A939572

For research use only.

Catalog No.S9607

1 publication

A939572 Chemical Structure

CAS No. 1032229-33-6

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.

Selleck's A939572 has been cited by 1 publication

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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. Combinatorial application of A939572 with temsirolimus synergistically inhibits tumor growth in vivo.[2]

Protocol

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: athymic nu/nu mice
  • Dosages: 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 39 mg/mL (100.55 mM)
Water Insoluble
Ethanol '''''5 mg/mL

* 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.

Chemical Information

Molecular Weight 387.86
Formula

C20H22ClN3O3

CAS No. 1032229-33-6
Storage powder
in solvent
Synonyms N/A
Smiles CNC(=O)C1=CC(=CC=C1)NC(=O)N2CCC(CC2)OC3=CC=CC=C3Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID