AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 17 nM. AG-636 has strong anticancer effects[1].
AG-636 has strong growth-inhibitory activity in cancer cell lines of hematologic versus solid tumor origin[1].
AG-636 (10-100 mg/kg ; oral gavage; twice daily; for 14 days) treatment results in robust tumor growth inhibition in the OCILY19 DLBCL tumor xenograft model[1].
[1]. Gabrielle McDonald, et al. Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase. Mol Cancer Ther. 2020 Dec;19(12):2502-2515.