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- Khattab M, .et al. Conformational Plasticity in Tyrosine Kinase Inhibitor-Kinase Interactions Revealed with Fluorescence Spectroscopy and Theoretical Calculations, J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. A pH-induced conformational switch in a tyrosine kinase inhibitor identified by electronic spectroscopy and quantum chemical calculations, Sci Rep, 2017, 7: 16271 PMID: 29176733
Biological Activity
AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
Targets
| EGFR (Cell-free assay) | HER2 (Cell-free assay) | PDGFR (Cell-free assay) | ||
| 3 nM | >100 μM | >100 μM |
| In vitro (25°C) | DMSO | 25 mg/mL (79.17 mM) | |
| Water | Insoluble | ||
| Ethanol | 13 mg/mL (41.17 mM) | ||
| In vivo | 15% Captisol | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 31.67 mL | 158.33 mL | 316.66 mL |
| 0.5 mM | 6.33 mL | 31.67 mL | 63.33 mL |
| 1 mM | 3.17 mL | 15.83 mL | 31.67 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.33 mL |
*The above data is based on the productmolecular weight 315.8 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11022 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 153436-53-4 |
| Formula | C16H14ClN3O2 |
| M. Wt | 315.8 |
| Purity | >98% |
| Synonyms | AG1478, AG 1478 |
| SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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