ORIC-101 | GR antagonist | Probechem Biochemicals

Chemical Structure : ORIC-101

ORIC-101 (ORIC101)

Catalog No.: PC-35571Not For Human Use, Lab Use Only.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

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Biological Activity

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.
ORIC-101 dose-dependently reduces the expression levels of two established GR target genes, GILZ and FKBP5 with IC50 of 24.9 and 19.5 nM in human PBMCs.
ORIC-101 demonstrates in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model.

Physicochemical Properties

M.Wt	501.755
Formula	C34H47NO2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(8R,9S,10R,11S,13S,14S,17S)-17-(3,3-Dimethylbut-1-yn-1-yl)-17-hydroxy-11-(4-(isopropyl(methyl)amino)phenyl)-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one

References

1. Rew Y, et al. J Med Chem. 2018 Aug 9. doi: 10.1021/acs.jmedchem.8b00743.

ORIC-101 (ORIC101)

Biological Activity

Physicochemical Properties

References

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