CB-839(Telaglenastat) chemical structure
Chemical structureResearch use only
CAT. NO. DC8042Featured

CB-839(Telaglenastat)

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Product overview

Description & Application

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

ParameterValue
Chemical NameTelaglenastat
CAS No.1439399-58-2
SynonymsCB-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
FormulaC26H24F3N7O3S
M.Wt571.57
SMILESS1C(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
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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

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].

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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