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AZD-8835

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Catalog No. T6774Cas No. 1620576-64-8
Alias AZD8835

AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM).

AZD-8835

AZD-8835

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Purity: 99.88%
Catalog No. T6774Alias AZD8835Cas No. 1620576-64-8
AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$43In StockIn Stock
10 mg$63In StockIn Stock
25 mg$119In StockIn Stock
50 mg$173In StockIn Stock
100 mg$317-In Stock
1 mL x 10 mM (in DMSO)$52In StockIn 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:99.88%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM).
Targets&IC50
PI3Kγ:90 nM, PI3Kα:6.2 nM, PI3Kδ:5.7 nM, PI3Kα (E542K):6 nM, PI3Kα (H1047R):5.8 nM, PI3Kβ:431 nM
In vitro
AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN null breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line)[2].
In vivo
AZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration[1][2].
Cell Research
BT474, MCF7, or T47D cells are seeded in 384-well plates at a density of 500 to 2,000 cells per well and incubated overnight. Cells are dosed with compound(s) and cell confluency is measured at 4-hour intervals over several days.(Only for Reference)
SynonymsAZD8835
Chemical Properties
Molecular Weight469.54
FormulaC22H31N9O3
Cas No.1620576-64-8
SmilesCCn1nc(nc1-c1cnc(N)c(n1)-c1nnc(o1)C(C)(C)C)C1CCN(CC1)C(=O)CCO
Relative Density.1.45 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: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 86 mg/mL (183.16 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.13 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
1mg5mg10mg50mg
1 mM2.1297 mL10.6487 mL21.2974 mL106.4872 mL
5 mM0.4259 mL2.1297 mL4.2595 mL21.2974 mL
10 mM0.2130 mL1.0649 mL2.1297 mL10.6487 mL
20 mM0.1065 mL0.5324 mL1.0649 mL5.3244 mL
50 mM0.0426 mL0.2130 mL0.4259 mL2.1297 mL
100 mM0.0213 mL0.1065 mL0.2130 mL1.0649 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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