Table 4.
ML04 is a Potent, Irreversible and Selective Inhibitor of the EGFR
| Investigated Tyrosine Kinase (Cell Line) | IC50 Values in Intact Cells [nM] a | IC50 Values in a Cell-Free Kinase Assay [nM] a | |
|---|---|---|---|
| Immediately after Removal of the Inhibitor | Eight Hours after Removal of the Inhibitor | ||
| EGFR (A431) | 4-10 b | 10-50 b | 0.11 ± 0.08 b |
| EGFR (MDA-MB 468) | 1-5 | 1-5 | |
| EGFR (PC10) | 10-50 | 10-50 | |
| EGFR (NCI-H1975) | 25 | ND | |
| EGFR (DHER14) | 4 b | ND | |
| HER2 (CSH12) | 25-50 b | ND | ND |
| PDGFR (NIHPDGFR) | > 1000 b | ND | ND |
| VEGFR-2 (PAE/ KDR) | > 10,000 | ND | ND |
| c-Src | ND | 118 ± 26 | |
| IGF-1R | ND | > 15,000 | |
a
The median inhibitory concentrations (IC50) values were obtained from at least three independent experiments. Where applicable, results are presented as mean ± SD.
b
Studies investigating the inhibitory potency toward the EGFR and related tyrosine kinases were carried out using either intact cells or a cell free kinase assay. ND: not determined.