Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0004913 |
| PMID | 21789172 |
| Assay Used | Enzymatic and Cell proloferation assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 0.56 ± 0.2 nM |
| HER2 (IC50) | 3.06 ± 1.5 nM |
| HER4 (IC50) | 0.86 ± 0.3 nM |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | 12 ± 2 nM |
| Average ERBB2 and ERBB1 (IC50) | - |
| Inhibition EGFR (%) | - |
| Inhibitory Concentration | - |
| Inhibition HER2 (%) | - |
| Inhibitory Concentration | - |
| Ki (EGFR) | - |
| Ki (HER2) | - |
| Ki (HER4) | - |
| Kd (EGFR) | - |
| Kd (L858R) | - |
| Kd (T790M) | - |
| Kd (L858R/T790M) | - |
| Kd (Other mutation) | - |
| Note | THe paper describes the AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | BT474 | - | 970 nM | - | - | - | - | - | - | - | - | |||
| 2 | CaLu3 | - | 230 nM | - | - | - | - | - | - | - | - | |||
| 3 | MCF-7 | - | 16000 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | Yes |
| Wild type | Yes |
| Mutant | L858R/T790M |
| Inhibitor Binding | |
| EGFR | CYS797 |
| HER2 | CYS805 |
| HER4 | - |