344559 | FTI-2628 - Calbiochem

344559
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₁H₃₄N₄O₃S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      344559-500UG
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          Plastic ampoule 500 μg
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          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 -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.