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HomeProduct name listGSK2194069

GSK2194069

Synonym(s):(S)-4-(4-(Benzofuran-5-yl)phenyl)-3-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)methyl)-1H-1,2,4-triazol-5(4H)-one

GSK2194069 Structural

What is GSK2194069?

The Uses of GSK2194069

GSK 2194069 is a potent human fatty acid synthase (hFASN) inhibitor.

Biochem/physiol Actions

GSK2194069 is a fatty acid synthase (FAS) inhibitor. GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM for the overall hFAS reaction. FAS is upregulated in some cancers, including prostate cancer. GSK2194069 was found to inhibit tumour growth in prostate cancer C42b cell xenografts generated in Nod-SCID-gamma mice. Cellular FAS inhibition reduced cell growth were also demonstrated in non-small-cell lung (A549) cancer cell lines with an average EC50 of 15 ± 0.5 nM.

Storage

Store at +4°C

Properties of GSK2194069

Density  1.44±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMF:30.0(Max Conc. mg/mL);70.01(Max Conc. mM)
DMSO:54.28(Max Conc. mg/mL);126.68(Max Conc. mM)
Ethanol:4.91(Max Conc. mg/mL);11.46(Max Conc. mM)
form  powder
pka 6.15±0.20(Predicted)
color  white to light brown

Safety information for GSK2194069

Computed Descriptors for GSK2194069

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