Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 47.00 | |
5 mg | In stock | $ 122.00 | |
10 mg | In stock | $ 198.00 | |
25 mg | In stock | $ 413.00 | |
50 mg | In stock | $ 618.00 | |
100 mg | In stock | $ 879.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 138.00 |
Description | FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors. |
Targets&IC50 | GGTase I:520 nM , Farnesyl transferase (FTase):250 nM |
In vitro | FGTI-2734 (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.?FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.?FGTI-2734 (1-30 μM;?72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. |
In vivo | FGTI-2734 (intraperitoneally;?100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors. |
Molecular Weight | 510.63 |
Formula | C26H31FN6O2S |
CAS No. | 1247018-19-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (97.92 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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FGTI-2734 1247018-19-4 Metabolism Transferase pancreatic patient-derived geranylgeranyl farnesyl inhibit Farnesyl Transferase mimetic Inhibitor membrane Ftase FGTI 2734 KRAS C-terminal transferase tumors localization FGTI2734 inhibitor