Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK).
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名称 | Rilzabrutinib |
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Iupac 化学名称 | (R,E)-2-(3-(4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)-4-methyl-4-(4-(oxetan-3-yl)piperazin-1-yl)pent-2-enenitrile |
同义词 | PRN1008; PRN 1008; PRN-1008; Rilzabrutinib; |
英文同义词 | PRN1008; PRN 1008; PRN-1008; Rilzabrutinib; |
分子式 | C36H40FN9O3 |
分子量 | 665.76 |
Smile | NC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([C@H]5CN(CCC5)C(/C(C#N)=C/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1 |
InChiKey | LCFFREMLXLZNHE-GBOLQPHISA-N |
InChi | InChI=1S/C36H40FN9O3/c1-36(2,45-15-13-43(14-16-45)26-21-48-22-26)18-24(19-38)35(47)44-12-6-7-25(20-44)46-34-31(33(39)40-23-41-34)32(42-46)29-11-10-28(17-30(29)37)49-27-8-4-3-5-9-27/h3-5,8-11,17-18,23,25-26H,6-7,12-16,20-22H2,1-2H3,(H2,39,40,41)/b24-18+/t25-/m1/s1 |
Cas号 | 1575596-29-0 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 类白色固体 |
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纯度 | 98% Min. |
存储 | 0-4℃,可保存几天到几周;-20℃,可保存 几个月。 |
可溶性 | 溶于DMSO等有机溶剂 |
处理方式 | |
运输条件 | 可以在室温下进行运输。 |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Smith PF, Krishnarajah J, Nunn PA, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017;83(11):2367-2376. doi:10.1111/bcp.13351
2: Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74(Suppl 2): 216.