Spebrutinib besylate  (Synonyms: AVL-292 benzenesulfonate; CC-292 besylate)

Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC₅₀<0.5 nM, K_inact/K_i=7.69×10⁴ M^-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 IC₅₀ value 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 EC₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC₅₀=6 nM) correlated directly with the cellular EC₅₀ of 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].

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

581.62

C₂₈H₂₈FN₅O₆S

1360053-81-1

COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1.O=S(C4=CC=CC=C4)(O)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.  [Content Brief]