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

FGTI-2734 mesylate 

Cat. No.: HY-128350A Purity: 98.73%
Handling Instructions

FGTI-2734 mesylate 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 mesylate 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 mesylate Chemical Structure

FGTI-2734 mesylate Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 467 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

FGTI-2734 mesylate 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 mesylate 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 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells[1].
FGTI-2734 mesylate (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, Calu6 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 72 hours
Result: Induced apoptosis in mutant KRAS-dependent human cancer cell lines

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 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[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

606.73

Formula

C₂₇H₃₅FN₆O₅S₂

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (123.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6482 mL 8.2409 mL 16.4818 mL
5 mM 0.3296 mL 1.6482 mL 3.2964 mL
10 mM 0.1648 mL 0.8241 mL 1.6482 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FGTI-2734FGTI2734FGTI 2734Farnesyl TransferaseFtaseC-terminalmimeticfarnesyltransferasegeranylgeranylmembranelocalizationKRASpatient-derivedpancreatictumorsInhibitorinhibitorinhibit

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FGTI-2734 mesylate
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HY-128350A
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