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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
IL-15; IL-2; IL-4; IL-7; JAK3; STAT3; STAT5; STAT6
Available Sizes
Frequently Asked Questions
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