Table 2.
Antifolate | IC50 | |
---|---|---|
In vitro (µM) | In situ (nM) | |
1 | >20 | >1000 |
2 | 2.44 (0.12) | 18(2.0) |
3 | 0.15 (0.01) | 6.8(0.9) |
4 | 2.26 (0.16) | 7.2(1.8) |
5 | 2.51 (0.25) | 8.6(0.7) |
Pemetrexed | >20 | 30(7.7) |
Lometrexol | 0.78 (0.08) | 14(5.6) |
GARFTase inhibition assays, both in vitro and in situ, were performed as described in the Experimental Section. The IC50 data shown are mean values from 3 (in vitro; SEM in parentheses) or 2 (in situ; range in parentheses) experiments.