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Barasertib

Name: Barasertib
Brand: TargetMol
SKU: T14371
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14371Cas No. 722543-31-9

Alias AZD1152

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

Barasertib

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Purity: 99.97%

Catalog No. T14371Alias AZD1152Cas No. 722543-31-9

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$42	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$118	In Stock	In Stock
25 mg	$219	In Stock	In Stock
50 mg	$386	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.97%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
Targets&IC50	Aurora B:0.37 nM
In vitro	Barasertib inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM and it also inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. Barasertib displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. Barasertib causes significant accumulation of cells with 4N/8N DNA content in KMS12 and U266 and induces apoptosis in KMS18 and U266. Barasertib has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. Barasertib induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[1]. Barasertib in combination with DEX, has negative effects on cell viability in comparison with single agent in PMI8226, KMS11 and U266[3].
In vivo	Administration of Barasertib (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[1]. Barasertib (25 mg/kg/day) treatment reduces xenograft levels such that they are slightly lower levels than after the first round of treatment, but this is not statistically significant indicating that residual cells might be more resistant to a second cycle of Barasertib[4]. In addition, Barasertib (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[2].
Synonyms	AZD1152

Chemical Properties

Molecular Weight	587.54
Formula	C₂₆H₃₁FN₇O₆P
Cas No.	722543-31-9
Smiles	CCN(CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1)CCOP(O)(O)=O
Relative Density.	1.463 g/cm3

Storage & Solubility Information

Storage

store under nitrogen | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 33 mg/mL (56.17 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.4 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7020 mL	8.5101 mL	17.0201 mL	85.1006 mL
5 mM	0.3404 mL	1.7020 mL	3.4040 mL	17.0201 mL
10 mM	0.1702 mL	0.8510 mL	1.7020 mL	8.5101 mL
20 mM	0.0851 mL	0.4255 mL	0.8510 mL	4.2550 mL
50 mM	0.0340 mL	0.1702 mL	0.3404 mL	1.7020 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc