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Poseltinib

SKU: orb1909042

Description

Poseltinib is a potent, selective, and irreversible BTK inhibitor (IC50=1.95 nM) that covalently targets Cys481. It exhibits high selectivity over related kinases and blocks key signaling pathways. This inhibitor is widely used in research for studying autoimmune diseases and B-cell malignancies in both cellular and animal models.

Research Area

Cardiovascular Research, Immunology & Inflammation, Signal Transduction

Images & Validation

Key Properties

CAS Number1353552-97-2
MW470.52
Purity99.98% (May vary between batches)
FormulaC26H26N6O3
SMILESO=C(C=C)NC=1C=CC=C(OC2=NC(=NC=3C=COC23)NC4=CC=C(C=C4)N5CCN(C)CC5)C1
TargetOthers,TLR,BTK
SolubilityDMSO:80 mg/mL (170.02 mM)

Bioactivity

Target IC50
BTK:1.95 nM
In Vivo
Methods: Poseltinib (3-30 mg/kg, daily) was orally administered to MRL/lpr and NZB/W F1 mouse models to evaluate the therapeutic effects of Poseltinib on systemic lupus erythematosus (SLE)-like disease characteristics in mice. Results: By inhibiting BTK, Poseltinib effectively reduced the overactivation of B cells and the production of autoantibodies, significantly alleviating the progression of SLE and lupus nephritis (LN) in mice. Poseltinib demonstrated notable improvements in skin lesions, renal function, kidney injury, and inflammation, while also increasing survival rates.
In Vitro
Methods: Ramos B lymphoma cells of Homo sapiens were treated with Poseltinib (0.1-100 nM, 30 min), and the expression of related proteins was analyzed by Western Blot. Results: Poseltinib simultaneously blocked the autophosphorylation of BTK and the phosphorylation of its physiological substrate PLCγ2, with IC50 values both less than 10 nM.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

HM 71224, HM71224, LY3337641, LY 3337641, Poseltinib

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  • Poseltinib [orb1226468]

    >98% (HPLC)

    1353552-97-2

    470.533

    C26H26N6O3

    5 mg, 10 mg, 50 mg, 1 g, 500 mg, 200 mg, 100 mg
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Key Properties

No computed properties available.

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Protocol Information

Poseltinib (orb1909042)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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2 mg
$ 70.00
1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 200.00
50 mg
$ 330.00
100 mg
$ 500.00
200 mg
$ 700.00
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