19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)-

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19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- Basic information
Product 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)-
Synonyms:19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)-;ORIC101,ORIC 101
CAS:2222344-98-9
MF:C34H47NO2
MW:501.76
EINECS:
Product Categories:
Mol File:2222344-98-9.mol
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- Structure
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- Chemical Properties
Boiling point 640.5±55.0 °C(Predicted)
density 1.11±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
pka12.82±0.60(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- Usage And Synthesis
UsesORIC-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
19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)- Preparation Products And Raw materials
Tag:19,21-Dinorchol-4-en-20(22)-yn-3-one, 17-hydroxy-23,23-dimethyl-11-[4-[methyl(1-methylethyl)amino]phenyl]-, (11β,17α)-(2222344-98-9) Related Product Information
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