ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC 50 of 5.6 nM. Anti-cancer activity. In Vitro ORIC-101 shows markedly reduced androgen receptor agonism (EC 50 , 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC 50 , >10 μM). ORIC-101 (1-1000 nM) dose-dependently reduces the expression of n GR-mediated target gene (FKBP5 and GILZ), with IC 50 s of 17.2 and 21.2 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: OVCAR5 xenograft tumor in cortisol-treated mice 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. Form:Solid IC50& Target:EC50: 5.6 nM (Glucocorticoid receptor)
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ORIC-101
CAS number:2222344-98-9 molecular formula:C34H47NO2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2222344-98-9 | molecular formula | C34H47NO2 |
| molecular weight | 501.74 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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