TABLE 5.
Inhibition of receptor phosphorylation
IC50 (values in nm) are calculated using GraphPad Prism 6 software. NF indicates no fit is used when either Prism does not return a value (e.g. “ambiguous”) or the fit is poor (95% confidence interval range is >4-fold). ND = not determined.
| Molecule and receptor | H292 |
SNU-5 |
H1993 |
||||||
|---|---|---|---|---|---|---|---|---|---|
| IC50 | S.E. | n | IC50 | S.E. | n | IC50 | S.E. | n | |
| JNJ-61186372 | |||||||||
| Phosphorylated EGFR | 29 | ND | 1 | 15 | 2.8 | 2 | 3.8 | 0.22 | 3 |
| Phosphorylated c-MET | 0.86 | 0.067 | 3 | NF | ND | 2 | 7.8 | 2.6 | 3 |
| EGFR × gp120 | |||||||||
| Phosphorylated EGFR | 13 | 1.1 | 4 | NF | ND | 2 | 10 | 0.15 | 2 |
| Phosphorylated c-MET | NF | ND | 2 | NF | ND | 2 | NF | ND | 2 |
| c-MET × gp120 | |||||||||
| Phosphorylated EGFR | NF | ND | 4 | NF | ND | 2 | NF | ND | 2 |
| Phosphorylated c-MET | 4.1 | 0.15 | 2 | NF | ND | 2 | 7.8 | ND | 1 |
| EGFR × gp120 + c-MET × gp120 | |||||||||
| Phosphorylated EGFR | 13 | ND | 1 | NF | ND | 2 | 9.2 | 0.21 | 2 |
| Phosphorylated c-MET | 2.8 | ND | 1 | NF | ND | 2 | 12 | ND | 1 |