Catalog Number: 3241
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:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Background References
  1. Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.
    Allen et al.
    Mol.Cancer Ther., 2002;1:417
  2. Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein.
    Allen et al.
    Cancer Res., 2003;63:1339
  3. Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines.
    Loevezijn et al.
    Bioorg.Med.Chem.Letts., 2001;11:29
  4. The inhibitor Ko143 is not specific for ABCG2.
    Weidner et al.
    J.Pharmacol.Exp.Ther., 2015;354:384
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