IDF-11774

IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC50 of 3.65 μM. IDF-11774 has been approved as a clinical candidate for a phase I study.

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

Research Areas >> Cancer

IC50: 3.65 μM (HIF-1)[1]

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].

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].

Female Balb/c nude mice are used in this study. Cancer cells are injected subcutaneously into 4- to 6-week-old female Balb/c nude mice to generate tumors (5 mice per group). When the tumors grow to 100 mm3, IDF-11774 is administered orally (per oral) or intravenously for 15 days. Tumor volumes (V) are determined using the following equation: V (mm3)=(length×width×height)×0.5. Percentage tumor growth inhibition (%TGI) values are calculated for each treatment group versus the control[1].

[1]. Ban HS, et al. The novel hypoxia-inducible factor-1α inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumor growth. Cell Death Dis. 2017 Jun 1;8(6):e2843.

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