Table 1.
T138067 is efficacious against MDR tumor cells
| Cell lines | T138067 | Vinblastine | Paclitaxel | Doxorubicin | Actinomycin D |
|---|---|---|---|---|---|
| MCF7 | 165 | 0.98 | 3.3 | 57 | 0.68 |
| MCF7/ADR | 165 (1) | 34 (35) | 150 (46) | 216 (3.8) | 1.67 (2.5) |
| CCRF-CEM | 29 | 2.6 | 2.2 | 550 | 0.35 |
| CCRF-CEM/VBL100 | 35 (1.2) | 471 (181) | 3,390 (1,541) | 2,600 (5.1) | 380 (109) |
| DC-3F | 25 | 3 | 51 | 33 | 0.09 |
| DC-3F/ADX | 47 (1.9) | 1,490 (497) | 3,100 (608) | 1,390 (42) | 419 (4,656) |
| P338 | 11 | 3.4 | 2.9 | 7.4 | 0.15 |
| P338/ADR | 23 (2.1) | 39 (115) | 323 (111) | 1,530 (207) | 1.2 (8) |
Comparison of the effects of T138067, paclitaxel, vinblastine, doxorubicin, and actinomycin D on the growth of human mammary adenocarcinoma (MCF7), human lymphoblastic leukemia (CCRF-CEM), hamster lung cell fibroblast (DC-3F), and murine lymphocytic leukemia (P338) cells and their MDR sublines (MCF7/ADR, CCRF-CEM/VBL100, DC-3F/ADX, and P388/ADR, respectively). The IC50 value (nM) for each agent is shown. The fold increase in drug resistance (numbers shown in parentheses) was calculated from the ratio of the IC50 values for each resistant subline relative to that for the parental cell line.