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。

Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC 50 of 1.3 nM.

Solid

BTK 1.3 nM (IC50) BMX 1.0 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Smith PF, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Brutons tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017 Nov;83(11):2367-2376.
[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

In Vitro: DMSO : ≥ 130 mg/mL (195.27 mM)配制储备液