CB-839, Glutaminase Inhibitor (TBI4556)

Description

Product Details

Formal Name: 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide

Alternate Names: Telaglenastat

Molecular Formula: C₂₆H₂₄F₃N₇O₃S

Formula Weight: 571.60

CAS Number: 1439399-58-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (20 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Glutaminase Inhibitor

Functions

Potent and noncompetitive inhibitor of both glutaminase GLS splice variants (KGA and GAC, IC50 ~ 25 nM), but not GLS2. It limits the entry of glutamine derivates into the TCA cycle, starves tumor cells of glutamine, and ablates stem-like cells in GLS-overexpressing glioblastoma cells. Effective in a variety of cancer models, including triple-negative breast cancer and squamous cell carcinoma.

Application Procedures

First dissolved in DMSO (20 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 2 months.