T-3764518 (T 3764518, T3764518) is a novel potent, orally active SCD1 inhibitor with binding IC50 of 4.7 nM for hSCD1.
T-3764518 induces phosphorylation and activation of AMPK in HCT-116 cells, which led to blockade of downstream fatty acid synthesis and acceleration of autophagy.
T-3764518 shows significant pharmacodynamic marker reduction (at 0.3mg/kg, bid) in HCT116 mouse xenograft model and tumor growth suppression (at 1mg/kg, bid) in 786-O mouse xenograft model; exhibits an excellent PK profile.
