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Rilzabrutinib

CAS No. : 1575596-29-0

MCE 国际站：Rilzabrutinib

产品活性：Rilzabrutinib (PRN1008) 是布鲁顿氏酪氨酸激酶 (BTK) 可逆的、选择性的、有口服活性的共价抑制剂，其 IC₅₀ 值为 1.3 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: Rilzabrutinib is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC₅₀ of 1.3±0.5 nM. Rilzabrutinib is also found to be highly selectively when tested in a panel of 251 other kinases. Cysteine targeting of BTK by Rilzabrutinib results in a slow off-rate demonstrated by retention of 79±2% of binding to BTK in PBMC 18 hours after washing away the compound in vitro. The covalent cysteine binding is completely reversible after denaturation of the target. Anti-IgM induces human B cell proliferation (10% serum) and B cell CD69 expression are inhibited by Rilzabrutinib with IC₅₀ of 5±2.4 nM and 123±38 nM, respectively.

In Vivo: In vivo Rilzabrutinib demonstrates enduring pharmacodynamic effects after the compound has cleared from circulation, consistent with extended target residence time. Rilzabrutinib also reverses and completely suppresses collagen-induced arthritis in rats in a dose dependent manner which allows correlation of target occupancy and disease modification.

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