Potent MTH1 inhibitor (Kd
= 49 nM). Inhibits Ras-induced malignant transformation and increases α
-actin promoter-driven CAT activity in Ras-transformed cells. Has no effect on Ras-induced ERK and JNK activation. Inhibits Ras-induced membrane ruffling in REF-52 fibroblasts and blocks anchorage-independent growth of Ras-transformed tumor cell lines. Also induces DNA damage in SW480 colon cancer cells.
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Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
Huber KV, Salah E, Radic B et al.
SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway.
Walsh et al.
SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway.
Kumar et al.