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LYC-55716

Chemical Structure : LYC-55716

CAS No.: 2055536-64-4

LYC-55716 (LYC55716;Cintirorgon)

Catalog No.: PC-63532Not For Human Use, Lab Use Only.

Cintirorgon (LYC-55716) is a potent, selective, and orally bioavailable Retinoic acid Receptor-related orphan receptor-γ (RORγ) agonist with FRET EC50 of 13 nM.

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Biological Activity

Cintirorgon (LYC-55716) is a potent, selective, and orally bioavailable Retinoic acid Receptor-related orphan receptor-γ (RORγ) agonist with FRET EC50 of 13 nM.
LYC-55716 displays high selectivity over other NRs, including RORα and RORβ (EC50>10 uM).
LYC-55716 modulates expression of genes that promote immune responses, reduces PD-1 expression in vitro and in vivo after adoptive cell transfer, relieves PD-1/PD-L1 inhibition of proliferation and IFNγ.|
LYC-55716 significantly augments anti-tumor activity of doxorubicin, results in immune-dependent decreased tumor growth and enhanced survival in preclinical models of cancer.

Physicochemical Properties

M.Wt 603.532
Formula C27H23F6NO6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Garry Alan Weems, et al. Lyc-55716: A novel small-molecule RORγ agonist immuno-oncology agent: Rationale for tumor selection and clinical evaluation of gastric and esophageal carcinoma in phase 2a expansion. DOI: 10.1200/JCO.2018.36.4_suppl.67 Journal of Clinical Oncology 36, no. 4_suppl (February 1 2018) 67-67.

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