular Weight:507.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Barasertib-HQPA
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Commun Signal. 2023 Sep 30;21(1):268. [Abstract]
- Int J Mol Sci. 2022 Jan 11;23(2):763. [Abstract]
- J Cell Sci. 2025 Sep 1:jcs.263766. [Abstract]
- J Cell Sci. 2019 Jul 1;132(13):jcs229385. [Abstract]
- Exp Cell Res. 2021 Sep 1;406(1):112741. [Abstract]
- Ann Transl Med. 2020 May;8(10):646. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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IF
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
All Aurora Kinase Isoforms
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Biological Activity
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Aurora B 0.37 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
0.1 μM
Compound: AAZD1152-HQPA
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Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
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[PMID: 25036791] |
| A549 | IC50 |
5.4 μM
Compound: AAZD1152-HQPA
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Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by transwell migration assay
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by transwell migration assay
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[PMID: 25036791] |
| A549 | IC50 |
8.3 μM
Compound: AAZD1152-HQPA
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Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by scratch wound model assay
Antimigratory activity against human A549 cells assessed as inhibition of cell migration after 8 to 24 hrs by scratch wound model assay
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[PMID: 25036791] |
| HepG2 | IC50 |
0.1 μM
Compound: AAZD1152-HQPA
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Cytotoxicity against human HepG2 cells by SRB assay
Cytotoxicity against human HepG2 cells by SRB assay
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[PMID: 25036791] |
| HL-60 | IC50 |
12.7 nM
Compound: AZD1152
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Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 25089810] |
| MOLM-13 | IC50 |
1 nM
Compound: AZD1152-HQPA
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Inhibition of clonogenic growth in human MOLM-13 cells incubated for 10 days
Inhibition of clonogenic growth in human MOLM-13 cells incubated for 10 days
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[PMID: 17495131] |
| MOLM-13 | IC50 |
12 nM
Compound: AZD1152-HQPA
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Inhibition of cell proliferation of human MOLM-13 cells incubated for 48 hrs by 3H-thymidine uptake assay
Inhibition of cell proliferation of human MOLM-13 cells incubated for 48 hrs by 3H-thymidine uptake assay
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[PMID: 17495131] |
| MOLM-13 | IC50 |
9.7 nM
Compound: AZD1152
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Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 25089810] |
| MV4-11 | IC50 |
2.8 nM
Compound: AZD1152-HQPA
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Inhibition of clonogenic growth in human MV4-11 cells incubated for 10 days
Inhibition of clonogenic growth in human MV4-11 cells incubated for 10 days
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[PMID: 17495131] |
| MV4-11 | IC50 |
8 nM
Compound: AZD1152-HQPA
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Inhibition of cell proliferation of human MV4-11 cells incubated for 48 hrs by 3H-thymidine uptake assay
Inhibition of cell proliferation of human MV4-11 cells incubated for 48 hrs by 3H-thymidine uptake assay
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[PMID: 17495131] |
| MV4-11 | IC50 |
8.6 nM
Compound: AZD1152
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Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 25089810] |
| SW-620 | IC50 |
0.017 μM
Compound: 7, AZD-1152 HQPA
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Inhibition of aurora B in human SW620 cells assessed as inhibition of histone H3 phosphorylation
Inhibition of aurora B in human SW620 cells assessed as inhibition of histone H3 phosphorylation
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[PMID: 19320489] |
| THP-1 | IC50 |
25.1 nM
Compound: AZD1152
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Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 25089810] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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.
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Concentration:0-100 nM. (Barasertib -HQPA)
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Incubation Time:48 h.
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Result:IC50 values ranged from 3 nM to 40 nM.
Barasertib-HQPA (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1].
