A939572

Catalog No.S9607 Batch:S960701

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Technical Data

Formula

C20H22ClN3O3

Molecular Weight 387.86 CAS No. 1032229-33-6
Solubility (25°C)* In vitro DMSO 39 mg/mL (100.55 mM)
Ethanol 5 mg/mL (12.89 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO Corn oil
1.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description A939572 is a potent and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
Targets
mSCD1 [1]
(Cell-free assay)
hSCD1 [1]
(Cell-free assay)
4 nM 37 nM
In vitro

A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5. In congruity with previous experimentation examining SCD1 lentiviral knockdown models, A939572 induces apoptosis confirmed by PARP cleavage via western blot analysis in all four cell lines. Treatment of ccRCC cells with A939572 induces Endoplasmic Reticulum Stress.[2]

In vivo

When compared to the placebo control, all treatment groups (A939572, Tem, and Combo) exhibits decreased proliferation as marked by reduction in percent positivity of nuclear Ki67 staining, with the combinatorial group demonstrating the most significant decline. 

Protocol (from reference)

Cell Assay:

[2]

  • Cell lines

    Caki1, A498, Caki2, ACHN ccRCC cells

  • Concentrations

    75 nM

  • Incubation Time

    24 h

  • Method

    In order to determine the mechanism of decreased proliferation and induction of cell death associated with loss of SCD1 activity in ccRCC cells, gene array analysis was performed with Caki1, A498, Caki2, and ACHN ccRCC cells treated for 24 hours with a 75nM dose of A939572 compared to DMSO control.

Animal Study:

[2]

  • Animal Models

    athymic nu/nu mice

  • Dosages

    30 mg/kg

  • Administration

    Oral gavage

Selleck's A939572 has been cited by 2 publications

CTC-derived pancreatic cancer models serve as research tools and are suitable for precision medicine approaches [ Cell Rep Med, 2024, 5(9):101692] PubMed: 39163864
LXRα activation and Raf inhibition trigger lethal lipotoxicity in liver cancer [ NAT CANCER, 2021, 2, 201–217] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.