生物活性
PD 0332991 HCl (Palbociclib)是一种高度选择性的CDK4/6抑制剂,它对CDK1/2/5,EGFR,FGFR,PDGFR,InsR等没有抑制活性,具有潜在的抗肿瘤活性。
Targets
| Target | Value |
| CDK4/CyclinD3 | IC50: 9nM |
| CDK4/CyclinD1 | IC50: 11nM |
| CDK6/CyclinD2 | IC50: 15nM |
| CDK2/CyclinE2 | IC50: >10μM |
| CDK2/CyclinA | IC50: >10μM |
| CDK1/CyclinB | IC50: >10μM |
| CDK5/p25 | IC50: >10μM |
| EGFR | IC50: >10μM |
| FGFR | IC50: >10μM |
| PDGFR | IC50: >10μM |
| Insulin Receptor | IC50: >10μM |
| VEGFR | IC50: >10μM |
| AMPK | IC50: >10μM |
| Chk1 | IC50: >10μM |
| CK1 | IC50: >10μM |
| CK2 | IC50: >10μM |
| c-Src | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| MAPK2/ERK2 | IC50: >10μM |
| MAPKAPK2 | IC50: >10μM |
| PKB | IC50: >10μM |
| PKC | IC50: >10μM |
| PHK | IC50: >10μM |
| SAPK2a | IC50: >10μM |
| SAPK3 | IC50: >10μM |
| SAPK4 | IC50: >10μM |
化学数据
| 目录号 | A10701 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 447.5 |
| Formula | C24H29N7O2.HCl |
| 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. | 827022-32-2 |
| SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl |
溶解度
| In vitro (25°C) | DMSO | Warmed: 3 mg/mL (6.19 mM) |
| Water | 30 mg/mL (61.98 mM) |
| Ethanol | Insoluble |
| In vivo | Saline | 5 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 | 22.35 mL | 111.73 mL | 223.46 mL |
| 0.5 mM | 4.47 mL | 22.35 mL | 44.69 mL |
| 1 mM | 2.23 mL | 11.17 mL | 22.35 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.47 mL |
*The above data is based on the productmolecular weight 447.5 . 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.