tcsc2736 WP1066

WP1066 is a novel 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.)does not further enhance the therapeutic effects of cyclophosphamide on pulmonary melanoma lesions, enhance the therapeutic effects of cyclophosphamide against CNS melanoma, or further enhance immune-mediated cytotoxic effects of CTX in C57BL/6J mice. WP1066 exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment^[2].