生物活性
PHA-793887是一种新型有效的CDK2，CDK5和CDK7抑制剂，IC50分别为8 nM，5 nM 和10 nM，作用于CDK2，5，和7比作用于CDK1，4，和9选择性高6倍以上。可在低浓度下靶向多种细胞周期蛋白依赖性激酶，并具有针对多种癌细胞的高活性。
Targets
| Target | Value |
| CDK5/p25 | IC50: 5nM |
| CDK2/CyclinA | IC50: 8nM |
| CDK2/CyclinE | IC50: 8nM |
| CDK7/CyclinH | IC50: 10nM |
| CDK1/CyclinB | IC50: 60nM |
| CDK4/CyclinD1 | IC50: 62nM |
| GSK-3β | IC50: 79nM |
| CDK9/CyclinT1 | IC50: 138nM |
化学数据
| 目录号 | A10716 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 361.5 |
| Formula | C19H31N5O2 |
| 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. | 718630-59-2 |
| Synonyms | PHA793887 |
| SMILES | CC(C)CC(=O)NC1=NNC2=C1CN(C2(C)C)C(=O)C3CCN(CC3)C |
溶解度
| In vitro (25°C) | DMSO | 61 mg/mL (168.75 mM) |
| Water | Insoluble |
| Ethanol | 61 mg/mL (168.75 mM) |
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 14 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 | 27.66 mL | 138.31 mL | 276.63 mL |
| 0.5 mM | 5.53 mL | 27.66 mL | 55.33 mL |
| 1 mM | 2.77 mL | 13.83 mL | 27.66 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
*The above data is based on the productmolecular weight 361.5. 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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