5.38005

BHPI

• Synonyme(s) : BHPI, 3,3- bis(4-Hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one, Estrogen Receptor α Inhibitor, 3,3-bis(4-Hydroxyphenyl)-7-methyl-1,3-dihydro-2H-indol-2-one, Estrogen Receptor α Inhibitor
• Formule empirique (notation de Hill): C₂₁H₁₇NO₃
• Numéro CAS: 56632-39-4
• Poids moléculaire : 331.36
• Code UNSPSC : 12352200
• ID de substance PubChem : 3860640
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: CC1=C2C(=CC=C1)C(C(=O)N2)(C3=CC=C(C=C3)O)C4=CC=C(C=C4)O

Description

Description générale

A 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.).

A 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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
ERα

Reversible: yes

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

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

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable