Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC 50 s of 49 nM and 26 nM, respectively[1]. Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1]. Cell Proliferation Assay[1]Cell Line: HCC1806, MDA-MB-231 cells Concentration: 0.1, 1, 10, 100, 1000 nM Incubation Time: 72 hours Result: Has a potent effect on the proliferation of the two TNBC cell lines (IC 50 of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells). Apoptosis Analysis[1]Cell Line: MDA-MB-231, HCC1806 cells Concentration: 1 μM Incubation Time: 72 hours Result: Caspase 3/7 activation.

Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1]. Animal Model: Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)[1]Dosage: 200 mg/kg Administration: Oral administration; twice daily for 28 days Result: Suppressed tumor growth by 61% relative to vehicle control at the end of study.