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Poseltinib

SKU: orb1226468

Description

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM; also inhibits BMX, TEC, TXK, EGFR in biochemical sense (IC50=0.3-2.5 nM); 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; inhibited 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.Rheumatoid Arthritis Phase 1 Clinical.

Images & Validation

Key Properties

CAS Number1353552-97-2
MW470.533
Purity>98% (HPLC)
FormulaC26H26N6O3
SMILESC=CC(NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
TargetBTK
SolubilityIn Vitro: DMSO : 100 mg/mL (212.53 mM)

Bioactivity

In Vivo
Animal model: MRL/lpr mice and NZB/W F1 mice models. Dosage: 3-30 mg/kg. Administration: p.o. Result: Decreased the spleen weights and prevented skin lesion progression. Ameliorated renal injury and inflammation and improved the survival rate. Animal model: Collagen-induced arthritis (CIA) mouse model. Dosage: 1-30 mg/kg. Administration: p.o. Result: Reduced the serum IL-6, circulating anti-collagen antibodies and total IgG levels. Reduced erosive bone changes and prevented bone loss.
In Vitro
Western blot analysis. Cell line: B cells. Concentration: 0.1-100 nM Incubation time: 30 min. Result: Blocked both autophosphorylation of BTK and phosphorylation of PLCγ2 with IC50 values of less than 10 nM. Decreased the production of both TNF-α and IL-6 in a dose-dependent manner.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

HM-71224 | LY-3337641

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Poseltinib (orb1226468)

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5 mg
$ 300.00
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