[CAS NO. 1202757-89-8]  Spebrutinib

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC ₅₀ value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC ₅₀ s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC ₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC ₅₀ =6 nM) correlated directly with the cellular EC ₅₀ of Btk kinase inhibition with Spebrutinib (EC ₅₀ =8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM ^[1] .

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