1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. ORIC-101

ORIC-101 

目录号: HY-112710
产品使用指南

ORIC-101 是一种有效、选择性的糖皮质激素受体 (glucocorticoid receptor) 拮抗剂,EC50 值为 5.6 nM。抗癌作用。

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ORIC-101 Chemical Structure

ORIC-101 Chemical Structure

CAS No. : 2222344-98-9

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Description

ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. Anti-cancer activity.

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].

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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

501.74

Formula

C₃₄H₄₇NO₂

CAS No.

2222344-98-9

SMILES

CN(C(C)C)C1=CC=C([C@@H]2[C@@]([C@](CC3)([H])C(CC4)=CC3=O)([H])[C@]4([H])[C@@](CC[C@]5(C#CC(C)(C)C)O)([H])[C@]5(C)C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
ORIC-101
目录号:
HY-112710
需求量:

ORIC-101

Cat. No.: HY-112710