CB-839(Telaglenastat)

Cas No.:	1439399-58-2
Chemical Name:	Telaglenastat
Synonyms:	CB-839;CB839;Telaglenastat;U6CL98GLP4;2-(pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide;N-[6-[4-[5-[(2-pyridin-2-ylacetyl)amino]-1,3,4-thiadiazol-2-yl]butyl]pyridazin-3-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide;2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-;2-Pyridineacetamide, N-(5-(4-(6-((2-(3-(trifluoromethoxy)phenyl)acet;2-(Pyridin-2-Yl)-N-(5-{4-[6-({[3-(Trifluoromethoxy)phenyl]acetyl}amino)pyridazin-3-Yl]butyl}-1,3,4-Thiadiazol-2-Yl)acetamide;N-[6-[4-[5-[(2-pyridin-2-ylacetyl)amino]-1,3,4-thiadiazol-2-yl]butyl
SMILES:	S1C(N([H])C(C([H])([H])C2=C([H])C([H])=C([H])C([H])=N2)=O)=NN=C1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=NN=1)N([H])C(C([H])([H])C1C([H])=C([H])C([H])=C(C=1[H])OC(F)(F)F)=O
Formula:	C26H24F3N7O3S
M.Wt:	571.5741
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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