Ko 143

Name: Ko 143
Brand: Tocris Bioscience
SKU: 3241

Tocris Bioscience, part of Bio-Techne | Catalog # 3241

Citations (95)

COA / SDS

Potent and selective BCRP inhibitor

Key Product Details

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)
Molecular Weight:	469.57

View Full Technical Details for Ko 143

Technical Data
Citations

Biological Activity for Ko 143

Ko 143 is a 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.

Compound Libraries for Ko 143

Ko 143 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Ko 143

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.

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

Solubility for Ko 143

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

Preparing Stock Solutions for Ko 143

The following data is based on the product molecular weight 469.57.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.13 mL	10.65 mL	21.30 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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References for Ko 143

References are publications that support the biological activity of the product.

Weidner The inhibitor Ko143 is not specific for ABCG2. J.Pharmacol.Exp.Ther. 2015 PMID: 26148857
Allen Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etop. resistance and transport, but etop. oral availability is limited primarily by P-glycoprotein. Cancer Res. 2003 PMID: 12649196
Loevezijn Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg.Med.Chem.Letts. 2001 PMID: 11140726
Allen 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. 2002 PMID: 12477054