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Chemical Structure : FGTI-2734
CAS No.: 1247018-19-4
Catalog No.: PC-73014Not For Human Use, Lab Use Only.
FGTI-2734 (FGTI2734) is a potent, CAAX tetrapeptide RAS C-terminal mimetic as dual farnesyltransferase (FT) and geranylgeranyltransferase-1 (GGT-1) inhibitor with IC50 of 250 and 520 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
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| 100 mg | Get quote |
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FGTI-2734 (FGTI2734) is a potent, CAAX tetrapeptide RAS C-terminal mimetic as dual farnesyltransferase (FT) and geranylgeranyltransferase-1 (GGT-1) inhibitor with IC50 of 250 and 520 nM, respectively.
FGTI-2734 inhibits both protein prenylation and membrane localization of KRAS and NRAS in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells, but not the highly selective FTI-2148 or GGTI-2418.
FGTI-2734 inhibits the prenylation of both HDJ2 and RAP1A.
FGTI-2734 inhibits RAF-1 kinase activity although cytosolic KRAS binds RAF-1, it requires KSR and the membrane environment to fully activate RAF-1.
FGTI-2734 induces apoptosis in mutant KRAS-dependent, but not mutant KRAS-independent human cancer cells.
FGTI-2734 inhibits the in vivo growth of mutant KRAS-dependent but not mutant KRAS–independent human tumors in mouse xenograft models (100 mg/kg, i.p.), also inhibits the growth of mutant KRAS PDXs from patients with pancreatic cancer.
| M.Wt | 510.632 | |
| Formula | C26H31FN6O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(2-((4-cyano-2-fluorophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-N-(cyclohexylmethyl)pyridine-2-sulfonamide |
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1. Sebti SM, et al. Clin Cancer Res. 2019 Jun 21. pii: clincanres.3399.2018. doi: 10.1158/1078-0432.CCR-18-3399.
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