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      LCL161
      LCL161

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      This product is for research use only, not for human use. We do not sell to patients.
      Number： - + Pieces（InventoryPieces）
      InvivoChem Cat #: V0056
      CAS #: 1005342-46-0Purity ≥98%

      Description: LCL161 (LCL-161) is a novel and potent SMAC (second mitochondrial-derived activator of caspases) mimetic agent with potential anticancer activity, acting by potently binding to and inhibiting multiple IAP (inhibitor of apoptosis) proteins such as XIAP and c-IAP. It inhibits XIAP in HEK293 cells and cIAP1 in MDA-MB-231 cells with IC50s of 35 and 0.4 nM, respectively. LCL161 showed anti proliferative activities in two human hepatocellular carcinoma (HCC) cells, Hep3B and PLC5 with IC50 values of 10 and 19 μM, respectively. 

      References: Biochem Pharmacol. 2012 Aug 1;84(3):268-77; Pediatr Blood Cancer. 2012 Apr;58(4):636-9. 


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      Molecular Weight (MW)500.63
      FormulaC26H33FN4O3S
      CAS No.1005342-46-0
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: Soluble in DMSO > 10 mM
      Water: <1 mg/mL (slightly soluble or insoluble)
      Ethanol: 20 mg/mL warming (39.94 mM)
      Other info

      Synonym: LCL161; LCL 161; LCL-161

      Chemical Name: (S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(methylamino)propanamide

      InChi Key: UFPFGVNKHCLJJO-SSKFGXFMSA-N

      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

      SMILES Code: C[[email protected]](NC)C(N[[email protected]@H](C1CCCCC1)C(N2[[email protected]](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O

      Chemical Name(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide


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      In VitroLCL161 binds to inhibitors of apoptosis proteins (IAPs) with high affinity and initiates the destruction of cIAP1 and cIAP2, which further induces apoptosis via caspase activation. LCL161 modestly inhibits the growth of FLT3-ITD-expressing cells when administered alone, with an IC50 ranging from ~0.5 μM (Ba/F3-FLT3-ITD cells) to ~4 μM (MOLM13-luc+ cells).
      In VivoLCL161 significantly enhances the ability of PKC412 to inhibit the growth of Ba/F3-FLT3-ITD-luc+ cells in vivo. LCL161 is also shown to positively combine with the standard chemotherapeutic agents, Ara-c and doxorubicin, against FLT3-ITD-expressing cells and against D835Y-expressing cells. 
      Animal modelHuh-7 xeonograft nude mice
      Formulation & Dosage50 mg/kg; p.o.; q.d., for 20 days
      ReferencesBiochemical pharmacology, 2012, 84(3): 268-277.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      LCL161

      Weisberg E, et al. Leukemia, 2010, 24(12), 2100-2109.
      		 

      LCL161

      Effects of IAP inhibitor treatment and FLT3 inhibition, alone and combined, on the growth of mutant FLT3-expressing cells in vivo
      		 
      LCL161
      Effects of IAP inhibitor treatment and Abl inhibition, alone and combined, on the growth of BCR-ABL-expressing cells in vitro and in vivo

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