IDF-11774

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC₅₀ of 3.65?μM. IC50 & Target: IC50: 3.65 μM (HIF-1α)^[1] In Vitro: IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC₅₀ of 3.65 μM in cancer cell line. IDF-11774 has been approved as a clinical candidate for a phase I study. Human umbilical vascular endothelial cells (HUVECs) treated with IDF-11774 show reduced capillary network formation on Matrigel. IDF-11774 treatment leads to reduced mRNA expression of GLUT1 and pyruvate dehydrogenase kinase 1 (PDK1). In addition, intracellular ATP levels are significantly reduced in the presence of IDF-11774 and are affected to a greater degree under low glucose conditions (5.5?mM)^[1]. In Vivo: Luciferase activity and HIF-1α accumulation are strongly suppressed in the tumors of mice treated by oral administration of IDF-11774, compare with the control. When IDF-11774 is orally administered daily for two weeks, significant dose-dependent tumor regression is observed in the mouse model^[1].