Table 1.
Relative receptor binding affinities and mitogenic potencies in L6hIR, H4IIE and COLO-205 cells.
| Compound | Mutations | hIR-A binding affinity (% of HI) | hIGF-1R binding affinity (% of HI) | mitogenic potency L6hIR cells (% of HI) | mitogenic potency H4IIE cells (% of HI) | Relative mitogenic potency COLO- 205 cells (% of HI) |
|---|---|---|---|---|---|---|
| HI | None | 100 | 100 | 100 | 100 | 100 |
| IX10 | B10Asp | 251 [231; 272] | 492 [472; 514] | 204 [155; 269] | 409 [347; 481] | 640 [472–870]* |
| Analogue A | A8Arg, B26Glu, B28Glu, desB30 | 398 [375; 422] | 18 [17; 19] | 76 [60; 97] | 158 [128; 196] | 23 [18–30] |
| Analogue B | A21Arg, B10Glu, B29Arg, B31Arg, B32Pro, B33Lys | 87 [80; 95] | 2465 [2261; 2688] | 83 [72; 96] | 115 [93; 142] | 4218 [3163–5625] |
Data are weighted mean values with 95% confidence intervals from at least three independent experiments.
*As reported previously10.