Network Version
Telaglenastat Data Sheet
| Product Name: | Telaglenastat |
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|---|---|---|
| CAS No.: | 1439399-58-2 | |
| Cat. No.: | HY-12248 | |
| MWt: | 571.57 | |
| Formula: | C26H24F3N7O3S | |
| Purity : | >98% | |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity[1].
IC50 & Target:IC50: 23 nM (GLS1 in kidney), 28 nM (GLS1 in brain), >1 μM (GLS2 in liver)[1]
In Vitro:Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s 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]. In Vivo:Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1]. |
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