RN486

• 常用名: RN486
• 英文名: RN486
• CAS号: 1242156-23-5
• 分子量: 606.689
• 密度: 1.4±0.1 g/cm3
• 沸点: 868.6±65.0 °C at 760 mmHg
• 分子式: C₃₅H₃₅FN₆O₃
• 熔点: N/A
• 闪点: 479.1±34.3 °C

RN486用途

RN486是高活性Btk抑制剂，IC50为4.0 nM。

RN486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

RN486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.

RN486物理化学性质

• 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℃

RN486安全信息

• 危害码 (欧洲): N

RN486靶点实验

查看更多实验

实验名称：Inhibition of anti-IgD antibody stimulated CD69 expression in mouse CIA model dosed p... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL2060655

实验名称：Inhibition of hypersensitive immune responses in rat passive cutaneous anaphylaxis mo... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL2060656

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Selectivity index, ratio of inhibition of SLK to IC50 for BTK 来源：ChEMBL 靶标：N/A External Id：CHEMBL2060653

实验名称：Antiinflammatory activity against collagen-induced arthritis Lewis rat model assessed... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4822483

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：A screen for small molecules that modulate mitochondrial supercomplex formation 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1482

实验名称：qHTS assay to identify novel small-molecules to repurpose for Merkel cell carcinoma t... 来源：NCGC 靶标：N/A External Id：MCC011

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RN486英文别名

• 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
• 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
• RN 486
• QCR-5
• 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
• RN486