538005 BHPI - Calbiochem

538005
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, bioavailable, non-toxic dihydroindolone derived compound that directly interacts with ERα and noncompetitively inhibits E2-ERα regulated gene expression. Selectively arrests the proliferation of therapy resistant ERα+ cancer cells (0.1 - 1.0 µM; IC50 = 15 nM for T47D cells) with no effect on ERα- cells. Shown to hyperactivate PLCγ, deplete endoplasmic reticulum calcium store, elicit massive UPR, and inhibit protein synthesis continually. Downregulates chaperones synthesis and sustains UPR activated cell death. Rapidly induces tumor regression (>60% inhibition) in mouse MCF-7 xenografts (15 mg/kg, i.p., q.d.).

      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 Number538005
      Brand Family Calbiochem®
      Synonyms3,3-bis(4-Hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one, Estrogen Receptor α Inhibitor
      DescriptionBHPI
      References
      ReferencesAndruska, N.D., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 4737.
      Product Information
      FormWhite powder
      Hill FormulaC₂₁H₁₇NO₃
      Chemical formulaC₂₁H₁₇NO₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetERα
      Purity≥98% 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 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      BHPI - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Andruska, N.D., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 4737.
      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.

      Revision23-September-2016 JSW
      Synonyms3,3-bis(4-Hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one, Estrogen Receptor α Inhibitor
      DescriptionA cell-permeable, bioavailable, non-toxic dihydroindolone derived compound that directly interacts with ERα and noncompetitively inhibits E2-ERα regulated gene expression. Selectively arrests the proliferation of therapy resistant ERα+ cancer cells (0.1 - 1.0 µM; IC50 = 15 nM for T47D cells) with no effect on ERα- cells. Shown to hyperactivate PLCγ, deplete endoplasmic reticulum calcium store, elicit massive UPR, and inhibit protein synthesis continually. Downregulates chaperones synthesis and sustains UPR activated cell death. Rapidly induces tumor regression (>60% inhibition) in mouse MCF-7 xenografts (15 mg/kg, i.p., q.d.).
      FormWhite powder
      Chemical formulaC₂₁H₁₇NO₃
      Purity≥98% 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAndruska, N.D., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 4737.