LYC-55716
LYC-55716 Basic information
- Product Name:
- LYC-55716
- Synonyms:
-
- LYC-55716
- (S)-3-(6-(3-(difluoromethoxy)-5-fluorophenyl)-4-((3-(trifluoromethyl)phenyl)sulfonyl)-3,4-dihydro-2H-benzo[b][1,4]oxazin-2-yl)-2,2-dimethylpropanoic acid
- Cintirorgon)
- LYC-55716 (LYC55716
- 2H-1,4-Benzoxazine-2-propanoic acid, 6-[3-(difluoromethoxy)-5-fluorophenyl]-3,4-dihydro-α,α-dimethyl-4-[[3-(trifluoromethyl)phenyl]sulfonyl]-, (2S)-
- Cintirorgon (LYC-55716)
- 9-hydroxy-3-isobutyl-10-methoxy-3,4,6,7-tetrahydro-1H-pyrido[2,1-a]isoquinolin-2(11bH)-one
- Cintirorgon（ LYC-557160
- CAS:
- 2055536-64-4
- MF:
- C27H23F6NO6S
- MW:
- 603.53
- Mol File:
- 2055536-64-4.mol
LYC-55716 Chemical Properties
- Boiling point:
- 669.1±65.0 °C(Predicted)
- Density
- 1.417±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 100 mg/ml
- form
- A crystalline solid
- pka
- 4.68±0.10(Predicted)
- color
- White to off-white
- InChIKey
- GULSIMHVQYBADX-XKGZFIRZNA-N
- SMILES
- S(C1C=CC=C(C(F)(F)F)C=1)(N1C[C@H](CC(C)(C)C(=O)O)OC2=CC=C(C3C=C(F)C=C(OC(F)F)C=3)C=C12)(=O)=O |&1:13,r|
LYC-55716 Usage And Synthesis
Uses
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].
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].
References
[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.
LYC-55716Supplier
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