SML1259

GSK2194069

≥97% (HPLC)

• Synonym(s): (S)-4-(4-(Benzofuran-5-yl)phenyl)-3-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)methyl)-1H-1,2,4-triazol-5(4H)-one
• Empirical Formula (Hill Notation): C₂₅H₂₄N₄O₃
• CAS Number: 1332331-08-4
• Molecular Weight: 428.48
• MDL number: MFCD28167807
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825751
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: powder
• color: white to light brown
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: 2-8°C
• SMILES string: O=C(C1CC1)N2CC[C@@H](CC(N3C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4)=NNC3=O)C2
• InChI: 1S/C25H24N4O3/c30-24(18-1-2-18)28-11-9-16(15-28)13-23-26-27-25(31)29(23)21-6-3-17(4-7-21)19-5-8-22-20(14-19)10-12-32-22/h3-8,10,12,14,16,18H,1-2,9,11,13,15H2,(H,27,31)/t16-/m0/s1
• InChI key: AQTPWCUIYUOEMG-INIZCTEOSA-N

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable