Crenolanib

Human 7, 8-Dihydro-8-oxoguanine triphosphatase MTH1 (NUDT1) is an enzyme that hydrolyzes oxidized purine nucleoside triphosphates which accumulate resulting from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells. The oxidized nucleosides helps protect cancer cells from proliferative stress and prevent cancer cell death. Containment of MTH1 is considered an anticancer strategy. (S)-Crizotinib, the opposite enantiomer of (R)-Crizotinib (PF02341066, Chemietek Prod No CT-PF0234), is a selective inhibitor of MTH1 with an IC50 value of 72 nM while R-enantiomer is inactive (IC50 > 1000 nM). In mouse xenograft studies using SW480 cells, (S)-Crizotinib, not the (R)-Crizotinib, was able to impair overall tumor progression as well as specifically reduce tumor volume by more than 50% (ref 1).

Soluble in DMSO, Ethanol