LCL-161

LCL-161 is a small molecule Smac mimetic that inhibits multiple inhibitor of apoptosis (IAP) family proteins. 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 (Cay-10459) in a mouse Ba/F3-FLT3-ITD-luc+ leukemia xenograft model. It exhibits additive effects with the chemotherapeutic agents doxorubicin (Cay-15007) and cytarabine (Cay-16069). LCL-161 also inhibits growth of nilotinib-resistant leukemia cell lines and exhibits synergy with nilotinib (Cay-10010422) in a Bcr-Abl expressing, 32D.p20-luc+ leukemia mouse xenograft model.Formal Name: N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2S-(methylamino)-propanamide. CAS Number: 1005342-46-0. Synonyms: NVP-LCL161. Molecular Formula: C26H33FN4O3S. Formula Weight: 500.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml. lambdamax: 271 nm. SMILES: O=C(N1CCC[C@H]1C2=NC(C(C3=CC=C(F)C=C3)=O)=CS2)[C@@H](NC([C@@H](NC)C)=O)C4CCCCC4. InChi Code: InChI=1S/C26H33FN4O3S/c1-16(28-2)24(33)30-22(17-7-4-3-5-8-17)26(34)31-14-6-9-21(31)25-29-20(15-35-25)23(32)18-10-12-19(27)13-11-18/h10-13,15-17,21-22,28H,3-9,14H2,1-2H3,(H,30,33)/t16-,21-,22-/m0/s1. InChi Key: UFPFGVNKHCLJJO-SSKFGXFMSA-N.