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<i>Tephorosia purpurea</i> subsp. <i>apollinea</i> was extracted with methanol and n-hexane to obtain sub-fractions. The chemical compounds identified with GC-MS and HPLC in <i>T. purpurea</i> subsp. <i>apollinea</i> extracts showed antioxidant and anticancer properties. The antioxidant and anticancer activities were investigated using DDPH and ABTS assays, and MTT assay, respectively. Stigmasta-5,24(28)-dien-3-ol, (3 β,24Z)-, 9,12,15-octadecatrienoic acid methyl ester, phytol, chlorogenic acid, and quercetin were the major chemical compounds detected in <i>T. purpurea</i> subsp. <i>apollinea.</i> These compounds possessed antioxidant and anticancer properties. The methanol extract showed antioxidant properties with DDPH and ABTS radical scavenging of 84% and 94%, respectively, relative to ascorbic acid and trolox. The anticancer effects of <i>T. purpurea</i> subsp. <i>apollinea</i> against the cancer cell lines MCF7 (IC₅₀ = 102.8 ± 0.6 μg/mL), MG63 (IC₅₀ = 118.3 ± 2.5 μg/mL), T47D (IC₅₀ = 114.7 ± 1.0 μg/mL), HeLa (IC₅₀ = 196.3 ± 2.3 μg/mL), and PC3 (IC₅₀ = 117.7 ± 1.1 μg/mL) were greater than its anticancer effects against U379 (IC₅₀ = 248.4 ± 7.5 μg/mL). However, it had no adverse effects on the normal cells (WI38) (IC₅₀ = 242.9 ± 1.8 μg/mL). Therefore, the major active constituents presented in <i>T. purpurea</i> subsp. <i>apollinea</i> can be isolated and studied for their potential antioxidant and anticancer effects against breast, cervical, and prostate cancers and osteosarcoma.