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. Inhibits ABCB1 and ABCC1 at higher concentrations. Rapidly metabolized in rat plasma.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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.

Weidner et al (2015) The inhibitor Ko143 is not specific for ABCG2. J.Pharmacol.Exp.Ther. 354 384. PMID: 26148857.

If you know of a relevant citation for this product please let us know.

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

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