1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  2. Glucocorticoid Receptor
  3. ORIC-101

ORIC-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.

For research use only. We do not sell to patients.

ORIC-101 Chemical Structure

ORIC-101 Chemical Structure

CAS No. : 2222344-98-9

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1 mg USD 620 In-stock
5 mg USD 1850 In-stock
10 mg USD 3000 In-stock
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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. 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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) 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
Molecular Weight

501.74

Formula

C34H47NO2

CAS No.
Appearance

Solid

Color

White to off-white

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.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (199.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9931 mL 9.9653 mL 19.9306 mL
5 mM 0.3986 mL 1.9931 mL 3.9861 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.30%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9931 mL 9.9653 mL 19.9306 mL 49.8266 mL
5 mM 0.3986 mL 1.9931 mL 3.9861 mL 9.9653 mL
10 mM 0.1993 mL 0.9965 mL 1.9931 mL 4.9827 mL
15 mM 0.1329 mL 0.6644 mL 1.3287 mL 3.3218 mL
20 mM 0.0997 mL 0.4983 mL 0.9965 mL 2.4913 mL
25 mM 0.0797 mL 0.3986 mL 0.7972 mL 1.9931 mL
30 mM 0.0664 mL 0.3322 mL 0.6644 mL 1.6609 mL
40 mM 0.0498 mL 0.2491 mL 0.4983 mL 1.2457 mL
50 mM 0.0399 mL 0.1993 mL 0.3986 mL 0.9965 mL
60 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8304 mL
80 mM 0.0249 mL 0.1246 mL 0.2491 mL 0.6228 mL
100 mM 0.0199 mL 0.0997 mL 0.1993 mL 0.4983 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
ORIC-101
Cat. No.:
HY-112710
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