Art. -Nr.: HY-15518

LCL161

44 Cited Publications

Kundenbewertung

Based on 44 publication(s) in Google Scholar

LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC₅₀s of 35 and 0.4 nM, respectively.

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Reinheit: 99.91%
CAS. Nr.: 1005342-46-0
Formel: C₂₆H₃₃FN₄O₃S
Molecular Weight:500.63

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LCL161 Chemical Structure

CAS. Nr.: 1005342-46-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (44)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC₅₀s of 35 and 0.4 nM, respectively.

IC₅₀ & Target

IC50: 35 nM (XIAP, in HEK293 cell), 0.40 nM (cIAP1, in MDA-MB-231)^[1]

Alle IAP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	GI₅₀	250 nM Compound: LCL-161	Antiproliferative activity against human CCRF-CEM cells Antiproliferative activity against human CCRF-CEM cells	[PMID: 28435526]
MDA-MB-231	EC₅₀	32.5 nM Compound: LCL161	Cytotoxicity against human MDA-MB-231 cells cultured as 3D spheroids incubated for 6 days and measured every 6 hrs by IncuCyte live-cell analysis Cytotoxicity against human MDA-MB-231 cells cultured as 3D spheroids incubated for 6 days and measured every 6 hrs by IncuCyte live-cell analysis	[PMID: 37262387]
MDA-MB-231	EC₅₀	37 nM Compound: LCL161	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell imaging analysis Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell imaging analysis	[PMID: 37262387]
MDA-MB-231	EC₅₀	57 nM Compound: LCL161	Induction of apoptosis in human MDA-MB-231 cells Induction of apoptosis in human MDA-MB-231 cells	[PMID: 37262387]
MDA-MB-231	EC₅₀	7.8 nM Compound: 2; LCL-161	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 72 hrs by alamar blue assay Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 72 hrs by alamar blue assay	[PMID: 28492317]
MDA-MB-231	IC₅₀	7.8 nM Compound: 2; LCL-161	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay	[PMID: 30091600]
SK-OV-3	EC₅₀	1 nM Compound: LCL161	Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 48 hrs by IncuCyte S3 live-cell analysis Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 48 hrs by IncuCyte S3 live-cell analysis	[PMID: 31095386]
SK-OV-3	EC₅₀	3 nM Compound: LCL161	Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 24 hrs by IncuCyte S3 live-cell analysis Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 24 hrs by IncuCyte S3 live-cell analysis	[PMID: 31095386]

In Vitro

LCL161 shows anti-proliferative effects and reduces cell viability significantly in Hep3B (IC₅₀=10.23 μM) and PLC5 (IC₅₀=19.19 μM) cells in a dose-dependent manner. LCL161 induces apoptosis significantly in both the sensitive cell lines in a dose-dependent manner. LCL161 significantly down regulates the expression of cIAP1, starting at very low concentrations. LCL161 at low concentrations inhibits cIAP1 starting at the concentration of 0.5 nM^[2]. LCL161 is a small molecule oral IAP antagonist in development for use in combination with cytotoxic agents. The effect of LCL161 on CYP3A4/5 (CYP3A) activity is investigated in vitro. Results in human liver microsomes indicated LCL161 inhibited CYP3A in a concentration- and time-dependent manner (K_I of 0.797 μM and K_inact of 0.0803 min^-1). LCL161 activates human PXR in a reporter gene assay and induced CYP3A4 mRNA up to ~5-fold in human hepatocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tumor-bearing mice are treated with vehicle or LCL161 p.o. at a dose of 50 mg/kg/day, or SC-2001 p.o. at a dose of 10 mg/kg/day, 5 days a week, or in combination for the duration of the study. Tumor growth is significantly inhibited by co-treatment with SC2001 and LCL161 and tumor size in the co-treatment group is only one third of that of the control group at the end of the study^[2]. LCL161 is a first-in-class oral Smac mimetic shown to induce degradation of cIAP1 and cleavage of caspase 3 in mouse xenograft models^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1005342-46-0
Appearance Solid
Molecular Weight 500.63
Formel C₂₆H₃₃FN₄O₃S
Color White to yellow
SMILES

