生物活性
A-674563是一种B/Akt抑制剂，IC50为14 nM，并且还显示出对PKA和CDK2的抑制活性，IC50分别为16和46 nM。
Targets
| Target | Value |
| Akt1 | ki: 11nM |
| PKA | ki: 16nM |
| CDK2 | ki: 46nM |
| GSK-3β | ki: 110nM |
| ERK2 | ki: 260nM |
| PKCδ | ki: 360nM |
| RSK2 | ki: 580nM |
| MAPK-AP2 | ki: 1.1μM |
| PKCγ | ki: 1.2μM |
| FLT1 | ki: >2.2μM |
| Chk1 | ki: 2.6μM |
| KDR | ki: >3.7μM |
| CK2 | ki: 5.4μM |
| c-Kit | ki: >5.8μM |
| Src | ki: 13μM |
| PDK-1 | ki: >20μM |
化学数据
| 目录号 | A11034 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 358.4 |
| Formula | C22H22N4O |
| 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. | 552325-73-2 |
| Synonyms | A674563 |
| SMILES | CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OC[C@H](CC4=CC=CC=C4)N |
溶解度
| In vitro (25°C) | DMSO | 71 mg/mL (198.08 mM) |
| Water | 71 mg/mL (198.08 mM) |
| Ethanol | 18 mg/mL (50.21 mM) |
| In vivo | Saline | 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 | 27.9 mL | 139.51 mL | 279.02 mL |
| 0.5 mM | 5.58 mL | 27.9 mL | 55.8 mL |
| 1 mM | 2.79 mL | 13.95 mL | 27.9 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.58 mL |
*The above data is based on the productmolecular weight 358.4 . 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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