GSK2194069 |
Catalog No.GC11562
One-Click Copy Product Info
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GSK2194069 est un puissant inhibiteur de la β-cétoyl réductase (KR) de la synthase des acides gras (FASN), avec une valeur IC50 de 7,7 nM. GSK2194069 montre spécifiquement un effet inhibiteur sur les cellules cancéreuses exprimant le FAS, en agissant sur l'acétoacétyl-CoA, le NADPH avec des valeurs IC50 ou Ki de 4,8 nM et 5,6 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1332331-08-4
Sample solution is provided at 25 µL, 10mM.
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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
| Cas No. | 1332331-08-4 | SDF | |
| Chemical Name | (S)-4-(4-(benzofuran-5-yl)phenyl)-3-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)methyl)-1H-1,2,4-triazol-5(4H)-one | ||
| Canonical SMILES | O=C1NN=C(C[C@@H]2CCN(C(C3CC3)=O)C2)N1C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4 | ||
| Formula | C25H24N4O3 | M.Wt | 428.48 |
| Solubility | DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 1.25 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3338 mL | 11.6692 mL | 23.3383 mL |
| 5 mM | 466.8 μL | 2.3338 mL | 4.6677 mL |
| 10 mM | 233.4 μL | 1.1669 mL | 2.3338 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)