Ritlecitinib

CAT: 0804-HY-100754-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-100754-01Size:5 mg
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Description
Ritlecitinib (PF-06651600) 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 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 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].
CAS Number
[1792180-81-4]
Product Name Alternative
PF-06651600
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
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/PF-06651600.html
Purity
99.80
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O
Molecular Formula
C15H19N5O
Molecular Weight
285.35
Precautions
H302, H315, H319, H335
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
IL-15; IL-4; IL-7; JAK3; STAT3; STAT5; STAT6

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