A-1155463

A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC₅₀ of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target: EC50: 70 nM (BCL-X_L, Molt-4 cell)^[1] In Vitro: A-1155463 shows picomolar binding affinity to BCL-X_L (K_i＜0.01 nM), and >1000-fold weaker binding to BCL-2 (K_i= 80 nM) and related proteins BCL-W (K_i= 19 nM) and MCL-1 (K_i> 440 nM) ^[2]. A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC₅₀ values ≤0.5 μM in the presence of 10 % FBS^[3]. In Vivo: A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses^[2].