Cintirorgon [2055536-64-4]
Referência HY-104037-1ml
Tamanho : 10mM/1mL
Marca : MedChemExpress
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Cintirorgon (LYC-55716) est un agoniste de RORγ premier de sa catégorie, sélectif et biodisponible par voie orale. Cintirorgon (LYC-55716) module l'expression génique des cellules immunitaires des lymphocytes T exprimant RORγ, ce qui entraîne une fonction effectrice améliorée, ainsi qu'une diminution de l'immunosuppression, entraînant une diminution de la croissance tumorale et une amélioration de la survie.
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
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Cintirorgon Chemical Structure
CAS No. : 2055536-64-4
This product is a controlled substance and not for sale in your territory.
Based on 6 publication(s) in Google Scholar
| Description |
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival[1][2]. |
IC50 & Target |
RORγ[1] |
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| In Vivo |
Upon oral administration of RORγ agonist Cintirorgon (LYC-55716), this agent selectively binds to the nuclear receptor transcription factor RORγ, forming a receptor complex that translocates to the nucleus, and binds to ROR response elements (ROREs), enhancing the function, proliferation and survival of type 17 T cells, including Th17 (helper T cells) and Tc17 (cytotoxic T cells). RORγ, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation, plays a key role in immune activation. Cintirorgon (LYC-55716) is also orally bioavailable, while the new generation of immuno-oncology drugs-ncluding PD-1/PD-L1 inhibitors are delivered by injection[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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| Essai clinique |
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| Masse moléculaire |
603.53 |
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| Formule |
C27H23F6NO6S |
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| CAS No. |
2055536-64-4 |
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| Appearance |
Solid |
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| Color |
White to off-white |
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| SMILES |
O=C(O)C(C)(C)C[C@@H]1OC2=CC=C(C3=CC(F)=CC(OC(F)F)=C3)C=C2N(S(=O)(C4=CC=CC(C(F)(F)F)=C4)=O)C1 |
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| Livraison | Room temperature in continental US; may vary elsewhere. |
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| Stockage |
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| Solvant et solubilité |
In Vitro:
DMSO : ≥ 113.3 mg/mL (187.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Ethanol : 100 mg/mL (165.69 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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| Pureté et documentation |
Purity: 98.53% |
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| Références |
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| Ethanol / DMSO | 1 mM | 1.6569 mL | 8.2846 mL | 16.5692 mL | 41.4230 mL |
| 5 mM | 0.3314 mL | 1.6569 mL | 3.3138 mL | 8.2846 mL | |
| 10 mM | 0.1657 mL | 0.8285 mL | 1.6569 mL | 4.1423 mL | |
| 15 mM | 0.1105 mL | 0.5523 mL | 1.1046 mL | 2.7615 mL | |
| 20 mM | 0.0828 mL | 0.4142 mL | 0.8285 mL | 2.0711 mL | |
| 25 mM | 0.0663 mL | 0.3314 mL | 0.6628 mL | 1.6569 mL | |
| 30 mM | 0.0552 mL | 0.2762 mL | 0.5523 mL | 1.3808 mL | |
| 40 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0356 mL | |
| 50 mM | 0.0331 mL | 0.1657 mL | 0.3314 mL | 0.8285 mL | |
| 60 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6904 mL | |
| 80 mM | 0.0207 mL | 0.1036 mL | 0.2071 mL | 0.5178 mL | |
| 100 mM | 0.0166 mL | 0.0828 mL | 0.1657 mL | 0.4142 mL |