Metabolism of [3H]AZT and [3H]CycloSal-AZTMP on 24-h incubation of CEM cells at different initial drug concentrations for 24 h
| Initial AZT Concentration | [CH3−3H]AZT | |||
|---|---|---|---|---|
| AZT (fr 2-3)2-a | AZTMP (fr 10-11)2-a | AZTDP (fr 15-16-17)2-a | AZTTP (fr 25-26-27)2-a | |
| μM | pmol/109cells | |||
| 0.09 | 83 | 8,437 | 261 | 444 |
| 1 | 640 | 41,170 | 450 | 860 |
| 10 | 2,800 | 113,600 | 590 | 840 |
| 100 | 34,000 | 414,000 | 1,900 | 2,700 |
| Initial CycloSal-AZTMP Concentration | [CH3−3H]CycloSal-AZTMP | |||
|---|---|---|---|---|
| AZT + Prodrug (fr 2-3)2-a | AZTMP (fr 10-11)2-a | AZTDP (fr 15-16-17)2-a | AZTTP (fr 25-26-27)2-a | |
| μM | pmol/109cells | |||
| 0.07 | 41 | 4,926 | 148 | 331 |
| 1 | 620 | 36,180 | 370 | 650 |
| 10 | 2,500 | 107,400 | 650 | 940 |
| 100 | 32,000 | 401,000 | 1,800 | 1,500 |
Values are the mean of two of four independent experiments.
↵2-a The values within parentheses represent the elution times (min) (or fraction numbers) of the metabolites. Each fraction contains 1 ml, collected in 1 min.