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A939572

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Catalog No. T4515Cas No. 1032229-33-6

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

A939572

A939572

🥰Excellent
Purity: 99.96%
Catalog No. T4515Cas No. 1032229-33-6
A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$71In StockIn Stock
10 mg$117In StockIn Stock
25 mg$237In StockIn Stock
50 mg$379In StockIn Stock
100 mg$596In StockIn Stock
200 mg$863In StockIn Stock
1 mL x 10 mM (in DMSO)$74In 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:99.96%
Color:White
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Product Introduction

Bioactivity
Description
A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.
Targets&IC50
SCD1 (human):37 nM, SCD1 (mouse):<4 nM
In vitro
A939572 has been used to induce cell death of hPSCs as well as to inhibit the proliferation of human non-small cell lung carcinoma H1299 cells in vitro[1][2].
In vivo
Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts were treated with A939572 and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) was recorded .?A939572 and Tem monotherapy generated similar growth responses with approximately 20 30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment.?The combination group yielded over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment.?All of the animals maintained a healthy weight throughout the course of the treatment , however those in both the A939572 and the Combo group exhibited increased blinking, and slight mucosal discharge from the eyes after the first week of treatment[3].
Kinase Assay
Caki1 and A498 cells were transiently transfected with p5xATF6-GL3 UPR luciferase reporter and pRL-CMV-renilla luciferase plasmid using Lipofectamine2000 (Invitrogen). Cells (DMSO vs. A939572, NT vs. shSCD780) were harvested after 48hrs using Dual Luciferase assay kit per the manufacturer s protocol and luciferase activity was measured using a Veritas Luminometer; reported as relative luminescence[3].
Animal Research
A498 cells were subcutaneously implanted in athymic nu/nu mice at 1×10^6 cells/mouse in 50%Matrigel.?Tumors reached ~50 mm^3 prior to 4wk treatment.?A939572 was re-suspended in strawberry-flavored Kool-Aid in sterilized H2O (0.2g/mL) vehicle at 30mg/kg in a 50μl dose.?Mice were orally fed by using a syringe to administer the 50μl dose twice daily/mouse.?This modified method was found to be effective and less stressful on the mice.?Temsirolimus was solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10mg/kg in a 50μl dose once every 72hrs/mouse.?Tumor volumes were calculated using the formula and body weight were measured every 3 days[3].
Chemical Properties
Molecular Weight387.86
FormulaC20H22ClN3O3
Cas No.1032229-33-6
SmilesCNC(=O)c1cccc(NC(=O)N2CCC(CC2)Oc2ccccc2Cl)c1
Relative Density.1.302 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (116.02 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.16 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 mM2.5782 mL12.8912 mL25.7825 mL128.9125 mL
5 mM0.5156 mL2.5782 mL5.1565 mL25.7825 mL
10 mM0.2578 mL1.2891 mL2.5782 mL12.8912 mL
20 mM0.1289 mL0.6446 mL1.2891 mL6.4456 mL
50 mM0.0516 mL0.2578 mL0.5156 mL2.5782 mL
100 mM0.0258 mL0.1289 mL0.2578 mL1.2891 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

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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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