Barasertib
Based on 25 publication(s) in Google Scholar
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.50%
- CAS No.: 722543-31-9
- 화학식: C26H31FN7O6P
- 분자량:587.54
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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용액&용해도
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Publications Citing Use of MedChemExpress (MCE) Barasertib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Commun. 2023 Oct 10;14(1):6332. [Abstract]
- Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
- Nucleic Acids Res. 2025 Apr 10;53(7):gkaf294. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(21):e17108. [Abstract]
- Cell Death Differ. 2025 Oct 30. [Abstract]
- Phytomedicine. 2026 May:154:158036. [Abstract]
- Clin Cancer Res. 2019 Jul 15;25(14):4552-4566. [Abstract]
- NPJ Precis Oncol. 2025 Dec 10. [Abstract]
- Dev Cell. 2023 Dec 4;58(23):2666-2683.e9. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Cell Rep. 2024 Sep 13;43(9):114739. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]
- Cell Signal. 2026 Jul:143:112490. [Abstract]
- J Biol Chem. 2025 Jan 16:108196. [Abstract]
- Am J Cancer Res. 2021 Jun 15;11(6):3021-3038. [Abstract]
- Leuk Lymphoma. 2020 Dec;61(14):3451-3459. [Abstract]
- bioRxiv. 2025 Jul 21.
- bioRxiv. 2023 Nov 30.
- Biomed Pharmacother. 2023 Oct:166:115343. [Abstract]
- Patent. US20210299273A1.
- bioRxiv. 2021 Feb 5.
- Patent. US20180263995A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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IF
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Cell Imaging/Staining
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Apoptosis Analysis
All Aurora Kinase Isoforms
More
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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| NCI-H82 | IC50 |
1 nM
Compound: AZD1152
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Growth inhibition of human NCI-H82 cells assessed as reduction in cell viability after 72 hrs by PrestoBlue Cell Viability assay
Growth inhibition of human NCI-H82 cells assessed as reduction in cell viability after 72 hrs by PrestoBlue Cell Viability assay
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[PMID: 34009981] |
| SK-N-BE(2) | IC50 |
1 nM
Compound: AZD1152
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Growth inhibition of human SKNBE2 cells assessed as reduction in cell viability after 72 hrs by PrestoBlue Cell Viability assay
Growth inhibition of human SKNBE2 cells assessed as reduction in cell viability after 72 hrs by PrestoBlue Cell Viability assay
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[PMID: 34009981] |
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 induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immune-deficient BALB/c nude mice (MOLM13 cells injected)[1].
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Dosage:5 or 25 mg/kg.
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Administration:Intraperitoneal injection 4 times a week or every another day.
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Result:Inhibited the growth of human MOLM13 cells growing as xenografts using an immunodeficient murine model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 722543-31-9
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Appearance Solid
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분자량 587.54
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화학식 C26H31FN7O6P
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CC(F)=C1)CC2=CC(NC3=C4C=CC(OCCCN(CC)CCOP(O)(O)=O)=CC4=NC=N3)=NN2
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Synonyms
AZD1152
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (25)
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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
Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer. [Abstract]2023 Oct 10;14(1):6332. PMID: 37816716
Barasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 10;14(1):6332. [Abstract]
Effects of Barasertib (25–1000 nM, 72 h) combination on cell viability of mut KRAS (H1792, H2009, A549, HCC44, H23, H358) cells.
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Nat Commun
AURKB as a target in non-small cell lung cancer with acquired resistance to anti-EGFR therapy. [Abstract]2019 Apr 18;10(1):1812 PMID: 31000705
Barasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
Western blot showing the dose-dependent decrease of pH3 levels induced by Barasertib (0.05, 0.1, 0.2 μM) at 24 h in PC9-ER and PC9-GR4 cells.
Barasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
ICC showing the inhibition of non-mitotic pH3 by Barasertib (0.05 μM) and the MET/AXL/FGFR/AURKB inhibitor S49076 after 24 h in PC9-ER and PC9-GR4 cells.
Barasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
Acidic beta-galactosidase staining of PC9-ER and PC9-GR4 cells after 48 h with Barasertib (0.01, 0.06 μM) or S49076, showing the induction of senescence-associated activity in PC9-GR4.
Barasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
Results of flow-cytometry experiments of PC9-GR1, PC9-GR4-AZD1, H1975 (p.T790M positive), PC9-GR3, and PC9-GR1-AZD3 (p.T790M negative), showing the induction of apoptosis only in p.T790M-negative cells after 24 h treatment with Barasertib (0.06 µM).
