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Table 1 EC50 of FL118 and SN-38 in NSCLC and colorectal cancer cell lines, including Top1 inhibitor-resistant HCT116 sub-lines

From: FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance

Cancer type Cell line FL118 EC50 (95%CI) (nM) SN-38 EC50 (95% CI) (nM) RP RR(FL118) RR(SN-38)
NSCLC H460 0.31 (0.21-0.47) 2.84 (1.98-4.09) 9.2   
  EKVX 0.56 (0.38-0.83) 2.58 (1.73-3.80) 4.6   
  A549 0.86 (0.61-1.22) 4.17 (2.30-7.57) 4.8   
Colorectal cancer SW620 0.30 (0.19-0.46) 1.82 (1.06-3.10) 6.1   
  HCT8 0.28 (0.15-0.53) 2.21 (1.38-3.55) 7.9   
  HCT116 0.36 (0.27-0.48) 3.15 (2.42-4.10) 8.8   
   HCT116-SN6 2.28 (1.70-3.05) 7.63 (6.14-9.48) 3.3 6.3 2.4
   HCT116-G7 4.14 (2.78-6.16) 20.3 (13.9-29.6) 4.9 11.5 6.4
   HCT116-SN50 4.04 (2.79-5.86) 135 (80.4-226) 33.4 11.2 42.9
   HCT116-A2 2.13 (1.48-3.07) 51.5(37.4-70.8) 24.2 5.9 16.3
  1. 95% CI = 95% confidence interval.
  2. RP = Relative potency, calculated by dividing the EC50 of SN-38 by the EC50 of FL118.
  3. RR = Relative resistance, calculated by dividing the EC50 of indicated drug in resistant cell line by EC50 in parental cell line.