tcsc3393 Telaglenastat

Telaglenastat (CB-839) is a potent and selective inhibitor of glutaminase with an IC₅₀ of less than 50 nM.

IC50 & Target: IC50: 23 nM (glutaminase in kindey), 28 nM (glutaminase in brain)^[1]

In Vitro: Telaglenastat has increased potency and distinct kinetic behavior, exhibiting a slow-on/slow-off mechanism. Telaglenastat has a potent effect on the proliferation of HCC1806 and MDA-MB-231 cell lines (IC₅₀ of 20-55 nM associated with cell loss at >100 nM). TNBC cell lines are sensitive to glutaminase inhibition withTelaglenastat^[1].

In Vivo: Telaglenastat (200 mg/kg, p.o.) has antitumor activity in xenograft models of TNBC and basal-like breast cancer, and inhibits tumor glutaminase activity and changes metabolite levels^[1].