5.38005

BHPI

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₂₁H₁₇NO₃
• Número CAS: 56632-39-4
• Peso molecular: 331.36
• Número MDL: MFCD01919164
• Código UNSPSC: 12352200
• ID de substância PubChem: 3860640
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: CC1=C2C(=CC=C1)C(C(=O)N2)(C3=CC=C(C=C3)O)C4=CC=C(C=C4)O
• chave InChI: FABLAHMQSQFDHR-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
ERα

Reversible: yes

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable