Ko 143

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Cat.No. 3241 - Ko 143 | C26H35N3O5 | CAS No. 461054-93-3
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% (HPLC)
Datasheet
Citations (8)
Literature

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.

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Technical Data

M. Wt 469.57
Formula C26H35N3O5
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 461054-93-3
PubChem ID 10322450
InChI Key NXNRAECHCJZNRF-JBACZVJFSA-N
Smiles O=C(N[C@H]4CCC(OC(C)(C)C)=O)[C@]3([H])CC1=C([C@H](CC(C)C)N3C4=O)NC2=C1C=CC(OC)=C2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.48 50
ethanol 46.96 100

Preparing Stock Solutions

The following data is based on the product molecular weight 469.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.13 mL 10.65 mL 21.3 mL
5 mM 0.43 mL 2.13 mL 4.26 mL
10 mM 0.21 mL 1.06 mL 2.13 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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 reference for Ko 143, please let us know.

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

8 Citations for Ko 143

Citations are publications that use Tocris products. Selected citations for Ko 143 include:

Hill et al (2013) Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. J Biol Chem 85 29 PMID: 23063411

Zander et al (2012) EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topotecan resistance in BRCA1-deficient mouse mammary tumors. PLoS One 7 e45248 PMID: 23028879

Lainey et al (2012) Erlotinib antagonizes ABC transporters in acute myeloid leukemia. Cell Cycle 11 4079 PMID: 23095522

Watson et al (2012) The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Antimicrob Agents Chemother 1436 111 PMID: 22200378

Moreno-Sanz et al (2011) The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system. Pharmacol Res 64 359 PMID: 21767647

Westover et al (2015) FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance. Brain Res 14 92 PMID: 25928015

Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572 PMID: 25691630

Moreno-Sanz et al (2014) Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain. Pharmacol Res 87 87 PMID: 24993496


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