A potent and selective inhibitor of BCRP

Ko 143 – 10 mg

Brand:
Cayman
CAS:
461054-93-3
Storage:
-20
UN-No:
Non-Hazardous - /

Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer.{24807} BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs.{24809,24808} Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).{24809} It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.{24809} Ko 143 is effective in vivo in mice.{24809,24808}  

 

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Description

A potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively); effective in vivo in mice

Formal name: (3S,6S,12aS)-1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-pyrazino[1′,2′:1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester

Synonyms: 

Molecular weight: 469.6

CAS: 461054-93-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Multidrug Resistance

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