WP1066

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. IC50 & Target: JAK2, STAT3^[1] In Vitro: WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC₅₀ value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform^[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC₅₀ doses of WP1066 for B16 cells is 2.43 µM (0.865 µg/mL)^[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation^[3]. In Vivo: WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment^[2].