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Poseltinib

Chemical Structure : Poseltinib

CAS No.: 1353552-97-2

Poseltinib (HM-71224, LY-3337641)

Catalog No.: PC-60536Not For Human Use, Lab Use Only.

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.

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Biological Activity

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
Poseltinib also inhibits BMX, TEC, TXK, EGFR in biochemical sense (IC50=0.3-2.5 nM).
Poseltinib effectively inhibits the phosphorylation of Btk and PLCγ2, and inhibits expression of CD40, CD69, and CD86 by activated primary human B cells with IC50 of 4.2, 4.2, and 7.7 nM, respectively.
Poseltinib inhibits the production of TNF-α, IL-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes; ameliorates arthritis in a mouse model.

Physicochemical Properties

M.Wt 470.533
Formula C26H26N6O3
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

2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]-

References

1. Park JK, et al. Arthritis Res Ther. 2016 Apr 18;18:91.

2. Akinleye A, et al. J Hematol Oncol. 2013 Aug 19;6:59.

3. Smith PF, et al. Br J Clin Pharmacol. 2017 Jun 21.

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