Information Remibrutinib (LOU064) Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. Targets BTK (Cell-free assay); IL-8 (Cell-free assay); CD69 (Cell-free assay) 1.3 nM; 2.5 nM; 18 nM In vitro LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. In vivo LOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. Cell Research(from reference) Cell lines：human monocytic cell line THP1, Human Blood B cell and Basophil. Concentrations：3 nM, 10 nM, 30 nM, 100 nM, 300 nM Incubation Time：25 min, 50 min, 75 min, 100 min
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Remibrutinib (LOU064)
Dangerous GoodsCAS number：1787294-07-8 molecular formula：C27H27F2N5O3
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compound introduction
Specs
| Chinese alias | 瑞布替尼 (LOU064) | ||
| English alias | Remibrutinib (LOU064) | GTPL10457 | N-(3-(6-Amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide | N-[3-[6-Amino-5-[2-[methyl(1-oxo-2-propen-1-yl)amino]ethoxy]-4-pyrimidinyl]-5-fluoro-2-methylpheny | ||
| CAS number | 1787294-07-8 | molecular formula | C27H27F2N5O3 |
| molecular weight | 507.53 g/mol | Exact mass | - |
| PSA | 110.000 Ų | logp | 4.374 |
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Safety information
pictogram：
GHS08 , GHS07
Signal word：
Danger
Hazard Statement：
H317: 可能引起皮肤过敏反应 H334: 吸入可能引起过敏或哮喘病症状或呼吸困难
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P342+P311: 如有呼吸系统病症：呼叫急救中心/医生。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P501: 将内容物/容器处理到。。。 P363: 再次使用之前，请清洗受污染的衣物。 P272: 被污染的工作服不允许离开工作场所 P333+P313: 如发生皮肤刺激或皮疹：求医/就诊。 P285: 如果通风不良，请佩戴呼吸防护装
UN Number：
2811
Packing Group：
III
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