Products for Research Use Only

CB-839

CAT: 0013-GTR19163219-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19163219-01Size:1 g
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Description
CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM) ; demonstrates antiproliferative activity in triple-negative breast cancer (TNBC) cell line HCC-1806 and MDA-MB-231 with IC50 of 20-55 nM, decreases glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates; exhibits vivo efficacy in breast cancer xenograft models, both as a single agent and in combination with paclitaxel. Kidney Cancer Phase 2 Clinical (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.Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells. (In Vivo) :Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC.
CAS Number
1439399-58-2
Product Name Alternative
CB839 | CB 839 | Telaglenastat
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 30 mg/mL
Smiles
O=C (NC1=CC=C (CCCCC2=NN=C (NC (CC3=NC=CC=C3) =O) S2) N=N1) CC4=CC (OC (F) (F) F) =CC=C4
Molecular Formula
C26H24F3N7O3S
Molecular Weight
571.5741
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Pyridineacetamide, N-[5-[4-[6-[[2-[3- (trifluoromethoxy) phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-