Ko 143

Catalog # Availability Size / Price Qty
3241/1
3241/10
Ko 143 | CAS No. 461054-93-3 | Multidrug Transporter Inhibitors
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Description: Potent and selective BCRP inhibitor

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

Purity: ≥99%

Product Details
Citations (13)
Supplemental Products
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. The inhibitor Ko143 is not specific for ABCG2.
    Weidner et al.
    J.Pharmacol.Exp.Ther., 2015;354:384
  2. 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
  3. Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines.
    Loevezijn et al.
    Bioorg.Med.Chem.Letts., 2001;11:29
  4. Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etop. resistance and transport, but etop. oral availability is limited primarily by P-glycoprotein.
    Allen et al.
    Cancer Res., 2003;63:1339

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Citations for Ko 143

The citations listed below are publications that use Tocris products. Selected citations for Ko 143 include:

13 Citations: Showing 1 - 10

  1. IGF-1 contributes to the expansion of melanoma-initiating cells through an epithelial-mesenchymal transition process.
    Authors: Coz Et al.
    Oncotarget  2016;7:82511
  2. Bioluminescent imaging of ABCG2 efflux activity at the blood-placenta barrier.
    Authors: Kumar Et al.
    Sci Rep  2016;6:20418
  3. A role for ABCG2 beyond drug transport: Regulation of autophagy.
    Authors: Ding Et al.
    Autophagy  2016;12:737
  4. ABCG2 Transporter Expression Impacts Group 3 Medulloblastoma Response to Chemotherapy.
    Authors: Morfouace Et al.
    Cancer Res  2015;75:3879
  5. Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters.
    Authors: Hoque Et al.
    Biochem Pharmacol  2015;59:2572
  6. FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irino. in colon and lung cancer models with ABCG2-induced resistance.
    Authors: Westover Et al.
    Brain Res  2015;14:92
  7. Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain.
    Authors: Moreno-Sanz Et al.
    Pharmacol Res  2014;87:87
  8. Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo.
    Authors: Hill Et al.
    J Biol Chem  2013;85:29
  9. Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.
    Authors: Moreno-Sanz Et al.
    J Med Chem  2013;56:5917
  10. EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topo. resistance in BRCA1-deficient mouse mammary tumors.
    Authors: Zander Et al.
    PLoS One  2012;7:e45248

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