330000 ESFTs Inhibitor, YK-4-279

330000
  
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      Áttekintés

      Replacement Information

      Kulcsspecifikációk táblázata

      Empirical Formula
      C₁₇H₁₃Cl₂NO₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable dihydroindolone compound that disrupts the Ewing's sarcoma oncogenic transcription factor, EWS-FLI1, complex assembly by competing against RHA (RNA helicase A) binding to EWS-FLI1 (KD = 9.48 µM) and inhibits EWS-FLI1-dependent transcription activity (by 76% and 88% in 18 h with 3 and 10 µM YK-4-279, respectively) in COS7-based reporter assays without affecting NF-κB-mediated transcription even at concentrations as high as 10 µM. Shown to exhibit apoptosis-inducing and antiproliferative activity toward ESFT (Ewing's sarcoma family tumor) cells both in cultures in vitro (IC50 between 0.5 and 8.0 µM) and in mice in vivo (Average tumor growth retardation >50% on day 14; Three 1.5 mg i.p. doses/mouse/day), while displaying little or much reduced activity toward non-EWS-FLI1 cancer cells or nontransformed cells (IC50 ≥25 µM).
      Catalogue Number330000
      Brand Family Calbiochem®
      SynonymsEWS-FLI1 Inhibitor, 4,7-Dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)-1,3-dihydro-2H-indol-2-one
      References
      ReferencesErkizan, H.V., et al. 2009. Nature Med. 15, 750.
      Product Information
      FormTan solid
      Hill FormulaC₁₇H₁₃Cl₂NO₄
      Chemical formulaC₁₇H₁₃Cl₂NO₄
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      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

      ESFTs Inhibitor, YK-4-279 Certificates of Analysis

      TitleLot Number
      330000

      References

      Hivatkozások áttekintése
      Erkizan, H.V., et al. 2009. Nature Med. 15, 750.
      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.

      Revision28-February-2011 RFH
      SynonymsEWS-FLI1 Inhibitor, 4,7-Dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)-1,3-dihydro-2H-indol-2-one
      DescriptionA cell-permeable dihydroindolone compound that disrupts the Ewing's sarcoma oncogenic transcription factor, EWS-FLI1, complex assembly by competing against RHA (RNA helicase A) binding to EWS-FLI1 (KD = 9.48 µM) and inhibits EWS-FLI1-dependent transcription activity (by 76% and 88% in 18 h with 3 and 10 µM YK-4-279, respectively) in COS7-based reporter assays without affecting NF-κB-mediated transcription even at concentrations as high as 10 µM. Shown to exhibit apoptosis-inducing and antiproliferative activity toward ESFT (Ewing's sarcoma family tumor) cells both in cultures in vitro (IC50 between 0.5 and 8.0 µM) and in mice in vivo (Average tumor growth retardation >50% on day 14; Three 1.5 mg i.p. doses/mouse/day), while displaying little or much reduced activity toward non-EWS-FLI1 cancer cells or nontransformed cells (IC50 ≥25 µM).
      FormTan solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₃Cl₂NO₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      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
      ReferencesErkizan, H.V., et al. 2009. Nature Med. 15, 750.