文献

APIM050044: 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.

CAS No.: 2055536-64-4
IUPAC/Chemical Name: (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
Molecular Formula: C₂₇H₂₃F₆NO₆S
Molecular Weight: 603.53
Purity: >99.5% chemical and optical purity (by achiral and chiral HPLCs)
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO
Storage: Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Note: Please contact us for COA, Spectra, and SDS information.

Background Information:

Target: RORγ

In Vivo: Upon oral administration of RORγ agonist Cintirorgon (LYC-55716) (CAS No. 2055536-64-4), 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]

What is the solubility of Cintirorgon (LYC-55716) (CAS No. 2055536-64-4) in vitro?
DMSO: > 113.3 mg/mL

What is the solubility of Cintirorgon (LYC-55716) (CAS No. 2055536-64-4) in vivo?
DMSO, PEG300, Tween-80, and saline
Please add 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline in order, solubility: 2.5 mg/mL.

Reference:
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[2]. Weems, G. A. 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.”, J. Clin. Oncol., 2018, DOI: 10.1200/JCO.2018.36.4_suppl.67

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