197228

BCRP Inhibitor IV, YHO-13351

The BCRP Inhibitor IV, YHO-13351 controls the biological activity of BCRP.

• Synonym(s): BCRP Inhibitor IV, YHO-13351, Diethylaminoacetic acid, 1-(5-(( Z)-2-cyano-2-(3,4-dimethoxyphenyl)vinyl)thiophen-2-yl)piperidin-4-yl ester, Methanesulfonate, Diethylaminoacetic acid, 1-(5-((Z)-2-cyano-2-(3,4-dimethoxyphenyl)vinyl)thiophen-2-yl)piperidin-4-yl ester, Methanesulfonate
• Empirical Formula (Hill Notation): C₂₆H₃₃N₃O₄S · xCH₄O₃S
• Molecular Weight: 483.62 (free base basis)
• UNSPSC Code: 12352200
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated (hygroscopic), protect from light
• color: yellow
• solubility: water: 25 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• SMILES string: O=C(CN(CC)CC)OC(CC1)CCN1C(S2)=CC=C2/C=C(C(C=C3)=CC(OC)=C3OC)\C#N.[xCH3SO3H]

Description

General description

An in vivo bioavailable (~87%; t_1/2<5 mins. during p.o. and i.v. administration) and highly water soluble (>100 mg/ml) diethylaminoacetate prodrug of YHO-13177 (Cat. No. 197227) that reverses BCRP-mediated irinotecan resistance in P388/BCRP and HCT116/BCRP xenograft mouse models, and suppresses tumor growth and significantly enhances the survival (100 or 200 mg/kg, i.p.).

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

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