LCL161
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.91%
- CAS No.: 1005342-46-0
- 화학식: C26H33FN4O3S
- 분자량:500.63
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LCL161
More- Cell Res. 2023 Nov;33(11):851-866. [Abstract]
- Immunity. 2021 Aug 10;54(8):1758-1771.e7. [Abstract]
- Adv Mater. 2023 Feb;35(7):e2208782. [Abstract]
- Nat Biomed Eng. 2025 Oct 22. [Abstract]
- Cell Mol Immunol. 2026 Jul;23(7):873-885. [Abstract]
- Nat Commun. 2024 Feb 12;15(1):1282. [Abstract]
- Nat Commun. 2023 Oct 30;14(1):6908. [Abstract]
- ACS Nano. 2025 Oct 21;19(41):36451-36464. [Abstract]
- J Am Chem Soc. 2025 Mar 26. [Abstract]
- Mol Cell. 2025 Apr 3:S1097-2765(25)00259-X. [Abstract]
- Theranostics. 2024 May 5;14(7):2934-2945. [Abstract]
- Theranostics. 2023 Jul 31;13(13):4376-4390. [Abstract]
- Cell Death Differ. 2026 Apr 4. [Abstract]
- Cell Death Differ. 2022 Jun;29(6):1176-1186. [Abstract]
- Cell Death Differ. 2020 May;27(5):1569-1587. [Abstract]
- Cell Death Dis. 2021 Jun 23;12(7):641. [Abstract]
- Pharmacol Res. 2020 Jul;157:104800. [Abstract]
- Cell Death Dis. 2020 Feb 5;11(2):94. [Abstract]
- Dev Cell. 2022 Jan 24;57(2):228-245.e6. [Abstract]
- Leukemia. 2025 Dec 19. [Abstract]
- Cell Rep. 2026 May 26;45(5):117360. [Abstract]
- J Med Chem. 2023 Jun 22;66(12):8159-8169. [Abstract]
- J Med Chem. 2021 Nov 11;64(21):16147-16158. [Abstract]
- J Med Chem. 2019 Oct 24;62(20):9188-9200. [Abstract]
- J Med Chem. 2019 Jun 13;62(11):5616-5627. [Abstract]
- J Med Chem. 2018 Jul 26;61(14):6350-6363. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Int Immunopharmacol. 2026 Mar 15:173:116271. [Abstract]
- Int J Mol Sci. 2026 Jan 7;27(2):618. [Abstract]
- Int J Mol Sci. 2023 Oct 20;24(20):15405. [Abstract]
- Exp Mol Pathol. 2022 Apr:125:104739. [Abstract]
- Am J Cancer Res. 2020 Sep 1;10(9):2813-2831. [Abstract]
- PLoS One. 2021 Mar 26;16(3):e0248175. [Abstract]
- Anticancer Agents Med Chem. 2020;20(6):687-699. [Abstract]
- bioRxiv. 2026 Jan 20.
- Patent. US20250127813A1.
- bioRxiv. 2025 Mar 17:2025.03.14.643359. [Abstract]
- bioRxiv. 2024 Nov 28:2024.11.25.625306. [Abstract]
- Harvard University. 2024 May.
- University of Portland. 2022.
- World J Clin Cases. 2021 Jul 6;9(19):5019-5027. [Abstract]
- 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.
Customer Validation & Images
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Flow Cytometry
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Flow Cytometry
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WB
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Cell Proliferation/Viability Assay
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WB
Biological Activity
IC50: 35 nM (XIAP, in HEK293 cell), 0.40 nM (cIAP1, in MDA-MB-231)[1]
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Cell Line
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Type | Value | Description | References |
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| CCRF-CEM | GI50 |
250 nM
Compound: LCL-161
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Antiproliferative activity against human CCRF-CEM cells
Antiproliferative activity against human CCRF-CEM cells
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[PMID: 28435526] |
| MDA-MB-231 | EC50 |
32.5 nM
Compound: LCL161
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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
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[PMID: 37262387] |
| MDA-MB-231 | EC50 |
37 nM
Compound: LCL161
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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
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[PMID: 37262387] |
| MDA-MB-231 | EC50 |
57 nM
Compound: LCL161
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Induction of apoptosis in human MDA-MB-231 cells
Induction of apoptosis in human MDA-MB-231 cells
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[PMID: 37262387] |
| MDA-MB-231 | EC50 |
7.8 nM
Compound: 2; LCL-161
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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
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[PMID: 28492317] |
| MDA-MB-231 | IC50 |
7.8 nM
Compound: 2; LCL-161
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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
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[PMID: 30091600] |
| SK-OV-3 | EC50 |
1 nM
Compound: LCL161
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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
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[PMID: 31095386] |
| SK-OV-3 | EC50 |
3 nM
Compound: LCL161
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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
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[PMID: 31095386] |
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 (KI of 0.797 μM and Kinact 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1005342-46-0
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Appearance Solid
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분자량 500.63
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화학식 C26H33FN4O3S
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Color White to yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (44)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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
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
2025 Apr 3:S1097-2765(25)00259-X. PMID: 40209701 -
Theranostics
2024 May 5;14(7):2934-2945. PMID: 38773971 -
Theranostics
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
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
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.
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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
2020;20(6):687-699. PMID: 32053082 -
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bioRxiv
2025 Mar 17:2025.03.14.643359. PMID: 40166148 -
bioRxiv
2024 Nov 28:2024.11.25.625306. PMID: 39651304 -
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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 -
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
순도&문서
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Data Sheet (281 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
LCL161 Related Classifications
HY-15518 Related Classifications
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