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PF-06651600 malonate

Chemical Structure : PF-06651600 malonate

CAS No.: 2140301-97-7

PF-06651600 malonate (Ritlecitinib, PF06651600 malonate)

Catalog No.: PC-62334Not For Human Use, Lab Use Only.

PF-06651600 malonate (Ritlecitinib) is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PF-06651600 malonate (Ritlecitinib) is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2.
PF-06651600 inhibits Th1 and Th17 cell differentiation and function, reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models.
PF-06651600 selectively targets γc cytokine pathways while preserving JAK1-dependent anti-inflammatory signaling such as the IL-10 suppressive functions following LPS treatment in macrophages and the suppression of TNFα and IL-1β production in IL-27-primed macrophages.

Physicochemical Properties

M.Wt 389.412
Formula C18H23N5O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malonate

References

1. Telliez JB, et al. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451.

2. Thorarensen A, et al. J Med Chem. 2017 Mar 9;60(5):1971-1993.

3. Robinette ML, et al. Mucosal Immunol. 2017 May 17. doi: 10.1038/mi.2017.38.

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