CVT-11127

Catalog No.S4470 Batch:S447001

Technical Data

Formula	C₂₅H₂₃Cl₂N₅O₃
Molecular Weight	512.39	CAS No.	1018674-83-3
Solubility (25°C)*	In vitro	DMSO	6 mg/mL (11.7 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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

CVT-11127 (FMK13918) is an inhibitor of stearoylCoA desaturase-1 (SCD1). CVT-11127 reduces lipid synthesis and impaires proliferation by blocking the progression of cell cycle through the G(1)/S boundary and by triggering programmed cell death.

Targets

SCD1 ^[1]

In vitro

CVT-11127, an SCD1 inhibitor, decreases expression of SCD1, prevents the growth of STK11/KEAP1 co-mutant cells and sensitizes those cells to ferroptosis induction.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines H358 isogenic clones (NTC, STK11^KO, KEAP1^KO, DKO) Concentrations 1 μM Incubation Time 4 days Method 3000 cells per well of the indicated genotype were plated in 96 well plates in triplicate for each drug dose. Cells were allowed to attach to the plate overnight in RPMI media supplemented with 10% FBS. Drug titrations were performed in full serum media in a separate 96 well plate with column 11 containing the highest dose of the drug, column 3 containing the lowest dose of the drug, and column 2 containing no drug. Outside wells were filled with PBS to avoid liquid precipitation. After cells were allowed to attached to the plate overnight, media was aspirated using a multi-channel aspirator, and replaced with drug media from the drug titration plates. Cells were inclubated at 37 degrees for 3–4 days as indicated. On the final day of drug treatment, media was once again aspirated using a multi-channel aspirator. Cells were washed 1× with PBS then fixed to the plate and stained with a solution of 0.5% crystal violet, 1% Methanol, and 1% Formaldehyde in PBS for 15 minutes at room temperature.

Cell Assay:^{^[2]}

Cell lines
H358 isogenic clones (NTC, STK11^KO, KEAP1^KO, DKO)
Concentrations
1 μM
Incubation Time
4 days
Method
3000 cells per well of the indicated genotype were plated in 96 well plates in triplicate for each drug dose. Cells were allowed to attach to the plate overnight in RPMI media supplemented with 10% FBS. Drug titrations were performed in full serum media in a separate 96 well plate with column 11 containing the highest dose of the drug, column 3 containing the lowest dose of the drug, and column 2 containing no drug. Outside wells were filled with PBS to avoid liquid precipitation. After cells were allowed to attached to the plate overnight, media was aspirated using a multi-channel aspirator, and replaced with drug media from the drug titration plates. Cells were inclubated at 37 degrees for 3–4 days as indicated. On the final day of drug treatment, media was once again aspirated using a multi-channel aspirator. Cells were washed 1× with PBS then fixed to the plate and stained with a solution of 0.5% crystal violet, 1% Methanol, and 1% Formaldehyde in PBS for 15 minutes at room temperature.

References

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SHIPPING AND STORAGE
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