526560 PI 3-Kδ/γ Inhibitor XV, SW-14 - Calbiochem

526560
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₈H₂₂FN₇O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      526560-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA cell permeable, ATP competitive tolyl quinazolinone inhibitor of PI 3-Kδ/γ that displays 70-fold selectivity over PI 3-Kβ and 900-fold selectivity over PI 3-Kα in enzymatic assays with an IC50 = 9 nM for PI3Kδ and 21 nM for PI 3-Kγ and in a cell-based assay with an EC50 = 132 nM for PI 3-Kδ and 4.5 nM for PI 3-K γ. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs stimulated with lipopolysacharide. Additionally, TNFα production decreases dose-dependently in the same cell lines treated with 370 nM to 10 µM of compound. SW14 exhibits a stronger effect compared to that of PI 3-Kδ inhibition (SW30) or pan-PI 3-K inhibition with different anti-inflammatory profile. In contrast to PI 3-Kα/β it also shows very little anti-proliferative effects even at the highest dose tested (10 µM) in HUVEC culture only.
          Catalogue Number526560
          Brand Family Calbiochem®
          Synonyms2-((4-amino-3-(3-fluoro-4-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one, PI 3-K Inhibitor XV
          References
          ReferencesWilliams, O., et al. 2010. Chem Biol. 17, 123.
          Product Information
          FormWhite powder
          Hill FormulaC₂₈H₂₂FN₇O₂
          Chemical formulaC₂₈H₂₂FN₇O₂
          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 Shipped with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -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.
          Packaging Information
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          526560

          References

          Reference overview
          Williams, O., et al. 2010. Chem Biol. 17, 123.
          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.

          Revision15-October-2011 RFH
          Synonyms2-((4-amino-3-(3-fluoro-4-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one, PI 3-K Inhibitor XV
          DescriptionA cell permeable, ATP competitive tolyl quinazolinone inhibitor of PI 3-Kδ/γ that displays 70-fold selectivity over PI 3-Kβ and 900-fold selectivity over PI 3-Kα in enzymatic assays with an IC50 = 9 nM for PI3Kδ and 21 nM for PI 3-Kγ and in a cell-based assay with an EC50 = 132 nM for PI 3-Kδ and 4.5 nM for PI 3-K γ. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs stimulated with lipopolysacharide. Additionally, TNFα production decreases dose-dependently in the same cell lines treated with 370 nM to 10 µM of compound. SW14 exhibits a stronger effect compared to that of PI 3-Kδ inhibition (SW30) or pan-PI 3-K inhibition with different anti-inflammatory profile. In contrast to PI 3-Kα/β it also shows very little anti-proliferative effects even at the highest dose tested (10 µM) in HUVEC culture only.
          FormWhite powder
          Chemical formulaC₂₈H₂₂FN₇O₂
          Structure formulaStructure formula
          Purity>95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -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
          ReferencesWilliams, O., et al. 2010. Chem Biol. 17, 123.