TABLE 1

Cytotoxicity of anticancer prodrugs and their metabolites toward P450-expressing 9L and CHO cells

Data are mean values based on two independent sets of 4-day cytotoxicity assays for each cell line. EC50 values were calculated using the sigmoidal dose-response (variable slope) method of GraphPad Prism software.



EC50

9L/pBabe
CHO/P450R
9L/2B1-P450R
9L/2B6-P450R
CHO/3A4-P450R
μM
CPA N.D.a N.D. 54.8 105.4 88.7
R-IFA N.D. N.D. 294.8 220.1 57.9
S-IFA N.D. N.D. 91.9 110.6 125.6
4OOH-CPA 3.0 3.2 b
4OOH-IFA 5.1 5.0
CAA
3.2
2.5



  • a N.D., not detectable, indicating <20% toxicity observed at the highest drug concentration tested.

  • b —, not investigated.