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Ritlecitinib (malonate)

Ritlecitinib (malonate)

Item no.	HY-100754A
Manufacturer	MedChem Express
CASRN	2140301-97-7
Amount	1 ea
Quantity options	1 ea 10 mg 5 mg
Category	Inhibitors & Compound Libraries Compound Libraries
Type	Inhibitors
Specific against	other
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.
Smiles	OC(CC(O)=O)=O.C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	PF-06651600 (malonate)
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	COVID-19-immunoregulation
Manufacturer - Targets	Interleukin Related; JAK; STAT
Shipping Temperature	Room temperature
Molecular Weight	389.41
Product Description	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].
Manufacturer - Research Area	Inflammation/Immunology
Solubility	10 mM in DMSO
Manufacturer - Pathway	Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Isoform	IL-15; IL-2; IL-4; IL-7; JAK3; STAT3; STAT5; STAT6
Clinical information	Launched

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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