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FGTI-2734 mesylate (1247018-19-4 free base)

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Catalog No. T11282LCas No. 2702297-24-1
Alias FGTI-2734 mesylate

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

FGTI-2734 mesylate (1247018-19-4 free base)

FGTI-2734 mesylate (1247018-19-4 free base)

😃Good
Catalog No. T11282LAlias FGTI-2734 mesylateCas No. 2702297-24-1
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
Pack SizePriceAvailabilityQuantity
5 mg$311Backorder
10 mg$575Backorder
50 mg$1,762Backorder
100 mg$3,081Backorder
200 mgInquiryBackorder
500 mgInquiryBackorder
1 mL x 10 mM (in DMSO)$414Backorder
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Product Introduction

Bioactivity
Description
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
Targets&IC50
FT:250 nM , GGT:520 nM
In vitro
FGTI-2734 mesylate (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells. ??FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.
In vivo
FGTI-2734 mesylate (intraperitoneally;?100 mg/kg/day for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors.
AliasFGTI-2734 mesylate
Chemical Properties
Molecular Weight606.73
FormulaC27H35FN6O5S2
Cas No.2702297-24-1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 75 mg/mL (123.61 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6482 mL8.2409 mL16.4818 mL82.4090 mL
5 mM0.3296 mL1.6482 mL3.2964 mL16.4818 mL
10 mM0.1648 mL0.8241 mL1.6482 mL8.2409 mL
20 mM0.0824 mL0.4120 mL0.8241 mL4.1204 mL
50 mM0.0330 mL0.1648 mL0.3296 mL1.6482 mL
100 mM0.0165 mL0.0824 mL0.1648 mL0.8241 mL

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