ORIC-101


CAS No. : 2222344-98-9

2222344-98-9
Price and Availability of CAS No. : 2222344-98-9
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10mg $3000 In-stock
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Cat. No. : HY-112710
M.Wt: 501.74
Formula: C34H47NO2
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL
Introduction of 2222344-98-9 :

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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target: EC50: 5.6 nM (Glucocorticoid receptor)[1] 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]. 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].

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