| Identification | Back Directory | [Name]
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- | [CAS]
2222344-98-9 | [Synonyms]
ORIC101,ORIC 101
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- | [Molecular Formula]
C34H47NO2 | [MDL Number]
MFCD32062751 | [MOL File]
2222344-98-9.mol | [Molecular Weight]
501.76 |
| Chemical Properties | Back Directory | [Boiling point ]
640.5±55.0 °C(Predicted) | [density ]
1.11±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.82±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [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. |
| [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. DOI:10.1021/acs.jmedchem.8b00743 |
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