Epidermal Growth Factor Receptor Inhibitor Database
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| Experimental Information | |
| Enzymatic Activity | |
| Molecule Id | EGIN0000002 |
| PMID | 20143778 |
| Assay Used | Enzymatic and Cellular assay |
| Experimently Validated | Yes |
| EGFR (IC50) | 48 nM |
| HER2 (IC50) | 134.5 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 | The paper describes the 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer |
| Extra | - |
| Cellular Activity | ||||||||||||||
| S.No. | Cell Line | Desp. | IC50 | IC80 | ED50 | GI50 | GI90 | EC50 | Kd | Inhibition (%) | Inhibitory Conc. | |||
| 1 | BxPc3 | - | 7600 nM | - | - | - | - | - | - | - | - | |||
| 2 | Capan1 | - | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 3 | H358 | - | 6000 nM | - | - | - | - | - | - | - | - | |||
| 4 | H460 | - | 8200 nM | - | - | - | - | - | - | - | - | |||
| 5 | HCC827 | - | 7500 nM | - | - | - | - | - | - | - | - | |||
| 6 | Hep3B2 | - | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 7 | HepG2 | - | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 8 | MCF-7 | - | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 9 | MDA-MB-231 | - | > 20000 nM | - | - | - | - | - | - | - | - | |||
| 10 | SKBR3 | - | 1560 nM | - | - | - | - | - | - | - | - | |||
| 11 | Sk-Hep-1 | - | 10370 nM | - | - | - | - | - | - | - | - | |||
| Activity against Receptor | |
| EGFR | Yes |
| HER2 | Yes |
| HER4 | - |
| Wild type | Yes |
| Mutant | - |
| Inhibitor Binding | |
| EGFR | - |
| HER2 | - |
| HER4 | - |