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RN486

SKU: orb1306892

Description

RN486 is a potent and selective small molecule inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 4 nM. It is a valuable research tool for investigating B-cell receptor signaling in immunological and oncological studies, applicable in both cellular assays and in vivo disease models.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

Key Properties

CAS Number1242156-23-5
MW606.69
Purity99.38% (May vary between batches)
FormulaC35H35FN6O3
SMILESCN1CCN(CC1)c1ccc(Nc2cc(cn(C)c2=O)-c2cccc(c2CO)-n2ccc3cc(cc(F)c3c2=O)C2CC2)nc1
TargetBTK
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:58 mg/mL (95.6 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
BTK:4 nM
In Vivo
RN486 selectively inhibits Bruton’s tyrosine kinase and demonstrates functional activity across multiple human cell types in vitro. It blocks mast cell degranulation induced by Fcε receptor cross-linking (IC50: 2.9 nM), inhibits the production of tumor necrosis factor α in monocytes triggered by the engagement of Fcγ receptors (IC50: 7.0 nM), and reduces the expression of the activation marker CD69 in B cells following B cell antigen receptor engagement in whole blood (IC50: 21.0 nM).
In Vitro
In the AIA model, RN486, either alone or in combination with methotrexate, effectively suppresses joint and systemic inflammation, reducing both paw swelling and the levels of inflammatory markers in the blood. Its functional activity in rodent models parallels these effects, efficiently preventing type I and III hypersensitivity reactions. Furthermore, RN486 demonstrates significant bone protection and anti-inflammatory properties in mouse CIA and rat adjuvant-induced arthritis models.

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

Bruton tyrosine kinase, BTK, Btk, inhibit, Inhibitor, RN486, RN-486, RN 486

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    C35H35FN6O3

    1 g, 500 mg, 200 mg, 50 mg, 100 mg, 25 mg, 5 mg, 10 mg
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Key Properties

No computed properties available.

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RN486 (orb1306892)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 120.00
5 mg
$ 150.00
1 ml x 10 mM (in DMSO)
$ 190.00
10 mg
$ 220.00
25 mg
$ 390.00
50 mg
$ 590.00
100 mg
$ 870.00
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