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344559

Sigma-Aldrich

FTI-2628 - Calbiochem

A cell-permeable benzyl ester prodrug form of FTI-2148 that preferentially inhibits protein farnesyltransferase activity.

Synonym(s):

FTI-2628 - Calbiochem, 2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2ʹ-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester

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About This Item

Empirical Formula (Hill Notation):
C31H34N4O3S
Molecular Weight:
542.69
UNSPSC Code:
12352200

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 200 mg/mL
methanol: 50 mg/mL

shipped in

wet ice

storage temp.

−20°C

General description

This product has been discontinued.



A cell-permeable benzyl ester prodrug form of FTI-2148 (Cat. No. 344557) that preferentially inhibits protein farnesyltransferase activity (IC50 = 530 nM for mammalian and 1.0 µM for P. falciparum) over protein geranylgeranyltransferase-I (IC50 >10 µM for mammalian) and displays anti-malarial properties. Potently disrupts Ras farnesylation in H-Ras-transformed NIH 3T3 cells (IC50 = 20 nM) and inhibits the growth of P. falciparum in red blood cells (ED50 = 150 nM). Also suppresses parasitemia in P. berghei-infected mice by 46.1% (50 mg/kg, ip) with no apparent toxicity.

A cell-permeable prodrug form of FTI-2148 (Cat. No. 344557) that preferentially inhibits protein farnesyltransferase activity (IC50 = 530 nM for mammalian and 1.0 µM for P. falciparum) over protein geranylgeranyltransferase-I (IC50 >10 µM for mammalian) and displays anti-malarial properties. Potently disrupts Ras farnesylation in H-Ras-transformed NIH 3T3 cells (IC50 = 20 nM) and inhibits the growth of P. falciparum in red blood cells (ED50 = 150 nM). Also suppresses parasitemia in P. berghei-infected mice by 46.1% (50 mg/kg, ip) with no apparent toxicity.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Protein farnesyltransferase (PFTase)
Product does not compete with ATP.
Reversible: no
Target IC50: 530 nM for mammalian and 1.0 µM for P. falciparum protein farnesyltransferase activity

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Carrico, D., et al. 2004. Bioorg. Med. Chem.12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem.47, 432.
Solubilize in DMSO (10 mg/ml), aliquot & freeze at -20*C; stable for 3 months.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

10-13 - German Storage Class 10 to 13

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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