In Vitro: GPX4-IN-4 (Compound 24; 0-1000 nM; 0-24 h) inhibits HT1080 cell viability in a concentration- and time- dependent manner. GPX4-IN-4 (0-10 μM; 72 h) inhibits NCI-H1703 cell viability with EC50s of 0.117 μM and 4.74 μM without and with Fer-1 (HY-100579), respectively.
In Vivo: GPX4-IN-4 (Compound 24; 100 and 200 mg/kg; i.p.; once) engages kidney GPX4 and induces PD markers in mice. GPX4-IN-4 (50 mg/kg; i.p.; daily for 20 days) has no effect on WSU-DLCL2 tumor growth in mice, although partial target engagement is observed in tumor homogenate.