Cat. No.: HY-10127

Barasertib

(Synonyms: AZD1152)

25 Cited Publications

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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.

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Pureté: 99.50%
CAS No.: 722543-31-9
Formule: C₂₆H₃₁FN₇O₆P
Masse moléculaire:587.54

Stockage:

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

Barasertib Chemical Structure

CAS No.: 722543-31-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (25)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Aurora B

0.37 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Aurora Kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H82	IC₅₀	1 nM Compound: AZD1152	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	[PMID: 34009981]
SK-N-BE(2)	IC₅₀	1 nM Compound: AZD1152	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	[PMID: 34009981]

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 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.

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].

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

Animal Model:

Female immune-deficient BALB/c nude mice (MOLM13 cells injected)^[1].
Dosage:

5 or 25 mg/kg.
Administration:

Intraperitoneal injection 4 times a week or every another day.
Result:

Inhibited the growth of human MOLM13 cells growing as xenografts using an immunodeficient murine model.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 722543-31-9
Appearance Solid
Masse moléculaire 587.54
Formule C₂₆H₃₁FN₇O₆P
Color Off-white to light yellow
SMILES

O=C(NC1=CC=CC(F)=C1)CC2=CC(NC3=C4C=CC(OCCCN(CC)CCOP(O)(O)=O)=CC4=NC=N3)=NN2
Synonyms

AZD1152
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (25)

All WBCell Proliferation/Viability AssayIFCell Imaging/StainingApoptosis Analysis

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

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.
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).
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

Dynamic phosphorylation of FOXA1 by Aurora B guides post-mitotic gene reactivation. [Abstract]

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
bioRxiv

2025 Jul 21.
bioRxiv

2023 Nov 30.
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
Patent

US20210299273A1.
bioRxiv

2021 Feb 5.
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7020 mL

8.5101 mL

17.0201 mL

5 mM

0.3404 mL

1.7020 mL

3.4040 mL

10 mM

0.1702 mL

0.8510 mL

1.7020 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

Protocol 3

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.

Protocol 4

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.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (3.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (254 KB)
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- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Barasertib

25 Cited Publications

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Barasertib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Barasertib

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Publications (25)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Barasertib Related Classifications

HY-10127 Related Classifications