For research use only. Not for therapeutic Use.
PRN1008（Cat No.:I019888）is an investigational oral drug developed by Principia Biopharma, designed to selectively inhibit Bruton’s tyrosine kinase (BTK), an enzyme involved in immune cell signaling. By targeting BTK, PRN1008 modulates B-cell activity, making it useful in the treatment of autoimmune diseases, where B cells contribute to pathological inflammation. The drug has shown potential in treating conditions such as systemic lupus erythematosus (SLE) and IgG4-related disease. PRN1008 is being studied in clinical trials to evaluate its safety, efficacy, and long-term effects in managing autoimmune disorders with fewer side effects compared to traditional therapies.
| Catalog Number | I019888 |
| CAS Number | 1575596-29-0 |
| Molecular Formula | C₃₆H₄₀FN₉O₃ |
| Purity | ≥95% |
| Target | Btk |
| IUPAC Name | (E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| 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 |
| InChIKey | LCFFREMLXLZNHE-GBOLQPHISA-N |
| SMILES | CC(C)(/C=C(\C#N)/C(=O)N1CCC[C@H](C1)N2C3=NC=NC(=C3C(=N2)C4=C(C=C(C=C4)OC5=CC=CC=C5)F)N)N6CCN(CC6)C7COC7 |
| Reference | [1]. Smith PF, 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 Nov;83(11):2367-2376.<br>[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. |