C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (44)

All Cell Proliferation/Viability AssayFlow CytometryWBIn Vivo Efficacy StudyIHC

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Journal Impact Factor

Cell Res

HSPA8 acts as an amyloidase to suppress necroptosis by inhibiting and reversing functional amyloid formation. [Abstract]

2023 Nov;33(11):851-866. PMID: 37580406
Immunity

Macrophage and neutrophil death programs differentially confer resistance to tuberculosis. [Abstract]

2021 Aug 10;54(8):1758-1771.e7. PMID: 34256013

LCL161 purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Aug 10;54(8):1758-1771.e7. [Abstract]

LCL161 (10 μM; 72 h) promoted killing of WT BMDMs infected with M. tuberculosis. BMDMs were infected with M. tuberculosis (MOI 1), and death (as percentage of total cells) was assessed by Annexin-V/DRAQ7 imaging.

LCL161 purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Aug 10;54(8):1758-1771.e7. [Abstract]

LCL161 and birinapant were able to penetrate the lungs of mice and diminish cIAP1 protein in lung-resident immune cells, priming them for death receptor-induced apoptosis. Western blot of cIAP1 expression in alveolar macrophages isolated from mice 6–8 h after treatment with 1 dose of LCL161 (100 mg/kg; po) or birinapant (30 mg/kg) in C57BL/6 mice.

LCL161 purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Aug 10;54(8):1758-1771.e7. [Abstract]

LCL161 showed greater efficacy in reducing lung bacterial numbers (65% reduction versus 44%) and also showed efficacy in the spleen, reducing bacterial numbers at least 6-fold. Bacterial numbers in the lungs and spleens of mice treated with LCL161 (100 mg/kg daily; po)for 3 weeks in C57BL/6 mice, beginning 4 w.p.i. Mice were euthanized 24 h after the final dose.

LCL161 purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Aug 10;54(8):1758-1771.e7. [Abstract]

LCL161 reduced F4/80+ macrophage populations in the lung sections of mice. Bacterial numbers in the lungs and spleens of mice treated with LCL161 (100 mg/kg daily; po)for 3 weeks in C57BL/6 mice, beginning 4 w.p.i. Mice were euthanized 24 h after the final dose.
Adv Mater

Dual Immunostimulatory Pathway Agonism through a Synthetic Nanocarrier Triggers Robust Anti-Tumor Immunity in Murine Glioblastoma. [Abstract]

2023 Feb;35(7):e2208782. PMID: 36427266
Nat Biomed Eng

Targeting immunosuppressive myeloid cells via implant-mediated slow release of small molecules to prevent glioblastoma recurrence. [Abstract]

2025 Oct 22. PMID: 41125869
Cell Mol Immunol

Mapping the holonomic signaling network that drives pathological changes in endotoxic shock. [Abstract]

2026 Jul;23(7):873-885. PMID: 42174141
Nat Commun

EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death. [Abstract]

2024 Feb 12;15(1):1282. PMID: 38346956

LCL161 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 12;15(1):1282. [Abstract]

TNF and LCL-161 (TS; TNF 20 ng/mL; LCL161 5 μM; 8 h) resulted in a significantly higher proportion of annexin V₊PI_- cells in the knockdown of EFHD2 HT-29 cells. Representative flow cytometric analysis of the cell apoptosis from WT and EFHD2_-/- HT-29 cells treated with TC or LCL161 (TS; 5 μM; 8 h) for the indicated time and quantification of proportions of annexin V₊PI_- apoptotic cells.

LCL161 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 12;15(1):1282. [Abstract]

TNF and LCL-161 (TS; TNF 20 ng/mL; LCL161 5 μM; 8 h) enhanced caspase-3/7 activity more than in controls. Representative flow cytometric analysis of caspase-3/7 activity from WT and EFHD2_-/- HT-29 cells.

LCL161 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 12;15(1):1282. [Abstract]

Western blot analysis of lysates from WT and EFHD2-/- HT-29 cells treated with TNF and LCL-161 (TS; TNF 20 ng/mL; LCL161 5 μM; 8 h) and zVAD-fmk for the indicated time. Quantifications of p-RIPK1, p-MLKL, and cleaved-caspase-7 are shown below. Western blot analysis and quantifications of p-IKKα/β and p-P65 in lysates from WT and EFHD2-/- HCT-116 cells treated with TNF for the indicated time.
Nat Commun

Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis. [Abstract]

2023 Oct 30;14(1):6908. PMID: 37903763
ACS Nano

A Myeloid Cell-Targeted Immunostimulant Cocktail (MyTai) Enhances Cancer Immunotherapy. [Abstract]

2025 Oct 21;19(41):36451-36464. PMID: 41061756
J Am Chem Soc

Fluorinated Ribonucleocarbohydrate Nanoparticles Allow Ultraefficient mRNA Delivery and Protein Expression in Tumor-Associated Myeloid Cells. [Abstract]

2025 Mar 26. PMID: 40135499
Mol Cell

MLKL activity requires a splicing-regulated, druggable intramolecular interaction. [Abstract]

2025 Apr 3:S1097-2765(25)00259-X. PMID: 40209701
Theranostics

A non-lipid nucleic acid delivery vector with dendritic cell tropism and stimulation. [Abstract]

2024 May 5;14(7):2934-2945. PMID: 38773971
Theranostics

Tackling regulated cell death yields enhanced protection in lung grafts. [Abstract]

2023 Jul 31;13(13):4376-4390. PMID: 37649611
Cell Death Differ

RIPK3 sequentially recruits MLKL and RIPK1 to induce PANoptosis and chemokine production. [Abstract]

2026 Apr 4. PMID: 41935203
Cell Death Differ

Bcl-3 promotes TNF-induced hepatocyte apoptosis by regulating the deubiquitination of RIP1. [Abstract]

2022 Jun;29(6):1176-1186. PMID: 34853447
Cell Death Differ

Membrane-bound TNF mediates microtubule-targeting chemotherapeutics-induced cancer cytolysis via juxtacrine inter-cancer-cell death signaling. [Abstract]

2020 May;27(5):1569-1587. PMID: 31645676
Cell Death Dis

Clinical stage drugs targeting inhibitor of apoptosis proteins purge episomal Hepatitis B viral genome in preclinical models. [Abstract]

2021 Jun 23;12(7):641. PMID: 34162831
Pharmacol Res

CCL22 signaling contributes to sorafenib resistance in hepatitis B virus-associated hepatocellular carcinoma. [Abstract]

2020 Jul;157:104800. PMID: 32278046
Cell Death Dis

Reversal of CYLD phosphorylation as a novel therapeutic approach for adult T-cell leukemia/lymphoma (ATLL). [Abstract]

2020 Feb 5;11(2):94. PMID: 32024820
Dev Cell

Sensing plasma membrane pore formation induces chemokine production in survivors of regulated necrosis. [Abstract]

2022 Jan 24;57(2):228-245.e6. PMID: 35016014
Leukemia

BET inhibitor-based combinations targeting novel dependencies in MECOM-rearranged (r) AML. [Abstract]

2025 Dec 19. PMID: 41419608
Cell Rep

ISG15 negatively regulates RIPK3-mediated cell death and viral pathogenesis. [Abstract]

2026 May 26;45(5):117360. PMID: 42139056
J Med Chem

Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist. [Abstract]

2023 Jun 22;66(12):8159-8169. PMID: 37262387
J Med Chem

Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein. [Abstract]

2021 Nov 11;64(21):16147-16158. PMID: 34705456
J Med Chem

Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy. [Abstract]

2019 Oct 24;62(20):9188-9200. PMID: 31550155
J Med Chem

Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues. [Abstract]

