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CVT-11127

Chemical Structure : CVT-11127

CAS No.: 1018674-83-3

CVT-11127 (FMK13918, GS-456332)

Catalog No.: PC-38545Not For Human Use, Lab Use Only.

CVT-11127 (FMK13918, GS-456332) is a specfiic small molecule stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 210 and 410 nM against rat microsomal SCD and HepG2 SCD, respectively.

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Biological Activity

CVT-11127 (FMK13918, GS-456332) is a specfiic small molecule stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 210 and 410 nM against rat microsomal SCD and HepG2 SCD, respectively.
CVT-11127 is selective for Δ9 desaturases, does not inhibit the activity of rat microsomal Δ5 and Δ6 desaturases at 30 uM.
CVT-11127 reduces cell proliferation in human lung and breast cancer cells, decreases de novo lipid synthesis from glucose.
CVT-11127 impairs the ligand-induced phosphorylation of epidermal growth factor (EGF) receptor, causing the inactivation of its downstream targets Akt, ERK and mammalian target of rapamycin in H460 lung cancer cells.

Physicochemical Properties

M.Wt 512.391
Formula C25H23Cl2N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(6-(3,4-dichlorobenzylamino)-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl)ethyl) acetamide

References

1. Koltun DO, et al. Bioorg Med Chem Lett. 2009;19:2048–52.

2. Natalia Scaglia, et al. PLoS One. 2009 Aug 27;4(8):e6812.

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