ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC 50 of 5.6 nM. Anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
EC50: 5.6 nM (Glucocorticoid receptor)
体外研究(In Vitro)
ORIC-101 shows markedly reduced androgen receptor agonism (EC50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC50, >10 μM).ORIC-101 (1-1000 nM) dose-dependently reduces the expression of n GR-mediated target gene (FKBP5 and GILZ), with IC50s of 17.2 and 21.2 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ORIC-101 (75 mg/kg, P.O. twice a day for 16-22 days) enhances the anti-tumor activity in combination with gemcitabine and carboplatin in OVCAR5 xenograft tumor in cortisol-treated mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.