197227

BCRP Inhibitor III, YHO-13177

The BCRP Inhibitor III, YHO-13177 controls the biological activity of BCRP.

• Sinônimo(s): BCRP Inhibitor III, YHO-13177, ( Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile, (Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile
• Fórmula empírica (Notação de Hill): C₂₀H₂₂N₂O₃S
• Número CAS: 912287-56-0
• Peso molecular: 370.47
• Número MDL: MFCD28900680
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: orange
• solubilidade: DMSO: 100 mg/mL
• Condições de expedição: wet ice
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: OC(CC1)CCN1C(S2)=CC=C2/C=C(C#N)/C3=CC(OC)=C(OC)C=C3

Descrição

Descrição geral

A cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01 - 1 µM) without altering the BCRP expression levels (in ≤ 6 hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC₅₀ >10 µM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available (Cat. No. 197228).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Yamazaki, R., et al. 2011. Mol. Cancer Ther.10, 1252.

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