OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity.
IC50&Target
IC50: 0.4 μM (Heparanase)
体外研究
Heparanase InhibitorOGT 2115 can suppress metastasis induced by endoplasmic reticulum (ER) stress in breast cancer cells, although not significantly. However, compared with the control group, the number and rate of migrated cells are significantly reduced following the exposure of the cells to Tunicamycin + OGT 2115. OGT 2115 significantly inhibits the invasion and migration induced by Adriamycin. Furthermore, the MTT assay results show that OGT 2115 does not decrease the anti-proliferative effect of Adriamycin.
体内研究
When administered to mice, OGT 2115 (Compound 12d) shows a plasma concentration of ~10x the heparanase IC50 following oral dosing at 20 mg/kg.
分子式
C24H16BrFN2O4
分子量
495.30
CAS号
853929-59-6
运输条件
Room temperature in continental US; may vary elsewhere.