2019 Jun 13;62(11):5616-5627. PMID: 31095386
J Med Chem

Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach. [Abstract]

2018 Jul 26;61(14):6350-6363. PMID: 29940121

LCL161 purchased from MedChemExpress. Usage Cited in: J Med Chem. 2018 Jul 26;61(14):6350-6363. [Abstract]

IAP inhibitors induce degradation of IAP protein levels. MOLT4 cells are treated for 3 hr with 1 μM and propped for XIAP, cIAP1 or cIAP2. The β-actin blot is detected to ensure equal sample loading.
Eur J Pharmacol

VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]

2025 Sep 15:1003:177942. PMID: 40651787
Int Immunopharmacol

Luteolin mitigates inflammatory organ injury by targeting XIAP to block PANoptosis and mitochondrial dysfunction. [Abstract]

2026 Mar 15:173:116271. PMID: 41637826
Int J Mol Sci

Gasdermin D Cleavage and Cytokine Release, Indicative of Pyroptotic Cell Death, Induced by Ophiobolin A in Breast Cancer Cell Lines. [Abstract]

2026 Jan 7;27(2):618. PMID: 41596270
Int J Mol Sci

Quaternary Benzophenanthridine Alkaloids Act as Smac Mimetics and Overcome Resistance to Apoptosis. [Abstract]

2023 Oct 20;24(20):15405. PMID: 37895085
Exp Mol Pathol

The combination of TRAIL and the Smac mimetic LCL-161 induces an irreversible phenotypic change of MCF-7 breast cancer cells. [Abstract]

2022 Apr:125:104739. PMID: 35007560
Am J Cancer Res

Novel mutations in BRCA2 intron 11 and overexpression of COX-2 and BIRC3 mediate cellular resistance to PARP inhibitors. [Abstract]

2020 Sep 1;10(9):2813-2831. PMID: 33042619
PLoS One

Induction of interferon-β and interferon signaling by TRAIL and Smac mimetics via caspase-8 in breast cancer cells. [Abstract]

2021 Mar 26;16(3):e0248175. PMID: 33770100
Anticancer Agents Med Chem

Proteomic Level Changes on Treatment in MCF-7/DDP Breast Cancer Drug- Resistant Cells. [Abstract]

2020;20(6):687-699. PMID: 32053082
bioRxiv

2026 Jan 20.
Patent

US20250127813A1.
bioRxiv

Antigenic cancer persister cells survive direct T cell attack. [Abstract]

2025 Mar 17:2025.03.14.643359. PMID: 40166148
bioRxiv

SMAC mimetics induce human macrophages to phagocytose live cancer cells. [Abstract]

2024 Nov 28:2024.11.25.625306. PMID: 39651304
Harvard University

2024 May.
University of Portland

2022.
World J Clin Cases

SMAC exhibits anti-tumor effects in ECA109 cells by regulating expression of inhibitor of apoptosis protein family. [Abstract]

2021 Jul 6;9(19):5019-5027. PMID: 34307552
University of Melbourne

2020 Sep.
für das Fach der Zahn-, Mund- und Kieferheilkunde an der Medizinischen Fakultät der Julius-Maximilians

2020 Sep.
bioRxiv

May 2, 2018.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (199.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9975 mL

9.9874 mL

19.9748 mL

5 mM

0.3995 mL

1.9975 mL

3.9950 mL

10 mM

0.1997 mL

0.9987 mL

1.9975 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.99 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[3]

Cells are plated (3×10⁴ viable cells/well) in 96-well clear bottom white plates and the plates are incubated for ~24 hours at 37°C (5% CO₂/95% air) in a humidified incubator. The cells (six replicate wells) are then treated with various concentrations (0.5, 1, 2.5, 5, 10, 25, or 50 µM) of LCL161, or vehicle control (0.1% DMSO, final concentration) for 24 hours in Puracyp dosing media. After the incubation period, the cells are washed with PBS, lysed and the luciferase substrate is added according to the vendor instructions. An aliquot of each well is transferred to the identical wells of black 96-well plates. The luminescence of each well is measured with a TopCount NXT Microplate Scintillation and Luminescence Counter. Cell viability is measured in separate plates treated identically to the PXR-reporter gene assay plates by measurement of ATP content of the cells using the CellTiter-Glo^® Luminescent Cell Viability Assay kit. Cell viability is >80% for all treatments^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]^[4]

