FGTI-2734

FGTI-2734 is a C-terminal mimetic of Ras and a dual inhibitor of farnesyltransferase (FTase) and geranylgeranyl transferase type I (GGTase I, IC50s = 250 and 520 nM, respectively). It inhibits prenylation of H-Ras and Rap1A in oncogenic H-Ras-transformed NIH3T3 cells (IC50s = 88.7 and 2,700 nM, respectively). FGTI-2734 inhibits membrane localization of K-Ras, which requires prenylation to induce oncogenic transformation, in human MIA PaCa-2 pancreatic and H460 lung cancer cells when used at concentrations of 10 and 30 µM. It reduces tumor growth, increases intratumoral p53 levels, induces intratumoral apoptosis, and decreases intratumoral HDJ2 farnesylation and Rap1A geranylgeranylation in patient-derived xenograft (PDX) mouse models of mutant KRAS-expressing pancreatic cancer when administered at doses of 50 or 100 mg/kg per day.Formal Name: N-[2-[(4-cyano-2-fluorophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl]-N-(cyclohexylmethyl)-2-pyridinesulfonamide. CAS Number: 1247018-19-4. Molecular Formula: C26H31FN6O2S. Formula Weight: 510.6. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: N#CC1=CC=C(N(CCN(S(=O)(C2=CC=CC=N2)=O)CC3CCCCC3)CC4=CN=CN4C)C(F)=C1. InChi Code: InChI=1S/C26H31FN6O2S/c1-31-20-29-17-23(31)19-32(25-11-10-22(16-28)15-24(25)27)13-14-33(18-21-7-3-2-4-8-21)36(34,35)26-9-5-6-12-30-26/h5-6,9-12,15,17,20-21H,2-4,7-8,13-14,18-19H2,1H3. InChi Key: BXNRVJLIEMQDOL-UHFFFAOYSA-N.