FGTI-2734, CAS 1247018-19-4

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.

• Artikelnummer: CAY37694-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 37694-1
• Green Labware: Nein
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK