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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C26H33N3O4S · xCH4O3S
Molecular Weight:
483.62 (free base basis)
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Level

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]

General description

An in vivo bioavailable (~87%; t1/2<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)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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