| Identification | Back Directory | [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 | [CAS]
461054-93-3 | [Synonyms]
Ko 143
12aS)-
4-dioxo-
6]pyrido[3
Ko143 ,99%
Pyrazino[1'
Ko143 hydrate
KO 143;KO-143;KO143
4-b]indole-3-propanoicacid
12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1
1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino
(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2'
tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7, 12,12a-octahydropyrazino[1
tert-butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl)propanoate
(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
(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 hydrate
Pyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid, 1,2,3,4,6,7,12,12a-octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-, 1,1-dimethylethyl ester, (3S,6S,12aS)-(Ko143) | [Molecular Formula]
C26H35N3O5 | [MDL Number]
MFCD11042273 | [MOL File]
461054-93-3.mol | [Molecular Weight]
469.57 |
| Chemical Properties | Back Directory | [Melting point ]
147 ºC | [Boiling point ]
689.8±55.0 °C(Predicted) | [density ]
1.24 | [storage temp. ]
Desiccate at -20°C | [solubility ]
DMSO: >10mg/mL | [form ]
powder | [pka]
13.31±0.60(Predicted) | [color ]
white to off-white | [Stability:]
Stable for 2 years from date of purchase as supplied. Protect from exposure to moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer. BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs. Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively). It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1. Ko 143 is effective in vivo in mice. | [Uses]
A potent BCRP (breast cancer resistance protein) inhibitor | [Definition]
ChEBI: LSM-6260 is a member of beta-carbolines and a tert-butyl ester. | [Biological Activity]
Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC 90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. | [Biochem/physiol Actions]
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner. | [storage]
Store at -20°C | [References]
1) 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
2) Weidner et al. (2015), The Inhibitor Ko143 Is Not Specific for ABCG2; J. Pharmacol. Exp. Ther., 354 384
3) Palasuberniam et al. (2015), ABCG2 transporter inhibitor restores the sensitivity of triple negative breast cancer cells to aminolevulinic acid-mediated photodynamic therapy; Sci. Rep., 5 13298
4) 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
5) Sabnis et al. (2017),?The Efflux Transporter ABCG2 Maintains Prostate Stem Cells;? Mol. Cancer Res., 15 128 |
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