Antitumor Activity Of The Glutaminase Inhibitor CB-839 In Hematological Malignances
Parlati F, Bromley-Dulfano S, Demo S et al.
Key Points:
CB-839 oral GLS inhibitor that inhibits recombinant human GLS with an I C50 of 15 nM.
Panel of 18 cell lines derived from MM, ALL and diffuse large B-cell lymphoma (DLBCL) tested on sensitivity to CB-839.
Majority of cell lines sensitive to CB-839 treatment with 16 cell lines exhibiting an antiproliferative IC50 of <100nM.
CB-839 has anti-tumor activity in vivo in xenograft model (RPMI-8226), which resulted in significant decrease in tumor volume (70% tumor growth inhibition).
Implications:
- Novel GLS inhibitor CB-839 may have therapeutic value in hematological malignances.
View the original abstract on the ASH website.
