生物活性
AEE788是一种口服生物可用的多受体酪氨酸激酶抑制剂，可抑制EGFR，HER2和VEGF2酪氨酸激酶的磷酸化。
Targets
| Target | Value |
| EGFR | IC50: 2nM |
| HER2/ErbB2 | IC50: 6nM |
| c-Abl | IC50: 52nM |
| FLT1 | IC50: 59nM |
| c-Fms | IC50: 60nM |
| c-Src | IC50: 61nM |
| KDR | IC50: 77nM |
| HER4/ErbB4 | IC50: 160nM |
| PDGFRβ | IC50: 320nM |
| FLT4 | IC50: 330nM |
| FLT3 | IC50: 730nM |
| RET | IC50: 740nM |
| c-Kit | IC50: 790nM |
| Tek | IC50: 2.1μM |
| C-Raf-1 | IC50: 2.8μM |
| c-Met | IC50: 2.9μM |
| CDK1/CyclinB | IC50: 8.0μM |
| IGF-1R | IC50: >10μM |
| Insulin Receptor | IC50: >10μM |
| PKCα | IC50: >10μM |
| PKA | IC50: >10μM |
化学数据
| 目录号 | A10043 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 440.6 |
| Formula | C27H32N6 |
| 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. | 497839-62-0 |
| Synonyms | AEE-788, NVP-AEE788 |
| SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4N[C@H](C)C5=CC=CC=C5 |
溶解度
| In vitro (25°C) | DMSO | 81 mg/mL (183.84 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 22.7 mL | 113.48 mL | 226.96 mL |
| 0.5 mM | 4.54 mL | 22.7 mL | 45.39 mL |
| 1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
*The above data is based on the productmolecular weight 440.6 . 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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