Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0005063 |
| PMID | 23936329 |
| Assay Used | Kinase assays |
| Experimently Validated | Yes |
| EGFR (IC50) | 120 ± 12 nM |
| HER2 (IC50) | 96 ± 4 nM |
| HER4 (IC50) | - |
| Mutant L858R (IC50) | - |
| Mutant T790M (IC50) | - |
| Double Mutant (IC50) | - |
| 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 | - |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A549 | carcinomic human alveolar basal epithelial cell | 1640 ± 27 nM | - | - | - | - | - | - | - | - | |||
| 2 | MCF-7 | breast cancer, with Her2/neu protein overexpression | 490 ± 18 nM | - | - | - | - | - | - | - | - | |||
| 3 | A431 | overexpression of EGFR. | 670 ± 2 nM | - | - | - | - | - | - | - | - | |||
| 4 | MDA-MB-453 | Breast tigcancer HER-2++, PTEN deficiency | 920 ± 19nM | - | - | - | - | - | - | - | - | |||
| 5 | H1781 | NSCLC HER-2 G776ins V_G/C | 770 ± 34nM | - | - | - | - | - | - | - | - | |||
| 6 | H1975 | NSCLC EGFR L858R/T790M | 3300 ± 233nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |