Relation between the cytostatic action of S2242 and metabolite formation in several cell lines
| Cell | CC50 | S2242-MP2-a | S2242-DP2-a | S2242-TP2-a |
|---|---|---|---|---|
| μg/ml | pmol/106 cells | |||
| CEM/0 | 1.0 ± 0.3 | 194 ± 31 | 150 ± 28 | 160 ± 18 |
| Vero | 12 ± 3.3 | 18 ± 8.0 | 29 ± 5.8 | 19 ± 3.8 |
| HEL | 32 ± 2 | 9.5 ± 4.2 | 13 ± 5.7 | 7.9 ± 3.7 |
| L1210/0 | 42 ± 9 | 8.9 ± 3.6 | 13 ± 9.1 | 7.9 ± 1.0 |
| FM3A/0 | >100 | 0.95 ± 0.05 | 1.2 ± 0.1 | 1.9 ± 0.5 |
The inverse correlation between the CC50 values and S2242-MP, S2242-DP, and S2242-TP levels was .94, .95, and .98, respectively (for this calculation, the CC50 value for FM3A/0 cells was considered to be 100 μg/ml).
↵2-a Cells were incubated with 100 μm[14C]S2242 (44 Ci/mmol) for 24 hr at 37°.