A939572

Catalog No.S9607 Batch:S960701

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.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (3.87mM)	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.73mM)	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.

* <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 (Cell-free assay)	hSCD1 (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, this compound induces apoptosis confirmed by PARP cleavage via western blot analysis in all four cell lines. Treatment of ccRCC cells with this chemical induces Endoplasmic Reticulum Stress.

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

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

References

https://pubmed.ncbi.nlm.nih.gov/18632269/
https://pubmed.ncbi.nlm.nih.gov/23633458/

Sellecks 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

RETURN POLICY
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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.