IDH2R140Q-IN-2

Names

[ Name ]:
IDH2R140Q-IN-2

Biological Activity

[Description]:

IDH2R140Q-IN-2 (compound 36) is an an orally active IDH2R140Q inhibitor (IC50: 29 nM). IDH2R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2R140Q (IC50: 10 nM). IDH2R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2R140Q-IN-2 can be used for research of acute myeloid leukemia (AML)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Isocitrate Dehydrogenase (IDH)

[References]

[1]. Wei Q, et al. Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2R140Q Inhibitors with High Selectivity and Reduced hERG Inhibitory Activity for the Treatment of Acute Myeloid Leukemia. J Med Chem. 2023 Sep 28;66(18):12894-12910.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₈F₆N₆O

[ Molecular Weight ]:
484.40

IDH2R140Q-IN-2

Names

Biological Activity

Chemical & Physical Properties

Related Compounds