Cantrixil (TRX-E-002-1) is a potent inducer of CD44+/MyD88+ ovarian cancer stem cell (OCSC) death with IC50 of 47 nM.
Cantrixil (TRX-E-002-1) induces cell death by the activation and enhanced expression of c-Jun, leading to the induction of caspases.
Cantrixil (TRX-E-002-1) is effective against both clones and was able to decrease the percentage of viable cells with IC50 of 68 nmol/L and 27 nmol/L for chemosensitive ovarian cancer cells (OCC1 and OCC2) respectively.
TRX-E-002-1 is effective in inducing death in 3D ovarian cancer spheroids, prevents OCSC recurrence in vitro.
TRX-E-002-1-induced cell death is associated with phosphorylation and increased expression levels of c-Jun, activates the caspase cascade and requires c-Jun activation.
TRX-E-002-1 (100 mg/kg daily, i.p.) demonstrates significant antitumor activity against both primary and recurrent disease in a mouse xenograft model of ovarian cancer.
The combination of TRX-E-002-1 and cisplatin is able to decrease tumor kinetics better than monotherapy.