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About This Item
Empirical Formula (Hill Notation):
C24H29N7O2 · xHCl
CAS Number:
Molecular Weight:
447.53 (free base basis)
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
Quality Segment
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
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.
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
signalword
Warning
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Chronic 2 - Muta. 2 - Repr. 2 - Skin Sens. 1B - STOT RE 2 Oral
target_organs
Bone marrow,male reproductive organs
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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