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编 号:F279310
分子式:C34H47NO2
分子量:501.74
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1mg
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生物活性:
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity. ORIC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
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.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.

体外研究:
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.
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