| Description | ORIC-101 is a highly effective and selective glucocorticoid receptor antagonist (EC50: 5.6 nM). It also has anti-cancer activity. |
| In vitro | ORIC-101 (1-1000 nM) dose-dependently decreases the expression of n GR-mediated target gene (IC50s: 17.2 and 21.2 nM, respectively). ORIC-101 displays markedly reduced androgen receptor agonism (EC50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC50, >10 μM)[1]. |
| In vivo | In OVCAR5 xenograft tumor in cortisol-treated mice, ORIC-101 (75 mg/kg, P.O. twice a day for 16-22 days) increases the anti-tumor activity in combination with gemcitabine and carboplatin[1]. |
| Target activity | GR:（EC50）5.6 nM |
| molecular weight | 501.74 |
| Molecular formula | C34H47NO2 |
| CAS | 2222344-98-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Rew Y, et al. Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). J Med Chem. 2018 Sep 13;61(17):7767-7784. |