Table 3.
Results of NCI-USA in vitro five-dose testing for conjugate 8a (NSC: D- 795311/1).
| Subpanel/tumour cell lines | Compound |
|||
|---|---|---|---|---|
| 8a | ||||
| GI50 (µM) | TGI (µM) | LC50 (µM) | ||
| Leukaemia | ||||
| CCRF-CEM | 1.94 | >100 | >100 | |
| HL60(TB) | 1.31 | 4.80 | >100 | |
| K-562 | 2.22 | 20.5 | >100 | |
| MOLT-4 | 0.68 | 4.54 | >100 | |
| RPMI-8226 | 1.33 | 3.96 | >100 | |
| SR | 0.52 | 8.72 | >100 | |
| Non-small cell lung cancer | ||||
| A549/ATCC | 7.18 | 39.6 | >100 | |
| EKVX | 2.36 | >100 | >100 | |
| HOP-62 | 4.17 | 25.0 | >100 | |
| HOP-92 | 1.87 | 6.57 | >100 | |
| NCI-H226 | 2.95 | 20.6 | >100 | |
| NCI-H23 | 3.13 | 38.2 | >100 | |
| NCI-H322M | 3.42 | >100 | >100 | |
| NCI-H460 | 2.17 | 10.6 | 75.7 | |
| NCI-H522 | 1.81 | 6.59 | >100 | |
| Colon cancer | ||||
| COLO 205 | 1.25 | 3.06 | 7.46 | |
| HCC-2998 | 2.09 | 5.14 | 19.0 | |
| HCT-116 | 1.75 | 4.17 | 9.96 | |
| HCT-15 | 2.63 | 42.2 | >100 | |
| HT29 | 3.4 | >100 | >100 | |
| KM12 | 3.22 | 19.7 | >100 | |
| SW-620 | 2.97 | 35.3 | >100 | |
| CNS cancer | ||||
| SF-268 | 3.33 | 28.0 | >100 | |
| SF-295 | 8.41 | 96.6 | >100 | |
| SF-539 | 2.69 | 17.1 | >100 | |
| SNB-19 | 4.24 | >100 | >100 | |
| SNB-75 | 2.31 | 46.0 | >100 | |
| U251 | 3.51 | 17.3 | >100 | |
| Melanoma | ||||
| LOX IMVI | 1.26 | 3.06 | 7.41 | |
| MALME-3M | 1.88 | 6.03 | 100 | |
| M14 | 1.92 | 4.70 | 17.2 | |
| MDA-MB-435 | 1.50 | 2.96 | 5.85 | |
| SK-MEL-2 | 2.42 | 8.03 | >100 | |
| SK-MEL-28 | 4.70 | 36.9 | >100 | |
| SK-MEL-5 | 2.86 | 13.50 | 39.0 | |
| UACC-257 | 12.30 | 66.60 | >100 | |
| UACC-62 | 2.24 | 12.10 | >100 | |
| Ovarian cancer | ||||
| IGROV1 | 3.38 | 63.10 | >100 | |
| OVCAR-3 | 1.36 | 5.11 | >100 | |
| OVCAR-4 | 0.93 | 25.60 | >100 | |
| OVCAR-5 | 4.04 | 25.8 | >100 | |
| OVCAR-8 | 5.41 | >100 | >100 | |
| NCI/ADR-RES | 6.39 | 89.90 | >100 | |
| SK-OV-3 | 1.17 | 67.10 | >100 | |
| Renal cancer | ||||
| 786-0 | 5.94 | 71.20 | >100 | |
| A498 | 1.37 | 7.50 | >100 | |
| ACHN | 3.56 | >100 | >100 | |
| RXF 393 | 2.17 | 7.94 | >100 | |
| SN12C | 3.20 | 75.90 | >100 | |
| TK-10 | 11.10 | >100 | >100 | |
| UO-31 | 2.28 | 6.18 | >100 | |
| Prostate cancer | ||||
| PC-3 | 1.83 | 5.17 | 47.40 | |
| DU-145 | 3.88 | 40.60 | >100 | |
| Breast cancer | ||||
| MCF7 | 1.54 | 15.50 | >100 | |
| MDA-MB-231/ATCC | 1.81 | 7.40 | >100 | |
| HS 578T | 11.3 | >100 | >100 | |
| BT-549 | 1.79 | 6.33 | >100 | |
| T-47D | 0.41 | 18.40 | >100 | |
| MDA-MB-468 | 1.69 | 5.78 | 79.40 | |
NT: not tested.