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Product Information:

PF-06651600 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].

Cat. No.: EX-A14814    Purity: >98%
Chemical
Chemical structure of PF-06651600 malonate


For research only, Do not use for Human!

SizeUnit Price (US$)StockQuantityOrder
100mg678Inquire
500mg1578Inquire
1g2450Inquire


SynonymsPF-06651600 malonate
CAS No.2140301-97-7
Purity>98%
FormulaC18H23N5O5
Mol Weight389.4057
StoragePlease store the product under the recommended conditions in the Certificate of Analysis.
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  

[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.

CoACoA of PF-06651600 malonate
Smiles:C[C@H]1CC[C@H](CN1C(=O)C=C)NC2=NC=NC3=C2C=CN3.C(C(=O)O)C(=O)O

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