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Ko-143

Chemical Structure : Ko-143

CAS No.: 461054-93-3

Ko-143 (Ko143)

Catalog No.: PC-42054Not For Human Use, Lab Use Only.

Ko-143 is a nontoxic analog of fungal toxin fumitremorgin C and potent, orally bioavailable inhibitor of BCRP (ABCG2) with EC90 of 26 nM.

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Biological Activity

Ko-143 is a nontoxic analog of fungal toxin fumitremorgin C and potent, orally bioavailable inhibitor of BCRP (ABCG2) with EC90 of 26 nM.
Ko-143 shows low activity against P-gp, MRP1 and other known drug transporter.
Ko-143 has an effect on the transport activity of both ABCB1 and ABCC1 at >1 uM.
Ko-143 reverses Bcrp-mediated drug resistance and markedly increases the oral availability of topotecan in mice.

Physicochemical Properties

M.Wt 469.5732
Formula C26H35N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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)-

References

1. Allen JD, et al. Mol Cancer Ther. 2002 Apr;1(6):417-25.

2. Weidner LD, et al. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93.

3. Ozvegy-Laczka C, et al. J Biol Chem. 2005 Feb 11;280(6):4219-27.

4. Elkind NB, et al. Cancer Res. 2005 Mar 1;65(5):1770-7.

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