生物活性
Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力 对Lck，VEGFR2/3，c-Kit，CDK2等有效。
Targets
| Target | Value |
| AuroraA | IC50: 13nM |
| Abl | IC50: 25nM |
| RET | IC50: 31nM |
| TrkA | IC50: 31nM |
| FGFR1 | IC50: 47nM |
| AuroraC | IC50: 61nM |
| AuroraB | IC50: 79nM |
化学数据
| 目录号 | A10715 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 474.6 |
| Formula | C26H30N6O3 |
| 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. | 827318-97-8 |
| Synonyms | PHA739358 |
| SMILES | CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=NNC4=C3CN(C4)C(=O)[C@@H](C5=CC=CC=C5)OC |
溶解度
| In vitro (25°C) | DMSO | 93 mg/mL (195.97 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% DMSO+30% polyethylene glycol+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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 21.07 mL | 105.35 mL | 210.7 mL |
| 0.5 mM | 4.21 mL | 21.07 mL | 42.14 mL |
| 1 mM | 2.11 mL | 10.54 mL | 21.07 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.21 mL |
*The above data is based on the productmolecular weight 474.6 . 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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