Palbociclib 99% Purity CDK4/6 Inhibitor CAS 571190-30-2 Anticancer Small Molecule Compound Research Grade

Product Overview

Palbociclib is a potent, orally bioavailable cyclin-dependent kinase 4/6 (CDK4/6) inhibitor used in the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Marketed under the brand name Ibrance, palbociclib was the first CDK4/6 inhibitor approved by the FDA in February 2015, representing a major breakthrough in breast cancer therapy. By selectively inhibiting CDK4/6 kinases, palbociclib blocks cell cycle progression from G1 to S phase, thereby inhibiting tumor cell proliferation.

Chemically, palbociclib is 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)pyridin-2-yl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one with the molecular formula C₂₄H₂₉N₇O₂ and a molecular weight of 447.53 g/mol. It is a yellow to orange-yellow crystalline powder with solubility in DMSO and DMF. The compound exhibits high selectivity for CDK4 and CDK6 over other CDKs and favorable pharmacokinetic properties including excellent oral bioavailability.

Mechanism of Action

Palbociclib exerts its anticancer effects through cell cycle regulation:

• CDK4/6 Inhibition: Potently and selectively inhibits cyclin-dependent kinases 4 and 6, key regulators of the G1 to S phase transition

• Cell Cycle Arrest: Blocks retinoblastoma protein (Rb) phosphorylation, preventing E2F transcription factor activation and S phase entry

• Antiproliferative Effect: Inhibits tumor cell proliferation by inducing G1 phase cell cycle arrest

• Synergy with Hormonal Therapy: Enhances the efficacy of endocrine therapies such as letrozole and fulvestrant in HR+ breast cancer

• Tumor Selectivity: Preferentially affects cells with dysregulated CDK4/6-Rb pathway, commonly seen in HR+ breast cancer

Research Applications & Market Significance

Palbociclib has transformed the treatment landscape for advanced HR+/HER2- breast cancer:

• First-line Breast Cancer: Standard of care in combination with aromatase inhibitors for HR+/HER2- metastatic breast cancer in postmenopausal women

• Second-line Therapy: Used with fulvestrant in patients with disease progression following endocrine therapy

• Male Breast Cancer: Approved for male patients with HR+/HER2- metastatic breast cancer

• Adjuvant Therapy: Clinical trials investigating potential use in early-stage breast cancer

• Other Tumor Types: Research in progress for liposarcoma, non-small cell lung cancer, and other CDK4/6-driven malignancies

• Combination Strategies: Extensive research combining with immunotherapy, PI3K inhibitors, and other targeted agents

The global CDK4/6 inhibitor market is expected to exceed $15 billion by 2028, driven by expanding indications and growing adoption in breast cancer and other tumor types. Palbociclib continues to lead the CDK4/6 inhibitor class with the most extensive real-world evidence and longest clinical track record.

Quality Specifications

Our palbociclib is manufactured under strict quality control conditions:

• Purity: ≥99.0% determined by HPLC

• Identity confirmed by NMR, mass spectrometry, and elemental analysis

• Water content: ≤0.5%

• Residual solvents: Meet ICH Q3C guidelines

• Heavy metals: ≤10 ppm

• Related substances: Each impurity ≤0.1%, total impurities ≤0.5%

• Enantiomeric purity: ≥99.5% ee

• Each batch accompanied by comprehensive Certificate of Analysis (COA)

• Stable for 24 months when stored at 2-8°C in sealed containers protected from light

Packaging & Shipping

We offer flexible packaging options to meet diverse customer needs:

• Research quantities: 100mg, 250mg, 500mg, 1g amber glass vials

• Bulk quantities: 5g, 10g, 50g, 100g amber glass bottles

• Industrial quantities: 1kg, 5kg, 25kg fiber drums with PE liners

• Custom packaging available upon request

• Shipped at ambient temperature for routine orders

• Cold chain shipping available upon request

• International shipping with proper documentation including MSDS and COA