AVL-292

AVL-292 (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM; also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 uM, 2.43 uM, 4.4 uM, and 7.15 uM, rspectively; shows anti-inflammatory activity in the collagen-induced arthritis model of autoimmune disease; also prevents NRG- and EGF-dependent growth factor-driven resistance to lapatinib in HER2 (+) breast cancer cells.Rheumatoid Arthritis Phase 2 Clinical. (In Vitro) :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.

1202757-89-8

Spebrutinib | CC-292

>98% (HPLC)

DMSO: ≥ 45 mg/mL

C=CC (NC1=CC=CC (NC2=NC (NC3=CC=C (OCCOC) C=C3) =NC=C2F) =C1) =O

C22H22FN5O3

423.4402

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.