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Apoptozole

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Catalog No. T3293Cas No. 1054543-47-3
Alias Apoptosis Activator VII

Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.

Apoptozole

Apoptozole

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Purity: 99.75%
Catalog No. T3293Alias Apoptosis Activator VIICas No. 1054543-47-3
Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$43In StockIn Stock
10 mg$76In StockIn Stock
25 mg$139In StockIn Stock
50 mg$247In Stock-
100 mg$368In Stock-
200 mg$543In Stock-
1 mL x 10 mM (in DMSO)$60In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.75%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.
Targets&IC50
HSP70:0.14 μM(Kd), HSC70:0.21 μM(Kd)
In vitro
Apoptozole induces caspase dependent apoptosis by blocking interaction of HSP70 with APAF-1, without affecting interactions of HSP70 with ASK1, JNK, BAX, and AIF[2]. However, apoptozole may form aggregates under aqueous conditions that could interact with HSP70 proteins in a non-specific manner, potentially leading to false positives and inconsistent data[3].
In vivo
Apoptozole greatly retards tumor growth in mice xenografted with cancer cells without affecting mouse viability. The elimination half-life time (T1/2) of Az in blood is found to be significantly longer than that of Dox (8.04 versus 1.60 hr) and the time needed to reach a maximum concentration (Tmax) of Az is shorter than that of Dox (1.00 versus 4.00 hr)[2].
Kinase Assay
Inhibition of HER2/erbB2 tyrosine kinase activity: BT-474 cells are seeded on 24-well plates and cultured overnight. Mubritinib is then added at various concentrations. After incubation for 2 hours, the cells are harvested directly into sodium dodecyl sulfate (SDS)-sample buffer (200 μL). Aliquots containing equal amounts of total cell extract are run on 7.5% to 15% gradient SDS–polyacrylamide gel electrophoresis (PAGE). Following electrophoresis, proteins are transferred onto a polyvinylidene fluoride (PVDF) membrane, for western blot analysis using a relevant primary antibody. Detection of protein is accomplished by an enhanced chemiluminescent (ECL) detection method. The extent of tyrosine phosphorylation of HER2/erbB2 is measured by the LAS-1000 plus lumino-image analyser. The concentration of Mubritinib that inhibits HER2/erbB2 phosphorylation by 50% (IC50) is calculated from a dose–response curve generated by least-squares linear regression of the response using SAS software.
Cell Research
Several cancer cell lines (A549, lung adenocarcinoma epithelial cells; HeLa, cervical cancer cells; MDA-MB-231, breast cancer cells; HepG2, liver cancer cells) are treated with various concentrations (0-15 μM) of Az or compound 7 as a negative control for 18 hr. Cell viabilities are then determined using an MTT assay.(Only for Reference)
SynonymsApoptosis Activator VII
Chemical Properties
Molecular Weight625.56
FormulaC33H25F6N3O3
Cas No.1054543-47-3
SmilesCOc1ccc(cc1)-c1nc(-c2cc(cc(c2)C(F)(F)F)C(F)(F)F)n(Cc2ccc(cc2)C(N)=O)c1-c1ccc(OC)cc1
Relative Density.1.33 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 24 mg/mL (38.37 mM), Sonication is recommended.
DMSO: 93 mg/mL (148.67 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.28 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.5986 mL7.9928 mL15.9857 mL79.9284 mL
5 mM0.3197 mL1.5986 mL3.1971 mL15.9857 mL
10 mM0.1599 mL0.7993 mL1.5986 mL7.9928 mL
20 mM0.0799 mL0.3996 mL0.7993 mL3.9964 mL
DMSO
1mg5mg10mg50mg
50 mM0.0320 mL0.1599 mL0.3197 mL1.5986 mL
100 mM0.0160 mL0.0799 mL0.1599 mL0.7993 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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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

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