R&D Systems Inc. Tocris Bioscience Boston Biochem

Ko 143

Cat. No. 3241

Ko 143 C26H35N3O5 [461054-93-3]

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Chemical Name: (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester

Biological Activity

Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.

Technical Data

M.Wt:
469.57
Formula:
C26H35N3O5
Solubility:
Soluble to 50 mM in DMSO and to 100 mM in ethanol
Purity:
>99 %
Storage:
Store at -20°C
CAS No:
461054-93-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

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References

Loevezijn et al (2001) Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg.Med.Chem.Letts. 11 29.

Allen et al (2002) Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol.Cancer Ther. 1 417. PMID: 12477054.

Allen et al (2003) Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein. Cancer Res. 63 1339. PMID: 12649196.

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View Related Products by Target

Keywords: Ko 143, supplier, Potent, selective, BCRP, inhibitors, MDR, Breast, Cancer, Resistance, Protein, Multidrug, Transporters, Ko143, ATP-binding, cassette

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