Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 μmol/L) and Cdk6 (IC50, 0.016 μmol/L), having no activity against a panel of 36 additional protein kinases.
基本介紹
- 中文名：帕博西林，帕博昔布
- 外文名：Palbociclib
- 原研企業：美國輝瑞製藥（Pfizer）
- 藥物類別：吡啶並嘧啶衍生化的CDK抑制劑
Palbociclib的生物活性:,化學信息:,臨床信息:,
Palbociclib的生物活性:
Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 μmol/L) and Cdk6 (IC50, 0.016 μmol/L), having no activity against a panel of 36 additional protein kinases.
化學信息:
外觀：黃色至灰白色晶狀固體
分子量: 447.53
分子式:C24H29N7O2
CAS號:571190-30-2
溶劑/溶解度: DMSO
晶型：2種，A和B，均為無水晶體
儲存條件: 參考CoA中推薦的條件進行儲存。
臨床信息:
| 發起人 | 狀況 | 開始日期 | 結束日期 | 階段 | 最後更改日期 |
|---|---|---|---|---|---|
Pfizer Inc | Metastatic breast cancer | 28-FEB-13 | 31-MAR-15 | Phase 3 Clinical | 15-NOV-13 |
German Breast Group | Breast tumor | 31-OCT-13 | 30-NOV-21 | Phase 3 Clinical | 12-SEP-13 |
Institut Bergonie | Gastrointestinal stromal tumor | 31-AUG-13 | 31-AUG-15 | Phase 2 Clinical | 12-SEP-13 |
Washington University in St Louis | Breast tumor | 30-JUN-13 | 31-AUG-15 | Phase 2 Clinical | 21-JUN-13 |
Pfizer Inc | Metastatic breast cancer | 30-SEP-13 | 31-JAN-17 | Phase 3 Clinical | 01-NOV-13 |
