1242156-23-5
中文名稱(chēng)
RN 486
英文名稱(chēng)
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
2024/12/26 17:36:50
1242156-23-5 結(jié)構(gòu)式
基本信息
中文別名
化合物DBEQ化合物RN486
英文別名
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
所屬類(lèi)別
生物化工：BTK 抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)868.6±65.0 °C(Predicted)
密度1.378±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度≥30.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
酸度系數(shù)(pKa)13.95±0.10(Predicted)
形態(tài)固體
顏色Off-white to light yellow
CAS 數(shù)據(jù)庫(kù)1242156-23-5
常見(jiàn)問(wèn)題列表
生物活性
RN486是一種有效的選擇性BTK 抑制劑，IC50為4 nM。體外研究
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.體內(nèi)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.