Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0003531 |
| PMID | 7990108 |
| Assay Used | Kinase assay and HaCaT keratinocyte proliferation assay |
| Experimently Validated | Yes |
| EGFR (IC50) | - |
| HER2 (IC50) | - |
| 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 | The paper describes the novel antiproliferative agents aerived from Lavendustin A |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | A431 | - | 14000 nM | - | - | - | - | - | - | - | - | |||
| 2 | HeLa | - | 18000 ±2800 nM | - | - | - | - | - | - | - | - | |||
| 3 | K562 | - | 14100 ±4100 nM | - | - | - | - | - | - | - | - | |||
| 4 | KB | - | 5600 ±1600 nM | - | - | - | - | - | - | - | - | |||
| 5 | L1210 | - | 14700 ±11000 nM | - | - | - | - | - | - | - | - | |||
| 6 | LOVO | - | 6000 ± 800 nM | - | - | - | - | - | - | - | - | |||
| 7 | MCF-7 | - | 15300 ± 12200 nM | - | - | - | - | - | - | - | - | |||
| 8 | MDA-MB-231 | - | 20500 ±700 nM | - | - | - | - | - | - | - | - | |||
| 9 | MDA-MB-468 | - | 6900 ±900 nM | - | - | - | - | - | - | - | - | |||
| 10 | P388 | - | 9500 ± 3500 nM | - | - | - | - | - | - | - | - | |||
| 11 | SKBR3 | - | 5000 ±1400 nM | - | - | - | - | - | - | - | - | |||
| 12 | u937 | - | 5200 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | - |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |