Home Metabolism SCD inhibitor A939572 For research use only.

A939572

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.

A939572 Chemical Structure

A939572 Chemical Structure

CAS: 1032229-33-6

Selleck's A939572 has been cited by 1 publication

Purity & Quality Control

Batch: S960701 DMSO] 39 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 98.99%
98.99

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models athymic nu/nu mice
Dosages 30 mg/kg
Administration Oral gavage

Chemical lnformation & Solubility

Molecular Weight 387.86 Formula

C20H22ClN3O3
CAS No. 1032229-33-6 SDF --
Smiles CNC(=O)C1=CC(=CC=C1)NC(=O)N2CCC(CC2)OC3=CC=CC=C3Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 39 mg/mL ( (100.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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