197227

BCRP Inhibitor III, YHO-13177

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

• Synonym(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
• Empirical Formula (Hill Notation): C₂₀H₂₂N₂O₃S
• CAS Number: 912287-56-0
• Molecular Weight: 370.47
• MDL number: MFCD28900680
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C
• SMILES string: OC(CC1)CCN1C(S2)=CC=C2/C=C(C#N)/C3=CC(OC)=C(OC)C=C3

Description

General description

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).

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable