LCL161

Catalog No.S7009

For research use only.

LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

LCL161 Chemical Structure

CAS No. 1005342-46-0

Selleck's LCL161 has been cited by 25 publications

Purity & Quality Control

Choose Selective IAP Inhibitors

Biological Activity

Description LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).
Targets
cIAP [1] XIAP [1]
In vitro

LCL161 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). The potency of LCL161 against the D835Y mutant is observed to be considerably higher, with an IC50 of ~50 nM when tested against Ba/F3-D835Y cells. Treatment of MOLM13-luc+ cells with a combination of LCL161 and PKC412 leads to significantly more killing of cells than either agent alone, with Calcusyn combination indices suggestive of synergy. PKC412 and LCL161 induces apoptosis of MOLM13-luc+ cells. The combination of PKC412 and LCL161 leads to a higher induction of apoptosis than either agent alone. LCL161 is able to override stromal-mediated rescue of mutant FLT3-expressing cells through positive combination with PKC412. LCL161 inhibits the growth of Ba/F3.p210 cells with an IC50 of ~100 nM. The combination of LCL161 and the ABL inhibitor, imatinib, is observed to be synergistic against BCR-ABL-expressing cells. LCL161 also has demonstrated activity against drug-resistant cells expressing point mutations in the target proteins. LCL161 at 1000 nM is able to mostly or completely kill Ba/F3-derived cell lines conferring resistance to PKC412, which express FLT3-ITD harboring point mutations in the ATP-binding pocket of FLT3. LCL161 also shows activity at concentrations ranging from 100 to 1000 nM against Ba/F3 cells expressing various imatinib- and nilotinib-resistant BCR-ABL point mutations. [1] LCL161 is evaluated against the 23 cell lines in the Pediatric Preclinical Testing Program (PPTP) in vitro panel using 96 hr. LCL161 achieves 50% growth inhibition against only 3 of the 23 tested PPTP cell lines under concentration of 10 μM. The three cell lines includes two T-cell ALL cell lines (COG-LL-317 and CCRF-CEM) and an anaplastic large cell lymphoma cell line (Karpas-299), with CCRF-CEM and Karpas-299 showing the lowest relative IC50 values (0.25 and 1.6 μM, respectively). [2] LCL161shows immunomodulatory properties on human immune subsets. T lymphocytes treated with LCL161 demonstrates significantly enhanced cytokine secretion upon activation, with little effect on CD4 and CD8 T-cell survival or proliferation. LCL161 treatment of peripheral blood mononuclear cells significantly enhances priming of naïve T cells with synthetic peptides in vitro. Myeloid dendritic cells undergoes phenotypic maturation upon LCL161 and demonstrates a reduced capacity to cross-present a tumor antigen-based vaccine. These effects are potentially mediated through an observed activation of the canonical and non-canonical NF-κB pathways, following LCL161 with a resulting upregulation of anti-apoptotic molecules. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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H460 NIHie3JHfW6ldHnvckBie3OjeR?= NFTHUYg{NjNidV2= M176N|Uh\GG7cx?= Ml\nVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZ5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFQ3OCClZXzsd{BifCB|LkOgeW0h[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfS=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB6M{e4Nkc,OjRyOEO3PFI9N2F-
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SW620 Moi0SpVv[3Srb36gZZN{[Xl? MXe1JIRigXN? NUXSOYdjUW6mdXP0bY9vKG:oIIPlcpNqfGm8YYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdHNidH:gZ49v[XS3bYXtZYIucW6mdXPl[EBieG:ydH;zbZMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfUwhTUN7MDC9JFYvPjZizszNMi=> NH3jOVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
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LOX MkfTSpVv[3Srb36gZZN{[Xl? MXKxNFAhdWdxa3e= Mn3mPEBpenN? MXrJckB3cX[xIHnubIljcXSrb36gc4YhYEmDUDDCTXIzKGSxbXHpckBqdiCqdX3hckBNV1hiY3XscJMhgGWwb3fyZYZ1\WRiaX6gcpVl\SCvb4Xz[UBie3Onc4Pl[EBieyCyb4TlcpRq[XSrb36gc4Yh[2:wYYT1cZVu[WJvaX7keYNm\CClYYPwZZNmKDNxNzDhZ5Rqfmm2eTDheEAyODBibXevb4ctKHCxIHHmeIVzKDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NV[zWpozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
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MDA-MB-231 NIDmWZdHfW6ldHnvckBie3OjeR?= NXrKNGNmOC5|NzD0c{A{NjNidV2= MnrJNVkhcHK| NGTQZ5dKdmirYnn0bY9vKG:oIHPJRXAyNzJiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDpcoR2[3Srb36gc4YhXE6IYXzwbIEhdGW4ZXygZZQhOC5|NzD0c{A{NjNidV2gZYZ1\XJiMUmgbJJ{KGK7IFXMTXNC NFHkSIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5N|k1OCd-MkSwPVM6PDB:L3G+
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SKMES1 M4XaTmZ2dmO2aX;uJIF{e2G7 MY[yMlUhfU1? M4r1flUh\GG7cx?= MmTKVI91\W62aXH0bY9vKG:oIHPvcoF1fW23bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGi3bXHuJHNMVUWVMTDj[YxteyCjdDCyMlUhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2WUzDhd5NigQ>? NVSxUXdpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVM6PDBpPkK0NFk{QTRyPD;hQi=>
