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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.