Product Information

• Product Code：A047060

• English Name：Apalutamide Impurity 60

• English Alias：1-(1-aminocyclobutanecarboxamido)cyclobutanecarboxylic acid

• CAS No.：1513077-71-8

• Molecular Formula：C??H??N?O?

• Molecular Weight：212.25

Advantages

• High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Apalutamide impurity analysis and quality control.

• Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.2% in acetonitrile-water solution within 6 months.

Applications

• Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 60 in Apalutamide API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).

• Process Optimization Research：Monitors Impurity 60 formation during Apalutamide synthesis, reducing generation by >50% by adjusting condensation 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 (0.005 ng/mL).

Background Description

Research Status

• Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 4 minutes, with LOD of 0.003 ng/mL for trace impurity analysis.

• Formation Mechanism：Formed by reaction of 1-aminocyclobutanecarboxylic acid with cyclobutanecarbonyl chloride under alkaline conditions (e.g., triethylamine catalysis); optimizing catalyst dosage and solvent polarity (e.g., DMF-water system) inhibits side reactions.

• Safety Evaluation：In vitro cytotoxicity shows IC?? of 178.6 μM against PC-3 cells (Apalutamide IC??=9.3 μM), with lower toxicity than the main drug but requiring strict content control. Long-term stability testing is ongoing to monitor degradation under different humidity, light, and temperature conditions.