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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: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 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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      Übersicht

      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
      Bestellnummer GTIN
      344559 0

      Documentation

      FTI-2628 - Calbiochem Analysenzertifikate

      TitelChargennummer
      344559

      Literatur

      Übersicht
      Carrico, D., et al. 2004. Bioorg. Med. Chem. 12, 6517.
      Ohkanda, J., et al. 2004. J. Med. Chem. 47, 432.
      Datenblatt

      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.