GIC-20, a dual inducer of apoptosis and ferroptosis, exhibits antitumor efficacy against fibrosarcoma [1].

GIC-20, when used at 1 μM for 48 hours, inhibits the proliferation and migration of HT1080 fibrosarcoma cells, exhibiting cytotoxicity with an IC50 of 1.6 μM [1]. At concentrations of 0.5-4 μM for 24 hours, GIC-20 induces ferroptosis by increasing intracellular lipid peroxides and ROS accumulation or degrading GPX4 [1]. Additionally, GIC-20 at 0-1 μM for 24 hours reduces cell viability in resistant MIA-PaCa-2-AMG510R cells, increasing their sensitivity to AMG510 [1]. In HT1080 cells, Western Blot analysis shows that GIC-20 at 0-4 μM for 24 hours inhibits GPX4 and Bcl-2 expression while promoting Bax expression. Apoptosis analysis further reveals that GIC-20 at 0-4 μM for 24 hours induces apoptosis in a dose-dependent manner.

GIC-20, administered at 20-40 mg/kg via intraperitoneal injection daily for 19 days, demonstrates antitumor activity in HT1080 xenograft BALB/c mice without significant toxicity to major organs [1]. In this animal model, a dosage of 40 mg/kg resulted in a tumor growth inhibition (TGI) of 63%, while preserving organ morphology with no apparent inflammatory response, edema, or necrosis.