CB-839 | B1179

CB-839 is a potent, selective, and orally bioavailable inhibitor of both splice variants of glutaminase (KGA and GAC); inhibits recombinant GAC with an IC₅₀ of <15 nM. CB-839 displays antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, that is associated with a marked decrease in glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.

CB-839 is a potent, selective, and orally bioavailable inhibitor of both splice variants of glutaminase (KGA and GAC); inhibits recombinant GAC with an IC₅₀ of <15 nM. CB-839 displays antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, that is associated with a marked decrease in glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.

B1179 | CB-839 DataSheet

Alternate Name/Synonyms: 2-(pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide

Appearance: Light yellow to yellow solid

Formulation: N/A

CAS Number: 1439399-58-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: N/A

Molecular Formula: C₂₆H₂₄F₃N₇O₃S

Molecular Weight: 571.57

Cell-Permeable?: Yes

Purity: ≥97% by HPLC

Solubilities: DMSO

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent glutaminase inhibitor

MDL Number: N/A

PubChem CID: 71577426

SMILES: C1=CC=NC(=C1)CC(=O)NC2=NN=C(S2)CCCCC3=NN=C(C=C3)NC(=O)CC4=CC(=CC=C4)OC(F)(F)F

InChi: InChI=1S/C26H24F3N7O3S/c27-26(28,29)39-20-9-5-6-17(14-20)15-22(37)31-21-12-11-18(33-34-21)7-1-2-10-24-35-36-25(40-24)32-23(38)16-19-8-3-4-13-30-19/h3-6,8-9,11-14H,1-2,7,10,15-16H2,(H,31,34,37)(H,32,36,38)

InChi Key: PRAAPINBUWJLGA-UHFFFAOYSA-N