生物活性
ZM 447439是Aurora A和Aurora B的选择性和ATP竞争性抑制剂，IC50分别为110 nM和130 nM。它对Aurora A/B的选择性是MEK1，Src，Lck的8倍以上，对CDK1/2/4，Plk1，Chk1等的影响很小。
Targets
| Target | Value |
| AuroraA | IC50: 110nM |
| AuroraB | IC50: 130nM |
| LCK | IC50: 880nM |
| Src | IC50: 1.03μM |
| MEK1 | IC50: 1.79μM |
| CDK1 | IC50: >10μM |
| CDK2 | IC50: >10μM |
| CDK4 | IC50: >10μM |
| PLK1 | IC50: >10μM |
| Chk1 | IC50: >10μM |
| IKK1 | IC50: >10μM |
| IKK2 | IC50: >10μM |
| cFLT2 | IC50: >10μM |
| KDR2 | IC50: >10μM |
| ZAP70 | IC50: >10μM |
| FAK | IC50: >10μM |
化学数据
| 目录号 | A11009 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 513.6 |
| Formula | C29H31N5O4 |
| 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. | 331771-20-1 |
| Synonyms | ZM447439 |
| SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)NC(=O)C4=CC=CC=C4)OCCCN5CCOCC5 |
溶解度
| In vitro (25°C) | DMSO | 90 mg/mL (175.23 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 | 19.47 mL | 97.35 mL | 194.7 mL |
| 0.5 mM | 3.89 mL | 19.47 mL | 38.94 mL |
| 1 mM | 1.95 mL | 9.74 mL | 19.47 mL |
| 5 mM | 0.39 mL | 1.95 mL | 3.89 mL |
*The above data is based on the productmolecular weight 513.6 . 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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