TABLE 1.
Mean IC50 values for GSK3179106 and motesanib against RET kinase in enzyme or cell-based assays
Values are mean IC50 ± S.D. of at least two experiments.
| Assay |
GSK3179106 |
Motesanib |
|---|---|---|
| nM | nM | |
| Human RET enzyme | 0.4 ± 0.2a | 46.9 ± 25.4a |
| Rat RET enzyme | 0.2 ± 0.1 | NA |
| TT cell phospho-RET | 11.1 ± 1.1a | 559.9 ± 219.5a |
| SK-N-AS cell phospho-RET | 4.6 ± 1.7 | 612.2 ± 197.0 |
| TT cell proliferation | 25.5 ± 3.4 | 1502.0 ± 540.7 |
| SK-N-AS cell proliferation | >10,000 | NA |
| A549 cell proliferation | 17,173 ± 5310b | 20,646 ± 4809b |
NA, not available.
a
Data previously reported (Schenck Eidam et al., 2018).
b
Value is mean IC30 ± S.D. of at least seven experiments.