BTK inhibitor 18 

BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC₅₀ of 142 nM. BTK inhibitor 18 has anti-inflammatory activities^[1].

IC50: 142 nM (Btk)^[1]

BTK inhibitor 18 (Compound 27) irreversibly inhibits BTK by targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation^[1].
BTK inhibitor 18 (Compound 27) inhibits anti-IgM-induced activation of B cells in human whole blood with an IC₅₀ of 84 nM^[1].
BTK inhibitor 18 (Compound 27) also inhibits BMX, LCK, ErbB4, TEC, and TXK kinases with IC₅₀ values of 129 nM, 130 nM, 377 nM, 409 nM, 1770 nM, respectively^[1].

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

BTK inhibitor 18 (Compound 27; 1-30 mg/kg; oral administration; once a day; for 7 days) treatment shows dose-dependent efficacy at reducing joint inflammation in a rat collagen-induced arthritis model^[1].
The IV and PO pharmacokinetics of BTK inhibitor 18 (Compound 27) are investigated in nonfasted rats (1 and 5 mg/kg IV and PO) and fasted dogs (0.5 and 2.5 mg/kg IV and PO). IV pharmacokinetics are characterized by moderate clearance in rat and low clearance in dog, a moderate volume of distribution, and a short plasma half-life across both species (T_1/2 of 0.3 h and 1.9 h for rat and dog, respectively). The oral bioavailability is 30% and 68% in rat and dog, respectively^[1].

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

571.67

C₂₉H₂₅N₅O₄S₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mark S Tichenor, et al. Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity. ACS Med Chem Lett. 2021 Apr 5;12(5):782-790.  [Content Brief]