1. Protein Tyrosine Kinase/RTK
  2. Btk

RN486 

Cat. No.: HY-18018 Purity: 99.38%
Handling Instructions

RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM.

For research use only. We do not sell to patients.

RN486 Chemical Structure

RN486 Chemical Structure

CAS No. : 1242156-23-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 208 In-stock
Estimated Time of Arrival: December 31
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 432 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM. IC50 Value: 4.0 nM [1] Target: Btk Kinase in vitro: In the enzymatic assay, the compound potently inhibited Btk kinase activity with an IC50 of 4.0 nM. RN486 not only potently and selectively inhibited the Btk enzyme, but also displayed functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM) [1]. In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which was dose-dependently blocked by RN486 [2]. in vivo: RN486 displayed similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood [1]. The administration of RN486 completely stopped disease progression, as determined by histologic and functional analyses of glomerular nephritis. The efficacy was associated with striking inhibition of B cell activation, as demonstrated by a significant reduction in CD69 expression in response to BCR crosslinking. RN486 markedly reduced the secretion of IgG anti-double-stranded DNA (anti-dsDNA) secretion, as determined by enzyme-linked immunosorbent and enzyme-linked immunospot assays [3].

Solvent & Solubility
In Vitro: 

DMSO : 24 mg/mL (39.56 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6483 mL 8.2414 mL 16.4829 mL
5 mM 0.3297 mL 1.6483 mL 3.2966 mL
10 mM 0.1648 mL 0.8241 mL 1.6483 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

606.69

Formula

C₃₅H₃₅FN₆O₃

CAS No.

1242156-23-5

SMILES

O=C1C(NC2=CC=C(N3CCN(C)CC3)C=N2)=CC(C4=CC=CC(N5C=CC(C=C(C6CC6)C=C7F)=C7C5=O)=C4CO)=CN1C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
RN486
Cat. No.:
HY-18018
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RN486

Cat. No.: HY-18018