1242156-23-5
中文名称
RN 486
英文名称
RN486
CAS
1242156-23-5
分子式
C35H35FN6O3
分子量
606.689
MOL 文件
1242156-23-5.mol
更新日期
2024/08/15 16:57:44
1242156-23-5 结构式
基本信息
中文别名
化合物DBEQ化合物RN486
英文别名
RN486RN468
RN486/RN-486
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-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one
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
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
所属类别
生物化工：BTK 抑制剂物理化学性质
沸点868.6±65.0 °C(Predicted)
密度1.378±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度≥30.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
酸度系数(pKa)13.95±0.10(Predicted)
形态固体
颜色Off-white to light yellow
CAS 数据库1242156-23-5
常见问题列表
生物活性
RN486是一种有效的选择性BTK 抑制剂，IC50为4 nM。体外研究
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.体内研究
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.