TABLE 1

Ko143-inhibitable efflux of fluorescent compounds in human and mouse ABCG2

Human ABCG2Mouse ABCG2
H460 MX20MCF FLV5003T3 MX15Ltk-HoeR415
SubstratesConc.Exc/EmEffluxa ± S.D. (%)
μM
Mitoxantroneb10 630/66078.3 ± 2.770.8 ± 1.569.9 ± 3.551.6 ± 4.5
Hoechst 33342b1350/53086.9 ± 2.367.6 ± 1.490.0 ± 6.552.9 ± 13.7
BODIPY-Prazosinb250 nM488/53086.8 ± 1.377.4 ± 4.277.8 ± 3.270.4 ± 0.8
Pheophorbide a10630/66085.4 ± 0.680.9 ± 6.091.4 ± 0.846.0 ± 7.9
Pyropheophorbide a methyl ester10630/66090.1 ± 3.169.9 ± 1.080.5 ± 1457.9 ± 12.2
Purpurin-1815630/66092.5 ± 1.476.7 ± 1.067.3 ± 4.766.0 ± 10.4
Chlorin e650630/66084.7 ± 1.652.0 ± 5.072.2 ± 2.348.2 ± 5.5
Daunorubicinb1488/57013.1 ± 1.917.3 ± 2.918.6 ± 11.619.6 ± 11.6
Rhodamine123b2488/5300021.3 ± 1.1c48.8 ± 2.3c
  • a Accumulation is normalized to the fluorescence of cells in each substrate in the presence of Ko143 (10 μM) and the mean percentage difference with and without the inhibitor is recorded. Data represent means ± S.D. of three observations. Negative values were assigned the value of zero.

  • b Also substrates of P-gp.

  • c Due to baseline P-gp efflux.