Chemical Structure : PRN1008
CAS No.: 1575596-29-0
Catalog No.: PC-62583Not For Human Use, Lab Use Only.
Rilzabrutinib (PRN1008) is a potent, selective, covalent reversible BTK inhibitorwith IC50 of 1.3 nM.
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Rilzabrutinib (PRN1008) is a potent, selective, covalent reversible BTK inhibitorwith IC50 of 1.3 nM.
PRN1008 displays highly selectively when tested in a panel of 251 other kinases.
PRN1008 inhibits anti-IgM induces human B cell proliferation (10% serum) and B cell CD69 expression, with IC50s of 5 nM and 123 nM, respectively.
Rilzabrutinib (PRN1008) demonstrates in vivo efficacy in rodent arthritis models, and clinical efficacy in canine pemphigus foliaceus.
Rilzabrutinib (PRN1008) is in phase 3 trials for pemphigus vulgaris and immune thrombocytopenia.
M.Wt | 665.774 | |
Formula | C36H40FN9O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(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 |
1. Smith PF, et al. Br J Clin Pharmacol. 2017 Nov;83(11):2367-2376.
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