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Forced degradation studies of silodosin under hydrolytic (acidic, alkaline and neutral), oxidation, photolysis and thermal stress conditions.Isolation of major degradation products (DP 1 and DP 2).Identification of 5 hitherto unknown DPs by LC–ESI–MS/MS experiments.In vitro anticancer activity studies on silodosin, DP 1 and DP 2 using PC 3 cells by MTT assay.Silodosin (SLD) a novel α1-adrenoceptor antagonist was subjected to forced degradation involving hydrolysis (acidic, alkaline and neutral), oxidative, photolysis and thermal stress, as per ICH specified conditions. The drug underwent significant degradation under hydrolytic (acidic, alkaline and neutral) and oxidative stress conditions whereas, it was found to be stable under other stress conditions. A rapid, precise, accurate and robust chromatographic method for the separation of the drug and its degradation products (DPs) was developed on a Fortis C18 analytical column (150 × 4.6 mm, 5 μm) using 0.1% formic acid and acetonitrile as a mobile phase in gradient elution mode at a flow rate of 1.0 mL/ min. A total of 5 (DP 1 to DP 5) hitherto unknown DPs were identified by LC-ESI-TOF-MS/MS experiments and accurate mass measurements. The most probable mechanisms for the formation of DPs have been proposed based on a comparison of the fragmentation of the [M+H]+ ions of silodosin and its DPs. The major DPs (DP 1 and DP 2) were isolated and evaluated for anticancer activity using PC3 (human prostate cancer) cell lines by MTT assay. The results revealed that silodosin, DP 1 and DP 2 have potential anticancer activity with IC50 values (μM) 72.74 (±4.51), 25.21 (±2.36), and, 114.07 (±11.90) respectively.