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].
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].
Kinase Assay
Cell Assay
Animal Administration
References
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