BTK-IN-17 

BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC₅₀ value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK^Y223 and p-PLCγ2^Y1217. BTK-IN-17 shows anti-inflammatory effects^[1].

IC₅₀: 13.7 nM (BTK)^[1]

BTK-IN-17 (compound 36R) shows hERG channel inhibition with an IC₅₀ value of 8.6 µM^[1].
BTK-IN-17 (0-10000 nM) decreases the expression of p-BTK^Y223 and p-PLCγ2^Y1217 in Ramos cells^[1].

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

BTK-IN-17 (1 mg/kg for i.v.; 10 mg/kg for p.o.) shows the plasma concentrations rapidly reached 125 nM and BTK occupancy reached 79%one hour after oral administration, target occupancy of roughly 62% was maintained after 24 h in rats^[1].
BTK-IN-17 (10, 30, 50 mg/kg; p.o.; once daily for 10 days) shows good anti-inflammatory effects in rats^[1].
Pharmacokinetic Parameters of BTK-IN-17 in Male Sprague-Dawley rats^[1].

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

465.51

C₂₆H₂₃N₇O₂

C=CC(N1CC[C@H](C1)N2N=C(C3=CNC4=NC=NC2=C34)NC5=CC=C(C=C5)OC6=CC=CC=C6)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Fang X, et al. Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis. Eur J Med Chem. 2022 Nov 25;246:114940.  [Content Brief]