BTK-IN-49 

BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC₅₀ of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis^[1].

BTK-IN-49 (compound 13) inhibits recombinant active BTK enzyme with an IC₅₀ of 0.14 nM and suppresses CD69 expression on human CD19⁺ B-cells in whole blood with an IC₅₀ of 0.23 μM^[1].
BTK-IN-49 inhibits hERG channels with an IC₅₀ of 25 μM, suggesting moderate cardiovascular risk^[1].
BTK-IN-49 (1 μM) shows good kinome selectivity, inhibiting only BTK, KIT, and SRC by > 90% at 1 μM across a panel of 468 kinases^[1].

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

BTK-IN-49 (compound 13) (50-250 mg/kg; p.o.; twice daily; 4-7 days) shows CNS exposures above the human WB anti-CD69 IC₇₀-IC₉₀ correlate with reduced tolerability, with the 50 mg/kg BID dose tolerated for 7 days in healthy C57BL/6 mice^[1].
BTK-IN-49 (5-50 mg/kg; p.o.; every 12 hours; 60 hours) robustly inhibits proliferation of CNS-compartmentalized B-cells in NOD.SCID mice, while peripherally restricted inhibitors show no activity^[1].

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

486.57

C₂₆H₃₀N₈O₂

CC(C)(C)C1=NC(C(N[C@H]2C3=CC=C(C4=CC=NC(NC5=NN(C)C=C5)=N4)C=C3CCCC2)=O)=NO1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Hopkins BT, et al. Leveraging Kinase Drugs for Neurosciences: Discovery of Selective, CNS-Penetrant Reversible Bruton's Tyrosine Kinase Inhibitors as Therapeutics for Neuroinflammation. J Med Chem. Published online April 7, 2026.