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538005 BHPI - CAS 56632-39-4 - Calbiochem

A bioavailable, noncompetitive E2-ERα regulated gene expression inhibitor. Effective in therapy-resistant ERa-positive cancer cells by sustained UPR activated cell death.

BHPI - CAS 56632-39-4 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 3,3-bis(4-Hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one, Estrogen Receptor α Inhibitor

538005
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Aperçu

Replacement Information

Products

RéférenceConditionnement Qté
5380050001 Flacon en verre 10 mg
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
CAS number56632-39-4
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
Global Trade Item Number
Référence GTIN
5380050001 04054839119415

Documentation

BHPI - CAS 56632-39-4 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Andruska, N.D., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 4737.
Fiche technique

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
CAS number56632-39-4
Chemical formulaC₂₁H₁₇NO₃
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°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
ReferencesAndruska, N.D., et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 4737.