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Table 2 Gedatolisib partially reversed ABCG2-medaited MDR

From: ABCB1 and ABCG2 restricts the efficacy of gedatolisib (PF-05212384), a PI3K inhibitor in colorectal cancer cells

Drug IC50 ± SD1(RF2)
LS180 (μM) LS180/MX (μΜ)
Mitoxantrone 0.112 ± 0.007 (1.00) 19.235 ± 2.639 (171.74)
+ Gedatolisib (0.1 μM) 0.132 ± 0.007 (1.18) 17.735 ± 2.489 (158.35)
+ Gedatolisib (0.2 μM) 0.109 ± 0.012 (0.97) 14.824 ± 1.112 (132.36)*
+ Ko143 (1 μM) 0.121 ± 0.009 (1.08) 0.616 ± 0.058 (5.5)*
Topotecan 0.098 ± 0.007 (1.00) 25.683 ± 2.031 (262.07)
+ Gedatolisib (0.1 μM) 0.089 ± 0.009 (0.90) 24.583 ± 1.543 (250.85)*
+ Gedatolisib (0.2 μM) 0.087 ± 0.008 (0.89) 18.632 ± 2.332 (190.12)*
+ Ko143 (1 μM) 0.091 ± 0.009 (1.02) 0.319 ± 0.054 (3.58)*
SN-38 0.111 ± 0.010 (1.00) 8.299 ± 0.923 (74.76)
+ Gedatolisib (0.1 μM) 0.107 ± 0.012 (0.96) 6.990 ± 0.777 (62.97)*
+ Gedatolisib (0.2 μM) 0.106 ± 0.011 (0.95) 5.676 ± 0.859 (51.62)*
+ Ko143 (1 μM) 0.112 ± 0.011 (1.01) 0.277 ± 0.031 (2.50)*
Cisplatin 2.511 ± 0.356 (1.00) 2.445 ± 0.390 (0.97)
+ Gedatolisib (0.1 μM) 2.620 ± 0.321 (1.04) 2.214 ± 0.342 (0.88)
+ Gedatolisib (0.2 μM) 2.582 ± 0.323 (1.03) 2.564 ± 0.367 (1.02)
+ Ko143 (1 μM) 2.391 ± 0.398 (0.95) 2.523 ± 0.369 (1.01)
  1. Resistance fold (RF) was calculated from dividing the IC50 values of LS180/MX cells by the IC50 values of LS180 cells in the presence or absence of gedatolisib or Ko143
  2. *Presents when p value is < 0.05. Data was showed with mean ± SD, which is representative for at least three independent experiments