| Description |
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity.
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| Related Catalog |
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| Target |
EC50: 5.6 nM (Glucocorticoid receptor)[1]
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| In Vitro |
ORIC-101 shows markedly reduced androgen receptor agonism (EC50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC50, >10 μM)[1]. 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[1].
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| 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[1]. Animal Model: OVCAR5 xenograft tumor in cortisol-treated mice[1] Dosage: 75 mg/kg with 100 mg/kg gemcitabine and 60 mg/kg carboplatin Administration: P.O. twice a day for 16-22 days Result: Significantly reduced tumor volume in combination with chemotherapeutic agents.
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| 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.
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