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500614 Survivin Inhibitor III, LLP-3 - Calbiochem

500614
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₂H₂₃ClN₂O₄

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      Glass bottle 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®
      Synonyms4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile, Survivin-Ran Interaction Blocker, LLP3
      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
      Quality LevelMQ100
      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

      Survivin Inhibitor III, LLP-3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Guvenc, H., et al. 2013. Clin. Cancer Res. 19, 1.
      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.

      Revision10-May-2013 JSW
      Synonyms4-(3,5-bis(Benzyloxy)phenyl)-6-(5-chloro-2-hydroxyphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile, Survivin-Ran Interaction Blocker, LLP3
      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.