197227 BCRP Inhibitor III, YHO-13177 - Calbiochem

197227
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₀H₂₂N₂O₃S

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197227-10MG
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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
      Quality LevelMQ100
      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

      BCRP Inhibitor III, YHO-13177 - Calbiochem MSDS

      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.