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

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of FTI-2148 diTFA:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

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.

817586-01-9

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.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

FTI-2148 diTFAFarnesyl TransferaseFtasemammarycarcinomasA-549lungcanceradenocarcinomaGGTase IFTaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
FTI-2148 diTFA
Cat. No.:
HY-118916A
Quantity:
MCE Japan Authorized Agent: