Biological activity In vitro In vivo
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RN486

Biological activity In vitro In vivo
Product Name
RN486
CAS No.
1242156-23-5
Chemical Name
RN486
Synonyms
RN486;RN468;CS-689;RN486/RN-486;RN486 LM-2078;RN486 TFA Salt;RN486; RN-486; RN 486;6-Cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2;6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one;6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one
CBNumber
CB02650908
Molecular Formula
C35H35FN6O3
Formula Weight
606.69
MOL File
1242156-23-5.mol
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RN486 Property

Boiling point:
868.6±65.0 °C(Predicted)
Density 
1.378±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≥30.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
form 
solid
pka
13.95±0.10(Predicted)
color 
Off-white to light yellow
CAS DataBase Reference
1242156-23-5
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
20536
Product name
RN-486
Purity
≥98%
Packaging
1mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
20536
Product name
RN-486
Purity
≥98%
Packaging
5mg
Price
$232
Updated
2024/03/01
Cayman Chemical
Product number
20536
Product name
RN-486
Purity
≥98%
Packaging
10mg
Price
$421
Updated
2024/03/01
TRC
Product number
R637000
Product name
RN486
Packaging
1mg
Price
$100
Updated
2021/12/16
ChemScene
Product number
CS-1814
Product name
RN486
Purity
99.87%
Packaging
1mg
Price
$96
Updated
2021/12/16
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RN486 Chemical Properties,Usage,Production

Biological activity

RN486 is an effective BTK inhibitor with an IC50 of 4 nM.

In vitro

RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems.

In vivo

RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.

Uses

RN 486 is a Bruton’s tyrosine kinase (Btk) inhibitor, blocking receptor cross-linking-induced degranulation in mast cells. May be used in the prevention of arthritis and other autoimmune diseases.

RN486 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from RN486 manufacturers

Career Henan Chemical Co
Product
RN486 1242156-23-5
Price
US $1.00/KG
Min. Order
1KG
Purity
95%~99%
Supply Ability
1ton
Release date
2019-12-18

1242156-23-5, RN486Related Search:


  • RN486
  • 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-yl)pyridin-2-yl)aMiNA)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquiNAlin-1(2H)-one
  • 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one
  • CS-689
  • RN486; RN-486; RN 486
  • RN486/RN-486
  • RN468
  • 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
  • RN486 LM-2078
  • RN486 TFA Salt
  • 6-Cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2
  • 6-cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-on
  • 6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one
  • 2-(3-(5-(5-(4-methylpiperazin-1-yl)pyridin-2-ylamino)-1,6-dihydro-1-methyl-6-oxopyridin-3-yl)-2-(hydroxymethyl)phenyl)-6-cyclopropyl-8-fluoroisoquinolin-1(2H)-one
  • 1(2H)-Isoquinolinone, 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-
  • 1242156-23-5
  • C35H35FN6O3
  • Inhibitors