ORIC-101

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ORIC-101 

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。

ORIC-101

ORIC-101 Chemical Structure

CAS No. : 2222344-98-9

规格 价格 是否有货
5 mg ￥47000 询问价格 & 货期

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生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

501.74

Formula

C34H47NO2
CAS 号

2222344-98-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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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