生物活性
AZD-9291 (Osimertinib)是第三代EGFR抑制剂，在临床前研究中显示出希望，并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。
靶点信息
| L858R/T790M EGFR (LoVo cells) | Exon 19 deletion EGFR (LoVo cells) | WT EGFR (LoVo cells) | | |
| 11.44 nM | 12.92 nM | 493.8 nM | | |
化学数据
| 目录号 | A13681 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 499.61 |
| Formula | C28H33N7O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1421373-65-0 |
| Synonyms | AZD 9291, AZD9291 |
| SMILES | CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC |
溶解度
| In vitro (25°C) | DMSO | Warmed: 90 mg/mL (180.14 mM) |
| Water | Insoluble |
| Ethanol | Warmed: 39 mg/mL (78.05 mM) |
| In vivo | 5%DMSO+40%PEG300+5%Tween80+50%ddH2O | 7.1 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.02 mL | 100.08 mL | 200.16 mL |
| 0.5 mM | 4 mL | 20.02 mL | 40.03 mL |
| 1 mM | 2 mL | 10.01 mL | 20.02 mL |
| 5 mM | 0.4 mL | 2 mL | 4 mL |
*The above data is based on the productmolecular weight 499.61. 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.
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