Cintirorgon (LYC-55716) (Synonyms: LYC-55716) |
رقم الكتالوجGC32713
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Cintirorgon (LYC-55716) (LYC-55716) هو RORγ من الدرجة الأولى في فئته وانتقائي ومتوفر بيولوجيًا ؛ ناهض. يعدل Cintirorgon (LYC-55716) (LYC-55716) التعبير الجيني لـ RORγ ؛ التعبير عن الخلايا المناعية للخلايا اللمفاوية التائية ، مما يؤدي إلى تعزيز وظيفة المستجيب ، وكذلك انخفاض كبت المناعة ، مما يؤدي إلى انخفاض نمو الورم وتحسين البقاء على قيد الحياة.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2055536-64-4
Sample solution is provided at 25 µL, 10mM.
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Cintirorgon (LYC-55716) is novel oral RAR-related orphan receptor γ (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 improves survival in 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). This may increase the expression of co-stimulatory molecules and decrease the expression of co-inhibitory molecules on T cells leading to increased production of cytokines and chemokines by T cells, decreases proliferation of regulatory T cells (Tregs), and abrogation of tumor-induced immunosuppression. This ultimately induces a T-cell-mediated immune response against cancer cells and leads to a reduction in tumor cell growth. 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].
[1]. Lycera Announces Initiation of Phase 1/2a Study ARGON of Immuno-Oncology Candidate LYC-55716 in Patients with Advanced Solid Tumors. Jan 04, 2017.
| Cas No. | 2055536-64-4 | SDF | |
| المرادفات | LYC-55716 | ||
| Canonical 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 | ||
| Formula | C27H23F6NO6S | M.Wt | 603.53 |
| الذوبان | DMSO : ≥ 113.3 mg/mL (187.73 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6569 mL | 8.2846 mL | 16.5692 mL |
| 5 mM | 331.4 μL | 1.6569 mL | 3.3138 mL |
| 10 mM | 165.7 μL | 828.5 μL | 1.6569 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)