生物活性
GSK690693是一种新型的ATP竞争性低纳摩尔泛Akt激酶抑制剂(IC50值分别为Akt1、2和3的2、13和9 nM)。
Targets
| Target | Value |
| Akt1 | IC50: 2nM |
| PKCη | IC50: 2nM |
| PKCθ | IC50: 2nM |
| PrkX | IC50: 5nM |
| Akt3 | IC50: 9nM |
| Akt2 | IC50: 13nM |
| PKCδ | IC50: 14nM |
| PKCβ | IC50: 19nM |
| PKCε | IC50: 21nM |
| PKA | IC50: 24nM |
| PKG1β | IC50: 33nM |
化学数据
| 目录号 | A11030 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 425.5 |
| Formula | C21H27N7O3 |
| 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. | 937174-76-0 |
| Synonyms | GSK-690693 |
| SMILES | CCN1C2=C(C(=NC=C2OC[C@H]3CCCNC3)C#CC(C)(C)O)N=C1C4=NON=C4N |
溶解度
| In vitro (25°C) | DMSO | 36 mg/mL (84.61 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+40%PEG300+5% tween80+50% H2O | 2 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 | 23.5 mL | 117.51 mL | 235.02 mL |
| 0.5 mM | 4.7 mL | 23.5 mL | 47 mL |
| 1 mM | 2.35 mL | 11.75 mL | 23.5 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
*The above data is based on the productmolecular weight 425.5 . 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.