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344559 FTI-2628 - Calbiochem

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

FTI-2628 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(((5-((1H-Imidazol-4-ylmethyl)-amino)-methyl)-2ʹ-methyl-biphenyl-2-carbonyl)-amino)-4-methylsulfanyl-butyric acid benzyl ester

Primary Target: Protein farnesyltransferase (PFTase)
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₁H₃₄N₄O₃S
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
Global Trade Item Number
Catalogue Number GTIN
344559 0

Documentation

FTI-2628 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

FTI-2628 - Calbiochem Certificates of Analysis

TitleLot Number
344559

References

Reference overview
Carrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.
Data Sheet

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 Protect from light
-20°C
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.