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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $47 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $198 | In Stock | |
25 mg | $413 | In Stock | |
50 mg | $618 | In Stock | |
100 mg | $879 | In Stock | |
1 mL x 10 mM (in DMSO) | $138 | In Stock |
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 , 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 |
Smiles | Cn1cncc1CN(CCN(CC1CCCCC1)S(=O)(=O)c1ccccn1)c1ccc(cc1F)C#N |
Relative Density. | 1.28 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (97.92 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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