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PHA-848125 (Milciclib)是一种有效的，ATP竞争性CDK抑制剂，作用于CDK2，IC50为45 nM，作用于CDK2比作用于CDK1，2，4，5和7选择性高3倍以上。
Targets
| Target | Value |
|---|---|
| CDK2/CyclinA | IC50: 45nM |
| TrkA | IC50: 53nM |
| CDK7/CyclinH | IC50: 150nM |
| CDK4/CyclinD1 | IC50: 160nM |
| CDK5/p35 | IC50: 265nM |
| CDK2/CyclinE | IC50: 363nM |
| CDK1/CyclinB | IC50: 398nM |
| In vitro (25°C) | DMSO | 91 mg/mL (197.58 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.71 mL | 108.55 mL | 217.11 mL |
| 0.5 mM | 4.34 mL | 21.71 mL | 43.42 mL |
| 1 mM | 2.17 mL | 10.86 mL | 21.71 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
*The above data is based on the productmolecular weight 460.6 . 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.
| 目录号 | A11047 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 460.6 |
| Formula | C25H32N8O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 802539-81-7 |
| Synonyms | Milciclib, PHA848125 |
| SMILES | CC1(CC2=CN=C(N=C2C3=C1C(=NN3C)C(=O)NC)NC4=CC=C(C=C4)N5CCN(CC5)C)C |
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