Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor ofBtkkinase activity (IC₅₀<0.5 nM,K_inact/K_i=7.69×10⁴M^-1s^-1s) in biochemical assays.

IC50:<0.5 nM (Btk)^[1]

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC₅₀value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC₅₀s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC₅₀of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC₅₀=6 nM) correlated directly with the cellular EC₅₀of Btk kinase inhibition with Spebrutinib (EC₅₀=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].

581.62

C₂₈H₂₈FN₅O₆S

1360053-81-1

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