Ritlecitinib (tosylate)

Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M) . Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) [1][2][3].

Product Specifications

CAS Number

[2192215-81-7]

Product Name Alternative

PF-06651600 (tosylate)

UNSPSC

12352005

Target

Interleukin Related; JAK; STAT

Type

Reference compound

Related Pathways

Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ritlecitinib-tosylate.html

Purity

99.77

Solubility

DMSO : 83.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(C=C1)=CC=C1S(O)(=O)=O.C=CC(N2[C@@H](C)CC[C@@H](NC3=C4C(NC=C4)=NC=N3)C2)=O

Molecular Formula

C22H27N5O4S

Molecular Weight

457.55

References & Citations

[1]Thorarensen A, et al. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1- ((2 S, 5 R) -5- ((7 H-Pyrrolo [2, 3-d] pyrimidin-4-yl) amino) -2-methylpiperidin-1-yl) prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. Journal of medicinal chemistry, 2017, 60 (5) : 1971-1993.|[2]Telliez JB, et al. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11 (12) :3442-3451.