LYC-55716 (CINTIRORGON)
$180.00 – $1,200.00
Cintirorgon (CAS No.: 2055536-64-4), 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. >99.5% Purity.
Synonyms: LYC-55716, LYC55716, RORγ agonist
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Description
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:
[1]. Aicher, T. D. et al. “Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer”, J. Med. Chem., 2021, 64, 13410-13428.
[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
[3]. Park, S. A. et al. “TIMP-1 mediates TGF-β-dependent crosstalk between hepatic stellate and cancer cells via FAK signaling”, Sci. Rep., 2015, 5, 16492.
[4]. Han, K. et al. “EW-7197 eluting nano-fiber covered self-expandable metallic stent to prevent granulation tissue formation in a canine urethral model”, Plos One 2018, https://doi.org/10.1371/journal.pone.0192430.
[5]. Yoon, S.-H. et al. “EW-7197, a Transforming Growth Factor-Beta Type I Receptor Kinase Inhibitor, Ameliorates Acquired Lymphedema in a Mouse Tail Model”, Lymphat. Res. Biol., 2020, https://doi.org/10.1089/lrb.2018.0070
[6]. Kim, B.-G. et al. “Abstract 2647: TGF-β type I receptor inhibitor (TEW-7197) diminishes myeloma progression by multiple immunomodulatory mechanisms in combination with ixazomib”, Cancer Res., 2017, DOI: 10.1158/1538-7445.AM2017-2647.
[7]. Malek, E. et al. “Preclinical Studies and a Phase I Trial of the TGF-β Receptor Inhibitor, Vactosertib (TEW-7197), in Combination with Pomalidomide in Patients with Multiple Myeloma Refractory to Bortezomib or Lenalidomide”, Blood, 2018, https://doi.org/10.1182/blood-2018-99-112449
[8]. Song, K.-M. et al. “AB083. TEW-7197, a novel orally bioavailable activin receptor-like kinase 5 inhibitor, promotes regression of fibrotic plaque in a rat model of Peyronie’s disease”, Transl. Androl. Urol., 2018, doi: 10.21037/tau.2018.AB083
[9]. Kim, B.-G. et al. “Vactosertib, a TGF-ß Receptor I Kinase/ALK5 Inhibitor, Diminishes Tumor Progression and Bone Disease in a Mouse Model of Multiple Myeloma and Overcomes Resistance to Proteasome Inhibitors”, Blood, 2018, https://doi.org/10.1182/blood-2018-99-117852
[10]. Jin, C. H. et al. “Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of TGF-β Type I Receptor Kinase as Cancer Immunotherapeutic/Antifibrotic Agent”, J. Med. Chem., 2014, https://doi.org/10.1021/jm500115w
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