Formulation: A solid
Formal Name: N-[2-[(4-cyano-2-fluorophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl]-N-(cyclohexylmethyl)-2-pyridinesulfonamide
Purity: ≥95%
Formula Markup: C26H31FN6O2S
Formula Weight: 510,6
Shelf life (days): 1460
CAS Number: 1247018-19-4
Notes: 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).{72030} 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.{72031} 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.
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