Palbociclib Impurity;2781952-66-5
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E-mail: anna@molcoo.com
Product Code：P005103
English Name：Palbociclib Impurity 103
English Alias：6-acetyl-2-((5-(4-butylpiperazin-1-yl)pyridin-2-yl)amino)-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one
CAS No.：2781952-66-5
Molecular Formula：C₂₈H₃₇N₇O₂
Molecular Weight：503.64
High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Palbociclib impurity analysis and quality control.
Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.3% in methanol-acetonitrile mixture within 6 months.
Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 103 in Palbociclib API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).
Process Optimization Research：Monitors impurity formation during Palbociclib synthesis, reducing generation by >30% by adjusting acetylation temperature (e.g., 60-70℃) and reaction time.
Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.01 ng/mL).
Palbociclib, an oral cyclin-dependent kinase (CDK4/6) inhibitor, is used for treating hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced breast cancer by inhibiting cell cycle progression to suppress tumor cell proliferation. Impurity 103, a process-related impurity in its synthesis, may originate from acetylation side reactions of pyridopyrimidine rings or incomplete alkylation of piperazine groups. Its acetyl, cyclopentyl, and piperazine chain may affect drug target binding, metabolic stability, and safety. Strict impurity control for anticancer drugs is critical, making research on this impurity essential for ensuring drug quality.
Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 10 minutes, with LOD of 0.005 ng/mL for trace impurity analysis.
Formation Mechanism：Formed by condensation of 2-amino-5-(4-butylpiperazin-1-yl)pyridine with 6-acetyl-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one using condensing agents (e.g., DCC); optimizing reaction solvent and catalyst dosage inhibits side reactions.
Safety Evaluation：In vitro cytotoxicity shows IC₅₀ of 189.3 μM against MCF-7 breast cancer cells (Palbociclib IC₅₀=9.8 μM), with lower toxicity than the main drug but requiring strict content control. Long-term stability testing is ongoing to monitor degradation under high temperature and humidity conditions and its potential impact on the main drug.
We can also customize related analogues and modified peptides including HPLC, MS, 1H-NMR, MS, HPLC, IR, UV, COA, MSDS.
This product is intended for laboratory use only!
WhatsAPP: +86 17386083646
E-mail: anna@molcoo.com
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