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GSK2194069

Catalog No.
B8005
human fatty acid synthase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$191.00
In stock
2mg
$128.00
In stock
5mg
$203.00
In stock
10mg
$353.00
In stock
50mg
$1,410.00
In stock
100mg
$2,325.00
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Background

IC50: 7.7 nM

GSK 2194069 is a potent human fatty acid synthase inhibitor.

Human fatty acid synthase (hFAS) is a multifunctional enzyme solely responsible for the de novo synthesis of long chain fatty acids. hFAS is expressed highly in a number of cancers, while with low observed expression in most normal tissues. Though normal tissues get fatty acids from the diet, tumor tissues can rely on de novo fatty acid synthesis, which makes hFAS an attractive metabolic target for cancer treatment.

In vitro: GSK2194069 displayed acceptable solubility and permeability and thus was chosen for further characterization. GSK2194069 had an IC50 of 29 ± 3.2 nM versus hFAS with acetoacetyl-CoA as the substrate but showed little or no inhibition with crotonyl-CoA andβ-hydroxybutyryl-CoA. GSK2194069 was also found not to inhibit the partial activities of the KS domain [1].

In vivo: In those mice dosed with GSK2194069, tumour growth was inhibited. There was no significant weight loss in the GSK2194069 treated group and no adverse effects were observed. The effect of GSK2194069 in decreasing acetate uptake was demonstrated by scintillation detection of C42b xenograft tumours by 56% 2 hours after dosing with GSK2194069. Inhibition of FAS caused by GSK2194069 led to a decrease in acetate signal in all animals [1].

Clinical trial: N/A

References:
[1] Hardwicke MA,Rendina AR,Williams SP,Moore ML,Wang L,Krueger JA,Plant RN,Totoritis RD,Zhang G,Briand J,Burkhart WA,Brown KK, Parrish CA.  A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol.2014 Sep;10(9):774-9.
[2] Greg Shaw, David Lewis, Joan Boren, Antonio Ramos-Montoya, Robert Bielik, Dmitry Soloviev, Brindle Kevin, Neal David.  509 THERAPEUTIC FATTY ACID SYNTHASE INHIBITION IN PROSTATE CANCER AND THE USE OF 11C-ACETATE TO MONITOR THERAPEUTIC EFFECTS. The Journal of Urology. 2013Volume 189, Issue 4, Supplement, Pagese208–e209

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at -20°C
M.Wt428.48
Cas No.1332331-08-4
FormulaC25H24N4O3
SolubilitySoluble in DMSO
Chemical Name(S)-4-(4-(benzofuran-5-yl)phenyl)-3-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)methyl)-1H-1,2,4-triazol-5(4H)-one
SDFDownload SDF
Canonical SMILESO=C1NN=C(C[[email protected]@H]2CCN(C(C3CC3)=O)C2)N1C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

GSK2194069