A selective BTK inhibitor
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RN-486

Item No. 20536

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-1(2H)-isoquinolinone
CAS Number
1242156-23-5
Molecular Formula
C35H35FN6O3
Formula Weight
606.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMSO: 0.2 mg/ml
λmax
213, 217, 294, 344 nm
SMILES
O=C1C2=C(F)C=C(C3CC3)C=C2C=CN1C4=CC=CC(C5=CN(C)C(C(NC6=NC=C(N7CCN(C)CC7)C=C6)=C5)=O)=C4CO
InChi Code
InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38)
InChi Key
ZTUJNJAKTLHBEX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

    $256

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    10 mg

    $464

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    Product Description

    RN-486 is a Bruton’s tyrosine kinase inhibitor (Kd = 0.31 nM; IC50 = 4 nM) that displays a high degree of selectivity when tested against a panel of 369 kinases.1 It has been shown to block Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated TNF-α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of CD69 in B cells whole blood (IC50 = 21 nM).1 RN-486 is reported to produce anti-inflammatory and bone-protective effects in mouse collagen-induced arthritis and rat adjuvant-induced arthritis models.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xu, D., Kim, Y., Postelnek, J., et al. RN486, a selective Bruton’s tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J. Pharmacol. Exp. Ther. 341(1), 90-103 (2012).