1. Metabolic Enzyme/Protease
  2. Farnesyl Transferase
  3. FTI-2148 diTFA

FTI-2148 diTFA 

Cat. No.: HY-118916A
Handling Instructions

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.

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

FTI-2148 diTFA Chemical Structure

FTI-2148 diTFA Chemical Structure

CAS No. : 817586-01-9

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Description

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively[1].

IC50 & Target

IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]

In Vitro

FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].
FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: KRAS HRAS, and NRAS-transformed NIH3T3 cells 
Concentration: 30 μM
Incubation Time:
Result: Inhibited the prenylation of KRAS and NRAS.
In Vivo

FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model[1].
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[3].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ras transgenic mouse model[3]
Dosage: 100 mg/kg/day
Administration: Subcutaneous injection; 100 mg/kg/day; 14 days
Result: Reduced regression by 87 ± 3% of mammary carcinomas in mice.
Molecular Weight

680.62

Formula

C₂₈H₃₀F₆N₄O₇S

CAS No.
SMILES

CSCC[[email protected]@H](C(O)=O)NC(C1=CC=C(CNCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

Ethanol : 5 mg/mL (7.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4692 mL 7.3462 mL 14.6925 mL
5 mM 0.2938 mL 1.4692 mL 2.9385 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

  • 2.

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

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

  • 3.

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

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

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

FTI-2148 diTFAFarnesyl TransferaseFtasemammarycarcinomasA-549lungcanceradenocarcinomaGGTase IFTaseInhibitorinhibitorinhibit

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FTI-2148 diTFA
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