| Description: |
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. |
| Target: |
IC50: 3.65 μM (HIF-1)[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]. |
| 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]. |
| Animal Administration: |
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]. |
| References: |
[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 |
