生物活性
Sotrastaurin是一种有效的 pan-PKC 抑制剂，作用于PKCθ，PKCβ，PKCα，PKCη，PKCδ 和PKCε，Ki 分别为 0.22 nM，0.64 nM，0.95 nM，1.8 nM，2.1 nM 和 3.2 nM。用于预防移植排斥反应和治疗牛皮癣。
Targets
| Target | Value |
| PKCθ | ki: 0.22nM |
| PKCβ1 | ki: 0.64nM |
| PKCα | ki: 0.95nM |
| PKCη | ki: 1.8nM |
| PKCδ | ki: 2.1nM |
| PKCε | ki: 3.2nM |
化学数据
| 目录号 | A11554 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 438.5 |
| Formula | C25H22N6O2 |
| 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. | 425637-18-9 |
| Synonyms | AEB 071, AEB-071 |
| SMILES | CN1CCN(CC1)C2=NC3=CC=CC=C3C(=N2)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65 |
溶解度
| In vitro (25°C) | DMSO | 79 mg/mL (180.17 mM) |
| Water | Insoluble |
| Ethanol | 2 mg/mL (4.56 mM) |
| In vivo | 2% DMSO+30% PEG 300+ddH2O | 9 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 | 22.81 mL | 114.03 mL | 228.05 mL |
| 0.5 mM | 4.56 mL | 22.81 mL | 45.61 mL |
| 1 mM | 2.28 mL | 11.4 mL | 22.81 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
*The above data is based on the productmolecular weight 438.5 . 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.
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