Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

344559 FTI-2628 - Calbiochem

344559
Purchase on Sigma-Aldrich

Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₃₁H₃₄N₄O₃S

Products

Número de referenciaEmbalaje Cant./Env.
344559-500UG Ampolla de plást. 500 μg
Description
Overview

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.

Catalogue Number344559
Brand Family Calbiochem®
Synonyms2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2ʹ-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester
References
ReferencesCarrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.
Product Information
ATP CompetitiveN
FormWhite solid
Hill FormulaC₃₁H₃₄N₄O₃S
Chemical formulaC₃₁H₃₄N₄O₃S
ReversibleN
Structure formula ImageStructure formula Image
Applications
Application CommentsSolubilize in DMSO (10 mg/ml), aliquot & freeze at -20*C; stable for 3 months.
Biological Information
Primary TargetProtein farnesyltransferase (PFTase)
Primary Target IC<sub>50</sub>530 nM for mammalian and 1.0 µM for P. falciparum protein farnesyltransferase activity
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

FTI-2628 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

FTI-2628 - Calbiochem Certificados de análisis

CargoNúmero de lote
344559

Referencias bibliográficas

Visión general referencias
Carrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.
Ficha técnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-June-2008 RFH
Synonyms2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2ʹ-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₁H₃₄N₄O₃S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (200 mg/ml) or Methanol (50 mg/ml)
CommentsSolubilize in DMSO (10 mg/ml), aliquot & freeze at -20*C; stable for 3 months.
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCarrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.