Ritlecitinib (malonate)

Ritlecitinib (PF-06651600) malonate 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 malonate 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 malonate 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

[2140301-97-7]

Product Name Alternative

PF-06651600 (malonate)

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-malonate.html

Solubility

10 mM in DMSO

Smiles

OC(CC(O)=O)=O.C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O

Molecular Formula

C18H23N5O5

Molecular Weight

389.41

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.