| Experimental Information |
| |
| Enzymatic Activity |
| Molecule Id | EGIN0000005 |
| PMID | 12384534 |
| Assay Used | Substrate inhibition assay with EGFR prepared from the human vulval squamous carcinoma cell line A431, MTT assay was used to measure cell growth |
| Experimently Validated | Yes |
| EGFR (IC50) | 33 nM |
| HER2 (IC50) | 3700 ± 10000 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 | ZD1839 is a potent EGFR-TKI in vitro. It is a competitive inhibitor of ATP and therefore binds at the ATP site on EGFR, it demonstrates remarkable selectivity for EGFR compared with other RTKs that share sequence homology in the ATP binding domain.The paper describes the ZD1839 (Iressa)as an Orally Active Inhibitor of Epidermal Growth Factor Signaling with Potential for Cancer Therapy |
| Extra | 0.027 µM [ EGFR (baculovirus lysate) ] |
| |
