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Biological Activity
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
Targets
| Target | Value |
|---|---|
| EGFR(L858R/T790M) | IC50: <1nM |
| EGFR(L861Q) | IC50: 1nM |
| EGFR(L858R) | IC50: 6nM |
| ErbB4 | IC50: 7nM |
| EGFR(wildtype) | IC50: 25nM |
| ACK1 | IC50: 27nM |
| BLK | IC50: 27nM |
| BRK | IC50: 45nM |
| MNK2 | IC50: 62nM |
| IGF1-R | IC50: 78nM |
| ALK | IC50: 97nM |
| TEC | IC50: 118nM |
| FES | IC50: 127nM |
| InsR | IC50: 127nM |
| FLT3 | IC50: 129nM |
| BTK | IC50: 132nM |
| FAK | IC50: 136nM |
| MLK1 | IC50: 141nM |
| FLT4 | IC50: 142nM |
| PYK2 | IC50: 284nM |
| IRR | IC50: 423nM |
| Txk | IC50: 426nM |
| BMX | IC50: 505nM |
| ITK | IC50: 925nM |
| JAK3 | IC50: 1358nM |
| In vitro (25°C) | DMSO | 90 mg/mL (185.34 mM) | |
| Water | Insoluble | ||
| Ethanol | Warmed: 21 mg/mL (43.24 mM) | ||
| In vivo | 1% Tween 80 | 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 | 20.59 mL | 102.97 mL | 205.94 mL |
| 0.5 mM | 4.12 mL | 20.59 mL | 41.19 mL |
| 1 mM | 2.06 mL | 10.3 mL | 20.59 mL |
| 5 mM | 0.41 mL | 2.06 mL | 4.12 mL |
*The above data is based on the productmolecular weight 485.58. 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 | A15516 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1421373-98-9 |
| Formula | C27H31N7O2 |
| M. Wt | 485.58 |
| Purity | >98% |
| Synonyms | AZ-5104, AZ 5104 |
| SMILES | CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=CC(=N2)C3=CNC4=CC=CC=C43)OC |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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