TRX-818 is an anticancer compound.1,2 It inhibits vasculogenic mimicry network formation in C8161 and SK-MEL-28 melanoma cells when used at concentrations ranging from less than or equal to 5 to 10 nM. 1 TRX-818 (10 nM) decreases pro-Nodal protein levels and Smad2 phosphorylation in C8161 cells. It reduces tumor volume with a minimum effective dose (MED) value of 50 mg/kg and decreases the number of vasculogenic mimicry channels in tumors when administered at a dose of 100 mg/kg in an HCT116 colon cancer mouse xenograft model. TRX-818 (7.5, 15, and 30 mg/kg) reduces tumor growth in a Hep3B mouse xenograft model in a dose-dependent manner.2
1.Chu, Y.-W., and Chien, D.-S.Use of aryl-quinolin derivatives as inhibitors of vasculogenic mimicry(2016) 2.Chou, L.-C., Tsai, M.-T., Hsu, M.-H., et al.Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agentsJ. Med. Chem.53(22)8047-8058(2010)