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Nucleic Acids Res
Chromatin-associated α-satellite RNA maintains chromosome stability by reestablishing SAF-A in the mitotic cell cycle. [Abstract]2025 Apr 10;53(7):gkaf294. PMID: 40219970 -
Adv Sci (Weinh)
Targeted Extracellular Vesicles Deliver Asiaticoside to Inhibit AURKB/DRP1-Mediated Mitochondrial Fission and Attenuate Hypertrophic Scar Formation. [Abstract]2026 Apr;13(21):e17108. PMID: 41637535 -
Cell Death Differ
CRISPR/Cas9 library screening uncovered CCT2 as a critical driver of acquired resistance to EGFR-targeted therapy by stabilizing TMX1 in non-small cell lung cancer. [Abstract]2025 Oct 30. PMID: 41168408 -
Phytomedicine
Diosmetin alleviates the immunosuppressive tumor microenvironment in esophageal squamous cell carcinoma by dually inhibiting angiogenesis and promoting CD8+T cell cytotoxicity. [Abstract]2026 May:154:158036. PMID: 41830859 -
Clin Cancer Res
High-throughput Chemical Screening Identifies Focal Adhesion Kinase and Aurora Kinase B Inhibition as a Synergistic Treatment Combination in Ewing Sarcoma. [Abstract]2019 Jul 15;25(14):4552-4566. PMID: 30979745 -
NPJ Precis Oncol
Targeting high-risk MYC-overexpressed osteosarcoma with an Aurora kinase inhibitor:--results from a pilot umbrella trial. [Abstract]2025 Dec 10. PMID: 41372533 -
Dev Cell
The anaphase-promoting complex controls a ubiquitination-phosphoprotein axis in chromatin during neurodevelopment. [Abstract]2023 Dec 4;58(23):2666-2683.e9. PMID: 37875116 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
Cell Rep
2024 Sep 13;43(9):114739. PMID: 39276350 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Cancers (Basel)
Targeting the EGFR and Spindle Assembly Checkpoint Pathways in Oral Cancer: A Plausible Alliance to Enhance Cell Death. [Abstract]2024 Nov 5;16(22):3732. PMID: 39594688 -
Cell Signal
Molecular mechanism of S100P promotes hepatocellular carcinoma by regulating MYBL2-mediated transcription of AURKB. [Abstract]2026 Jul:143:112490. PMID: 41856224 -
J Biol Chem
Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]2025 Jan 16:108196. PMID: 39826695 -
Am J Cancer Res
Epigenetic heterogeneity promotes acquired resistance to BET bromodomain inhibition in ovarian cancer. [Abstract]2021 Jun 15;11(6):3021-3038. PMID: 34249442 -
Leuk Lymphoma
Let-7b regulates the adriamycin resistance of chronic myelogenous leukemia by targeting AURKB in K562/ADM cells. [Abstract]2020 Dec;61(14):3451-3459. PMID: 32856506 -
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Biomed Pharmacother
Barasertib impedes chondrocyte senescence and alleviates osteoarthritis by mitigating the destabilization of heterochromatin induced by AURKB. [Abstract]2023 Oct:166:115343. PMID: 37634474 -
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용액&용해도
DMSO : ≥ 33 mg/mL (56.17 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.17 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Yang J, 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 [Content Brief]
[2]. 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]
[3]. 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]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7020 mL | 8.5101 mL | 17.0201 mL | 42.5503 mL |
| 5 mM | 0.3404 mL | 1.7020 mL | 3.4040 mL | 8.5101 mL | |
| 10 mM | 0.1702 mL | 0.8510 mL | 1.7020 mL | 4.2550 mL | |
| 15 mM | 0.1135 mL | 0.5673 mL | 1.1347 mL | 2.8367 mL | |
| 20 mM | 0.0851 mL | 0.4255 mL | 0.8510 mL | 2.1275 mL | |
| 25 mM | 0.0681 mL | 0.3404 mL | 0.6808 mL | 1.7020 mL | |
| 30 mM | 0.0567 mL | 0.2837 mL | 0.5673 mL | 1.4183 mL | |
| 40 mM | 0.0426 mL | 0.2128 mL | 0.4255 mL | 1.0638 mL | |
| 50 mM | 0.0340 mL | 0.1702 mL | 0.3404 mL | 0.8510 mL |
Barasertib Related Classifications
HY-10127 Related Classifications
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