General description
Potent oral CDK4/6 inhibitor induces reversible G1 arrest by blocking Rb phosphorylation, suppressing cancer proliferation and extending survival.
Palbociclib (PD 0332991), an oral, cell-permeable, ATP-competitive dual CDK4/6 inhibitor, arrests G1-S transition by preventing Rb phosphorylation and E2F sequestration. Its high specificity is evidenced by nanomolar IC50s (CDK4/D1: 11 nM; CDK4/D3: 9 nM; CDK6/D2: 15 nM) versus >5 µM for other CDKs (CDK1/2/5) and minimal broader kinase activity. This reversible G1 arrest reduces proliferation, induces senescence, and decreases tumor burden preclinically. Its targeted inhibition of a key cell cycle regulator offers a pivotal advantage over broad cytotoxic agents, mitigating systemic toxicities, demonstrating robust efficacy, and clinically translating to increased PFS in HR+/HER2- metastatic breast cancer with endocrine therapy. Moreover, its recent identification as a direct STING dimerization/activation inhibitor implies novel repurposing in autoinflammatory diseases and enhancing anti-tumor immunity, extending utility beyond cell cycle.
Disclaimer
Hygroscopic Store with desiccant
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (warmed) |
| storage temp. | -10 to -25°C |
