197227 | BCRP Inhibitor III, YHO-13177 - Calbiochem

197227
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₀H₂₂N₂O₃S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      197227-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01 - 1 µM) without altering the BCRP expression levels (in ≤ 6 hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC50 > 10 µM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available (Cat. No. 197228).
          Catalogue Number197227
          Brand Family Calbiochem®
          Synonyms(Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile
          References
          ReferencesYamazaki, R., et al. 2011. Mol. Cancer Ther. 10, 1252.
          Product Information
          FormOrange powder
          Hill FormulaC₂₀H₂₂N₂O₃S
          Chemical formulaC₂₀H₂₂N₂O₃S
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Yamazaki, R., et al. 2011. Mol. Cancer Ther. 10, 1252.
          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-July-2012 JSW
          Synonyms(Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile
          DescriptionA cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01 - 1 µM) without altering the BCRP expression levels (in ≤ 6 hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC50 > 10 µM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available (Cat. No. 197228).
          FormOrange powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₀H₂₂N₂O₃S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 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
          ReferencesYamazaki, R., et al. 2011. Mol. Cancer Ther. 10, 1252.