Mice^[2]
Male NCr athymic nude mice (5-7 weeks of age) are used. Each mouse is inoculated s.c. in the dorsal flank with 1×10⁶ Huh-7 cells suspended in 0.1 mL of serum-free medium containing 50% Matrigel. When tumors reach 200-300 mm³, mice receives LCL161 (50 mg/kg) or SC-2001 (10 mg/kg) p.o., or a combination of LCL161 and SC-2001, once daily. Controls receive vehicle. Tumors are measured weekly using calipers and their volumes calculated using the following standard formula: width²×length×0.52. LCL161 is a first-in-class oral Smac mimetic shown to induce degradation of cIAP1 and cleavage of caspase 3 in mouse xenograft models .
Rats^[4]
LCL161 is administered orally, once weekly in 21-day cycles, at a starting dose of 10 mg (calculated by using one tenth of the dose that caused severe toxicity in 10% of rats and converted to a human-equivalent dose). In the MDA-MB-231 triple-negative breast cancer xenograft model, once-weekly and twice-daily LCL161 dosing are similarly efficacious. Once weekly is better tolerated, with reduced weight loss.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Maria Ahn, et al. Potent, Dual cIAP1/XIAP Antagonists Induce Apoptosis in a Melanoma Stem Cell Population.

[2]. Chen KF, et al. Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells. Biochem Pharmacol. 2012 Aug 1;84(3):268-77. [Content Brief]

[3]. Dhuria S, et al. Time-dependent inhibition and induction of human cytochrome P4503A4/5 by an oral IAP antagonist, LCL161, in vitro and in vivo in healthy subjects. J Clin Pharmacol. 2013 Jun;53(6):642-53. [Content Brief]

[4]. Infante JR, et al. Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2014 Oct 1;32(28):3103-10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9975 mL	9.9874 mL	19.9748 mL	49.9371 mL
	5 mM	0.3995 mL	1.9975 mL	3.9950 mL	9.9874 mL
	10 mM	0.1997 mL	0.9987 mL	1.9975 mL	4.9937 mL
	15 mM	0.1332 mL	0.6658 mL	1.3317 mL	3.3291 mL
	20 mM	0.0999 mL	0.4994 mL	0.9987 mL	2.4969 mL
	25 mM	0.0799 mL	0.3995 mL	0.7990 mL	1.9975 mL
	30 mM	0.0666 mL	0.3329 mL	0.6658 mL	1.6646 mL
	40 mM	0.0499 mL	0.2497 mL	0.4994 mL	1.2484 mL
	50 mM	0.0399 mL	0.1997 mL	0.3995 mL	0.9987 mL
	60 mM	0.0333 mL	0.1665 mL	0.3329 mL	0.8323 mL
	80 mM	0.0250 mL	0.1248 mL	0.2497 mL	0.6242 mL
	100 mM	0.0200 mL	0.0999 mL	0.1997 mL	0.4994 mL

Keywords

LCL161

44 Cited Publications

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LCL161

Birinapant

Xevinapant

GDC-0152

BV6

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AZD5582

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CUDC-427

Venetoclax

Trametinib

Ruxolitinib

Z-VAD-FMK

Publications Citing Use of MedChemExpress (MCE) LCL161

Alle IAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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LCL161

Birinapant

Xevinapant

GDC-0152

BV6

SM-164

AZD5582

Tolinapant

CUDC-427

Venetoclax

Trametinib

Ruxolitinib

Z-VAD-FMK

Publications Citing Use of MedChemExpress (MCE) LCL161

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Biologische Aktivität

Chemical Information

Publications (44)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LCL161 Related Classifications

HY-15518 Related Classifications