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AZD1152

Catalog No.GC14709

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AZD1152 Chemical Structure

Cas No.: 722543-31-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$67.00
In stock
5mg
$62.00
In stock
10mg
$105.00
In stock
50mg
$346.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Leukemia cells from patients, bone marrow mononuclear cells from healthy volunteers

Preparation method

The solubility of this compound in DMSO is >5.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1-100 nM

Applications

AZD1152-HQPA (1-100 nM) induced growth arrest of a variety of types of leukemia cells with the IC50s of approximately 5, 12, and 8 nM for Philadelphia chromosome–positive ALL PALL-2, acute monocytic leukemia MOLM13, and biphenotypic leukemia MV4-11 cells, respectively. AZD1152 (3 μM, 3 hours) significantly decreased expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells. AZD1152 increased cell 4N/8N DNA content in a dose- and time-dependent manner in MOLM13 and PALL2 cells. AZD1152-HQPA treatment (1-10 nM) for 24 or 48 hours induced apoptosis in a dose-dependent manner.

Animal experiment [2]:

Animal models

Female immune-deficient BALB/c nude mice xenografted with human MOLM13 cells

Dosage form

5 or 25 mg/kg, Intraperitoneal injection, 4 times a week or every another day,

Application

AZD1152 (25 mg/kg) markedly suppressed the growth and weights of AZD1152-treated tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Yang J, Ikezoe T, Nishioka C, 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[J]. Blood, 2007, 110(6): 2034-2040.

[2] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20.

Background

Chemical Properties

Cas No. 722543-31-9 SDF
Chemical Name 2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate
Canonical SMILES CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O
Formula C26H31FN7O6P M.Wt 587.54
Solubility ≥ 30 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.702 mL 8.5101 mL 17.0201 mL
5 mM 0.3404 mL 1.702 mL 3.404 mL
10 mM 0.1702 mL 0.851 mL 1.702 mL
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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