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LCL-161 is a small molecule Smac mimetic that inhibits multiple inhibitor of apoptosis (IAP) family proteins.1 As a single agent, LCL-161 inhibits growth of FLT3-ITD-expressing leukemia cells via induction of apoptosis with IC50 values ranging from 0.5-4 μM. In vivo, LCL-161 enhances growth inhibition driven by PKC 412 (Item No. 10459) in a mouse Ba/F3-FLT3-ITD-luc+ leukemia xenograft model. It exhibits additive effects with the chemotherapeutic agents doxorubicin (Item No. 15007) and cytarabine (Item No. 16069). LCL-161 also inhibits growth of nilotinib-resistant leukemia cell lines and exhibits synergy with nilotinib (Item No. 10010422) in a Bcr-Abl expressing, 32D.p20-luc+ leukemia mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. Smac mimetics: Implications for enhancement of targeted therapies in leukemia. Leukemia 24(12), 2100-2109 (2010).