1242156-23-5

• 常用中文名：RN486
• 常用英文名：RN486
• CAS号：1242156-23-5
• 分子式：C₃₅H₃₅FN₆O₃
• 分子量：606.689
• 相关类别： 生物化工 抑制剂 血管生成(Angiogenesis) BTK 抑制剂
• 发布时间：2016-08-28 09:31:19
• 更新时间：2026-07-08 17:54:05
• RN486是高活性Btk抑制剂,IC50为4.0 nM。

名称

• 中文名: RN486
• 英文名: 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
• 中文别名: 6-环丙基-8-氟-2-(2-(羟甲基)-3-(1-甲基-5-((5-(4-甲基哌嗪-1-基)吡啶-2-基)氨基)-6-氧代-1,6-二氢吡啶-3-基)苯基)异喹啉-1(2H)-酮
• 英文别名: 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; 6-Cyclopropyl-8-fluoro-2-(2-hydroxymethyl-3-{1-methyl-5-[5-(4-methyl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-pyridin-3-yl}-phenyl)-2H-isoquinolin-1-one; RN486 LM-2078; 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; RN486, 10 mM in DMSO; RN 486; RN486; RN-486; RN; 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-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2; RN486/RN-486; 6-Cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-(1-methyl-5-{[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino}-6-oxo-1,6-dihydro-3-pyridinyl)phenyl]-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-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; RN486 TFA Salt; 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; RN468; QCR-5; 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

物化性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 868.6±65.0 °C at 760 mmHg
• 分子式: C₃₅H₃₅FN₆O₃
• 分子量: 606.689
• 闪点: 479.1±34.3 °C
• 精确质量: 606.275452
• PSA: 95.63000
• LogP: 2.95
• 外观性状: 粉末
• 蒸汽压: 0.0±0.3 mmHg at 25°C
• 折射率: 1.696
• 储存条件: -20℃

生物活性

• 描述: RN486是高活性Btk抑制剂,IC50为4.0 nM。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> BTK
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. Xu D, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.

  [2]. Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104.

  [3]. Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91.

安全

• 危害码 (欧洲): N