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Purity: ≥98%
Cintirorgon (formerly also known as LYC55716; LYC-55716), a novel and potent immune modulatory medicine developed by Lycera, is a synthetic and orally bioavailable small molecule agonist of RAR-related orphan receptor γ (RORγ). It combines multiple anti-tumor mechanisms into a single therapeutic by modulating gene expression to reprogram immune cells for improved function, as well as decrease immunosuppressive mechanisms. In January 2018, Lycera announced the initiation of a multi-center Phase 1B combination study in patients with advanced, relapsed, or refractory solid tumors such as metastatic Non-Small Cell Lung Cancer in combination with pembrolizumab.
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| ln Vivo |
Cintirorgon (LYC-55716), a RORγ agonist, is administered orally and forms a receptor complex with the nuclear receptor transcription factor RORγ. The drug then translocates to the nucleus where it binds to the ROR response element (RORE) to improve function. Type 17 T cells, such as Th17 (helper T cells) and Tc17 (cytotoxic T cells), proliferate and survive. Th17/Tc17 differentiation is facilitated by the nuclear receptor transcription factor RORγ, which is also essential for immune activation. While next generation immuno-oncology medications, such as PD-1/PD-L1 inhibitors, are provided by injection, cintirorgon (LYC-55716) is also bioavailable when taken orally [1].
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| Additional Infomation |
Cintirorgon is an orally bioavailable agonist of retinoic acid-related orphan receptor gamma (RORg), with potential immunomodulatory and antineoplastic activities. Upon oral administration of cintirorgon, this agent selectively binds to the nuclear receptor transcription factor RORg, 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, decreased 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. RORg, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation, plays a key role in immune activation.
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| Molecular Formula |
C27H23F6NO6S
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| Molecular Weight |
603.530047655106
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| Exact Mass |
603.115
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| CAS # |
2055536-64-4
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| Related CAS # |
2055538-47-9 (sodium);2055536-64-4 (free acid);
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| PubChem CID |
124126348
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| Appearance |
White to off-white solid powder
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| LogP |
6.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
1
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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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| InChi Key |
GULSIMHVQYBADX-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C27H23F6NO6S/c1-26(2,24(35)36)13-20-14-34(41(37,38)21-5-3-4-17(11-21)27(31,32)33)22-10-15(6-7-23(22)39-20)16-8-18(28)12-19(9-16)40-25(29)30/h3-12,20,25H,13-14H2,1-2H3,(H,35,36)/t20-/m0/s1
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.14 mM) (saturation unknown) in 5% DMSO + 40% PEG300 +5% Tween-80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6569 mL | 8.2846 mL | 16.5692 mL | |
| 5 mM | 0.3314 mL | 1.6569 mL | 3.3138 mL | |
| 10 mM | 0.1657 mL | 0.8285 mL | 1.6569 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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