ORIC-101 |
| カタログ番号GC65370 |
ORIC-101 は、5.6 nM の EC50 を持つ、非常に強力で選択的なグルココルチコイド受容体アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2222344-98-9
Sample solution is provided at 25 µL, 10mM.
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ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity.
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].
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].
[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.
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