Ko 143
Tocris Bioscience, part of Bio-Techne | Catalog # 3241
Potent and selective BCRP inhibitor
Key Product Details
Description
Potent and selective BCRP inhibitor
Product Description
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.Product Specifications
Molecular Weight
469.57
Formula
C26H35N3O5
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazinopyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for Ko 143
For research use only
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