Barasertib-HQPA (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 722544-51-6
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Appearance Solid
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Molecular Weight 507.56
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Formula C26H30FN7O3
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Color White to yellow
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SMILES
O=C(CC1=NNC(NC2=C3C=CC(OCCCN(CCO)CC)=CC3=NC=N2)=C1)NC4=CC=CC(F)=C4
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Synonyms
AZD2811; INH-34; AZD1152-HQPA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Commun Signal
Identification of novel SCD1 inhibitor alleviates nonalcoholic fatty liver disease: critical role of liver-adipose axis. [Abstract]2023 Sep 30;21(1):268. PMID: 37777801 -
Int J Mol Sci
Aurora Kinase A Is Involved in Controlling the Localization of Aquaporin-2 in Renal Principal Cells. [Abstract]2022 Jan 11;23(2):763. PMID: 35054947
Barasertib-HQPA purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Jan 11;23(2):763. [Abstract]
MCD4 were left untreated or treated with DMSO (0.3% or 0.2%, 1 h), Alisertib (AURKA inhibitor; 30 µM or 20 µM, 1 h), or Barasertib-HQPA (AURKB inhibitor; 30 µM or 20 µM, 1 h) alone or in combination with forskolin (Fsk; 30 µM, 30 min) or arginine-vasopressin (AVP; 100 nM, 30 min) where indicated. AQP2 was detected by immunofluorescence microscopy. Shown are representative images of four independent experiments; scale bar 30 µm. AQP2 was quantified using a segmentation-based approach. Ratios > 1 indicate a predominant localization at the plasma membrane.
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J Cell Sci
An acentrosomal aster with atypical microtubule polarity recruits cytokinesis signals to its center in Xenopus egg extracts. [Abstract]2025 Sep 1:jcs.263766. PMID: 40888042
Barasertib-HQPA purchased from MedChemExpress. Usage Cited in: J Cell Sci. 2025 Sep 1:jcs.263766. [Abstract]
Confocal images of microtubule dynamics in control extracts (top row) and extracts with 40 µM Aurora kinase B inhibitor Barasertib-HQPA (bottom row). n=6. Each image is a maximum-intensity projection of nine confocal planes spanning 16 µm of depth. Imaging started at an arbitrary time point when asters had just begun to form in the untreated extracts. The results showed that Aurora kinase B inhibition by Barasertib-HQPA abolishes the aster, and the cell-like compartments form with a substantial delay.
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J Cell Sci
Repair-independent functions of DNA-PKcs protect irradiated cells from mitotic slippage and accelerated senescence. [Abstract]2019 Jul 1;132(13):jcs229385. PMID: 31189537 -
Exp Cell Res
RNA-binding protein RNPC1 acts as an oncogene in gastric cancer by stabilizing aurora kinase B mRNA. [Abstract]2021 Sep 1;406(1):112741. PMID: 34302858
Barasertib-HQPA purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2021 Sep 1;406(1):112741. [Abstract]
The IC50 of AURKB inhibitors (AZD1152-HQPA (Barasertib-HQPA, 48 h) and hesperadin) was explored by CCK-8 in gastric cancer cells (MGC-803 and SGC-7901).
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Ann Transl Med
ALKBH5 promotes the proliferation of renal cell carcinoma by regulating AURKB expression in an m6A-dependent manner. [Abstract]2020 May;8(10):646. PMID: 32566583
Barasertib-HQPA purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 May;8(10):646. [Abstract]
The effect of AURKB inhibitor (AZD1152 (Barasertib)-HQPZ (10 μM; 48 h) and hesperidin) on Caki-1 and 786-0 cells with ALKBH5 overexpression was measured by CCK8 and clone formation assays. The colony fold (NC/ALKBH5) is stated under the histogram.
Solvent & Solubility
DMSO : ≥ 22 mg/mL (43.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Yang, Jing., et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 15;110(6):2034-40. [Content Brief]
[2]. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. [Content Brief]
[3]. Zekri A, et al. AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Tumour Biol. 2015 Feb;36(2):623-32. [Content Brief]
[4]. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9702 mL | 9.8511 mL | 19.7021 mL | 49.2553 mL |
| 5 mM | 0.3940 mL | 1.9702 mL | 3.9404 mL | 9.8511 mL | |
| 10 mM | 0.1970 mL | 0.9851 mL | 1.9702 mL | 4.9255 mL | |
| 15 mM | 0.1313 mL | 0.6567 mL | 1.3135 mL | 3.2837 mL | |
| 20 mM | 0.0985 mL | 0.4926 mL | 0.9851 mL | 2.4628 mL | |
| 25 mM | 0.0788 mL | 0.3940 mL | 0.7881 mL | 1.9702 mL | |
| 30 mM | 0.0657 mL | 0.3284 mL | 0.6567 mL | 1.6418 mL | |
| 40 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2314 mL |
Barasertib-HQPA Related Classifications
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