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CCRF-CEM M1fBOWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mkm2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQ2LGMWNGVSClZXzsd{whT0l3MDC9JFAvOjVizszNMi=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|NUWyOkc,Ojh2M{W1NlY9N2F-
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HEK293 NVLscGh3TnWwY4Tpc44h[XO|YYm= MXGyJIhzew>? MXfJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIF\MRWcufGGpZ3XkJHhKSVBiKIXub45wf25ib4Lp[4lvMSCrboTldoFkfGmxbjD3bZRpKG[3bHygcIVv\3SqIIXueIFo\2WmIHPhd5Bie2VvOTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHmeIVzKDJiaILzJIJ6KGmvbYXuc5Bz\WOrcHn0ZZRqd25iYYPzZZktKEWFNUCgQUAxNjB|NTFOwG0v Mn\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2OUKzNVcoRjJ6NEmyN|E4RC:jPh?=
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MDA-MB-231 MmP1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MoK2O|IhcHK| M3rFV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA4OiCqcoOgZpkhSWyjbXHyJIJtfWViYYPzZZktKEmFNUCgQUAxNjByN{ig{txONg>? NX;HWlc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwPVE3ODBpPkOwNFkyPjByPD;hQi=>
HEK293 MmTMSpVv[3Srb36gZZN{[Xl? NEjKZokzKGi{cx?= NFHqPWpKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJGZNSUdvdHHn[4VlKFiLQWCgLJVvc26xd36gc5Jq\2mwKTDpcpRmemGldHnvckB4cXSqIH\1cIwhdGWwZ4ToJJVvfGGpZ3XkJINie3Cjc3WtPUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IEKgbJJ{KGK7IHntcZVvd3C{ZXPpdIl1[XSrb36gZZN{[XluIFnDOVAhRSByLkCzOUDPxE1w MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB7MU[wNEc,OzByOUG2NFA9N2F-
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A549 NY\s[4xmTnWwY4Tpc44h[XO|YYm= MV2xJJVO MXmzJIhzew>? NV\mPI14UW6mdXP0bY9vKG:oIHPJRXAzKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPJRXAzKHC{b4TlbY4hdGW4ZXygZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDNiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= Mk\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NUCxOVUoRjNzNUWwNVU2RC:jPh?=
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HEK293T NWT5NWRXTnWwY4Tpc44h[XO|YYm= NF;zeWkyOCC3TR?= NIj3OGU3KGi{cx?= MX;Dc5ZidGWwdDDibY5lcW6pIHHm[olvcXS7IITvJGhCNUKLUkOg[I9u[WmwIH;mJHhKSVBiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|VDDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBj[W6mIHnueIVve2m2eTDheEAyOCC3TTDpcoN2[mG2ZXSg[o9zKDZiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MnvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3NUCxOVUoRjNzNUWwNVU2RC:jPh?=
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Assay
Methods Test Index PMID
Western blot cIAP1 / cIAP2 / XIAP / surivivin 27737687
Growth inhibition assay Cell viability 27737687
In vivo LCL161 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. There is an additive effect achieved by combining both Nilotinib and LCL161 in suppressing leukemia growth. LCL161 (100 mg/kg) enhances in vivo effects of high-moderate doses of nilotinib (100 mg/kg) on leukemia burden in mice. [1] CL161 is tested against the Pediatric Preclinical Testing Program (PPTP) in vivo panels (30 or 75 mg/kg [solid tumors] or 100 mg/kg [ALL]) administered orally twice in a week. LCL161 induces significant differences in EFS distribution in approximately one-third of solid tumor xenografts (osteosarcoma and glioblastoma), but not in ALL xenografts. No objective tumor responses are observed. In vivo LCL161 demonstrates limited single agent activity against the pediatric preclinical models studied. [2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Human T-cell ALL cell lines COG-LL-317
  • Concentrations: ~10 μM
  • Incubation Time: 96 hours
  • Method:

    In vitro testing is performed using DIMSCAN

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(199.74 mM)
Water Insoluble
Ethanol '20 mg/mL warmed

Chemical Information

Molecular Weight 500.63
Formula

C26H33FN4O3S

CAS No. 1005342-46-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(=O)NC(C1CCCCC1)C(=O)N2CCCC2C3=NC(=CS3)C(=O)C4=CC=C(C=C4)F)NC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03111992 Completed Drug: PDR001|Drug: CJM112|Drug: LCL161 Multiple Myeloma Novartis Pharmaceuticals|Novartis December 18 2017 Phase 1
NCT01934634 Unknown status Drug: LCL161|Drug: Gemcitabine|Drug: nab-Paclitaxel Metastatic Pancreatic Cancer US Oncology Research|Novartis Pharmaceuticals|Delta Clinical Research LLC March 2014 Phase 1
NCT01968915 Completed Drug: LCL161|Drug: Paclitaxel Neoplasms Novartis Pharmaceuticals|Novartis November 2013 Phase 1
NCT01617668 Completed Drug: LCL161|Drug: paclitaxel Breast Cancer Novartis Pharmaceuticals|Novartis August 2012 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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