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.
Product information
CAS Number: 2055536-64-4
Molecular Weight: 603.53
Formula: C27H23F6NO6S
Chemical Name: 3-[(2S)-6-[3-(difluoromethoxy)-5-fluorophenyl]-4-[3-(trifluoromethyl)benzenesulfonyl]-3,4-dihydro-2H-1,4-benzoxazin-2-yl]-2,2-dimethylpropanoic acid
Smiles: CC(C)(C[C@H]1CN(C2=CC(=CC=C2O1)C1=CC(F)=CC(=C1)OC(F)F)S(=O)(=O)C1=CC=CC(=C1)C(F)(F)F)C(O)=O
InChiKey: GULSIMHVQYBADX-FQEVSTJZSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 113.3 mg/mL (187.73 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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