GSK 2194069

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Cat.No. 5303 - GSK 2194069 | C25H24N4O3 | CAS No. 1332331-08-4
Description: Potent human fatty acid synthase (hFASN) inhibitor
Chemical Name: 4-[4-(5-Benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent human fatty acid synthase (hFASN) inhibitor (IC50 = 7.7 nM); inhibits hFAS β-ketoacyl reductase activity. Inhibits lipid synthesis and attenuates proliferation of A549 non-small-cell lung cancer cells (EC50 = 15 nM) in vitro.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

GSK 2194069 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 428.48
Formula C25H24N4O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1332331-08-4
PubChem ID 67376285
InChI Key AQTPWCUIYUOEMG-INIZCTEOSA-N
Smiles O=C1NN=C(C[C@@H]2CCN(C(C3CC3)=O)C2)N1C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.85 100
ethanol 8.57 20

Preparing Stock Solutions

The following data is based on the product molecular weight 428.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.67 mL 23.34 mL
5 mM 0.47 mL 2.33 mL 4.67 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Hardwicke et al (2014) A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat.Chem.Biol. 10 774 PMID: 25086508


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Keywords: GSK 2194069, supplier, GSK2194069, fatty, acid, synthases, hFAS, beta-ketoacyl, reductases, b-ketoacyl, β-ketoacyl, lipid, synthesis, inhibitors, inhibits, Fatty, Acid, Synthase, Fatty, Acid, Synthase, Tocris Bioscience

Citations for GSK 2194069

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Cancer

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