1. Metabolic Enzyme/Protease
  2. Farnesyl Transferase
  3. FGTI-2734

FGTI-2734 

Cat. No.: HY-128350
Handling Instructions

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

For research use only. We do not sell to patients.

FGTI-2734 Chemical Structure

FGTI-2734 Chemical Structure

CAS No. : 1247018-19-4

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Description

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1].

IC50 & Target

IC50: 250 nM (FT) and 520 nM (GGT)[1]

In Vitro

FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells[1].
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[1].

Apoptosis Analysis[1]

Cell Line: MiaPaCa2, L3.6pl and Calu6 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 72 hours
Result: Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.

Western Blot Analysis[1]

Cell Line: KRAS, HRAS, and NRAS-transformed NIH3T3 cells
Concentration: 3, 10, 30 μM
Incubation Time: 72 hours
Result: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.
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[1].

Animal Model: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
Dosage: 100 mg/kg
Administration: Intraperitoneally; daily; for 18 to 25 days
Result: Inhibited tumor growth in mutant KRAS-dependent tumors.
Molecular Weight

510.63

Formula

C₂₆H₃₁FN₆O₂S

CAS No.

1247018-19-4

SMILES

O=S(C1=NC=CC=C1)(N(CCN(C2=CC=C(C#N)C=C2F)CC3=CN=CN3C)CC4CCCCC4)=O

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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