A-1155463

Description	in vitro: A-1155463 represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization. A-1155463 demonstratsstrong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS. in vivo: A-1155463 causes a mechanism-based and reversible thrombocytopenia in mice and inhibits H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses. he ability of A-1155463 to exert in vivo on-target activity was demonstrated through a rapid and reversible reduction in platelets in SCID-Beige mice following a single IP dose. Additionally, administration of A-1155463 to tumor bearing SCID-Beige mice afforded modest but statistically significant tumor growth inhibition. Detailed mechanistic studies of A-1155463 and combination activity with relevant chemotherapy across multiple tumor types will be reported in an accompanying manuscript.
Pathways	Apoptosis Pathway
Targets	Bcl2

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