538005 BHPI - Calbiochem

538005
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      Overview

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38005.0001
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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
          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.