Barasertib (Synonyms: AZD1152)

Name: Barasertib
Brand: MedChemExpress
SKU: HY-10127
Rating: 5.0 (25 reviews)

Cat. No.: HY-10127 Pureza: 99.50%: Ficha de datos
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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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No. CAS : 722543-31-9

Tamaño	Stock	Cantidad

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 25 publication(s) in Google Scholar

Other Forms of Barasertib:

Barasertib-HQPA In-stock
Barasertib dihydrochloride Obtener un presupuesto
Barasertib (Standard) Obtener un presupuesto

25 Publications Citing Use of MCE Barasertib

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Apoptosis Analysis

: 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.

: 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).

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Aurora Kinase:

Ver todas las isoformas

Aurora Kinase Aurora A Aurora B Aurora C

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target^[1]

Aurora B

0.37 nM (IC₅₀)

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.

Ensayo clínico

Peso molecular

587.54

Fòrmula

C₂₆H₃₁FN₇O₆P

No. CAS

722543-31-9

Appearance

Solid

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Pureza y Documentación

Purity: 99.50%

Select Batch:

Ficha de datos (281 KB) SDS (254 KB)

COA (254 KB) HNMR (144 KB) RP-HPLC (245 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Barasertib722543-31-9AZD1152AZD 1152AZD-1152Aurora KinaseApoptosiscolonbreastlungcancerleukemiaInhibitorinhibitorinhibit

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Barasertib (Synonyms: AZD1152)

Revisión del cliente

Other Forms of Barasertib:

Barasertib Related Antibodies

25 Publications Citing Use of MCE Barasertib

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Aurora Kinase:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Barasertib Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Barasertib Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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