500614 | Survivin Inhibitor III, LLP-3 - Calbiochem

500614
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      概要

      Replacement Information

      主要スペック表

      Empirical Formula
      C₃₂H₂₃ClN₂O₄

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      カタログ番号在庫状況 包装 Qty/Pk 価格 数量
      5.00614.0001
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          ガラスビン 10 mg
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          Description
          OverviewA cell-permeable, dihydropyridinone compound that selectively disrupts survivin-Ran interaction in cell-free binding assays (IC50 <0.3 µM) and in U87 glioma cells (by 55% in 24 h; 20 µM) via direct binding at survivin protein-protein interaction interface, while exhibiting much reduced or little potency against survivin-Smac/DIABLO, survivin-survivin, or XIAP-Smac/DIABLO interaction. LLP-3 treatment abrogates neurosphere formation in GMB cultures (IC50 ≤35 µM) by selectively depleting CD133+ GSC population via apoptosis induction. TMZ (Cat. No. 500609), in comparison, enriches GMB GSC population by preferentially eradicating non-GSC population. LLP-3 is also efficacious in treating human GMB xenograft in mice in vivo (25 mg/kg/day via i.p.).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number500614
          Brand Family Calbiochem®
          SynonymsSurvivin-Ran Interaction Blocker, LLP3, 4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile
          References
          ReferencesGuvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.
          Product Information
          FormYellow solid
          Hill FormulaC₃₂H₂₃ClN₂O₄
          Chemical formulaC₃₂H₂₃ClN₂O₄
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targetsurvivin
          Purity≥99% 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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          (M)SDS

          タイトル

          英語版製品安全データシート((M)SDS) 

          参考資料

          参考資料の概要
          Guvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.
          データシート

          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.

          Revision10-May-2013 JSW
          SynonymsSurvivin-Ran Interaction Blocker, LLP3, 4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile
          DescriptionA cell-permeable, bioavailable dihydropyridinone compound that selectively disrupts survivin-Ran interaction (IC50 <0.3 µM) in cell-free binding assays and in cells (by 55% in U87 glioma cells after 24 h 20 µM treatment) via direct binding at survivin protein-protein interaction interface, while exhibiting much reduced or little potency against survivin-Smac/DIABLO, survivin-survivin, or XIAP-Smac/DIABLO interaction. Survivin and Ran expressions are reported to be upregulated in GSCs (glioma stem cells; CD133-/Nestin-/Sox2-/MELK-positive and TuJ1-negative) when compared to non-GSC (TuJ1-positive) population in patients-derived GMB (Glioblastoma multiforme) cultures and LLP-3 treatment abrogates neurosphere formation in GMB cultures (IC50 ≤35 µM) by selectively depleting CD133+ GSC population (89% drop of CD133+ population vs. 33% drop in CD133- population in GBM528 cultures after 7 d 25 µM treatment) via apoptosis induction. TMZ treatment, in comparison, results in GMB GSC population enrichment by preferentially eradicating non-GSC population. LLP-3 is also efficacious in treating human GMB xenograft in mice in vivo (median survival days = 35 vs. 15.5 with or without treatment; 25 mg/kg/day via i.p.; 5 d/wk for 2 wks starting d10 post GMB xenograft). TMZ (Cat. No. 500609), in comparison, enriches GMB GSC population by preferentially eradicating non-GSC population.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₃₂H₂₃ClN₂O₄
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage +2°C to +8°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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesGuvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.