Lenalidomide (CC-5013) | Immunomodulator - MedChemExpress

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                                1. PROTAC Apoptosis
                                2. Ligands for E3 Ligase Molecular Glues Apoptosis
                                3. Lenalidomide
                                Lenalidomide (Synonyms: CC-5013) Cat. No.: HY-A0003 Purity: 99.95% Data Sheet COA SDS Handling Instructions FAQs Technical Support

                                Solubility

                                In Vivo Dissolution Calculator

                                Help & FAQs

                                Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.

                                For research use only. We do not sell to patients.

                                Lenalidomide

                                Lenalidomide Chemical Structure

                                CAS No. : 191732-72-6

                                Size Price Stock Quantity
                                Free Sample (0.1 - 0.2 mg) Apply Now
                                Solid + Solvent (Highly Recommended)
                                10 mM * 1 mL in DMSO ready for reconstitution In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                Solution
                                10 mM * 1 mL in DMSO In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                Solid
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                                Customer Review

                                Based on 60 publication(s) in Google Scholar

                                Other Forms of Lenalidomide:

                                • Lenalidomide-d5 In-stock
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                                Lenalidomide Related Antibodies

                                Top Publications Citing Use of Products

                                56 Publications Citing Use of MCE Lenalidomide

                                • Nature. 2024 Sep;633(8030):670-677. [Abstract]
                                • Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4. [Abstract]
                                • Nat Cancer. 2022 May;3(5):595-613. [Abstract]
                                • Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]
                                • Nat Commun. 2025 Nov 6;16(1):9805. [Abstract]
                                • Nat Commun. 2025 Sep 1;16(1):8155. [Abstract]
                                • Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
                                • Nat Commun. 2017 May 22;8:15398. [Abstract]
                                • Cell Rep Med. 2025 Apr 2:102053. [Abstract]
                                • Microbiome. 2025 Feb 28;13(1):56. [Abstract]
                                • Leukemia. 2025 Mar;39(3):720-733. [Abstract]
                                • Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
                                • Nat Chem Biol. 2021 Jun;17(6):711-717. [Abstract]
                                • Cell Commun Signal. 2025 May 7;23(1):216. [Abstract]
                                • Acta Pharmacol Sin. 2025 Mar 25. [Abstract]
                                • Free Radic Biol Med. 2023 Jul:203:86-101. [Abstract]
                                • Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254. [Abstract]
                                • Neoplasia. 2025 Oct 27:70:101243. [Abstract]
                                • J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
                                • Cell Rep. 2024 May 8;43(5):114211. [Abstract]
                                • Elife. 2018 Aug 1;7:e38430. [Abstract]
                                • Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
                                • Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
                                • Int Immunopharmacol. 2025 May 14:158:114831. [Abstract]
                                • Mol Ther Oncol. 2025 Feb 20;33(1):200952. [Abstract]
                                • ACS Omega. 2024 Dec 3;9(50):49739-49748. [Abstract]
                                • Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
                                • Cancers (Basel). 2024 Mar 28, 16(7), 1319.
                                • Int J Mol Sci. 2023 Sep 14;24(18):14097.
                                • Cancer Sci. 2019 Dec;110(12):3802-3810. [Abstract]
                                • Front Cell Infect Microbiol. 2022 Jul 28;12:954814. [Abstract]
                                • iScience. 2022 Jul 19;25(8):104781.
                                • Biochim Biophys Acta Mol Basis Dis. 2022 Oct 1;1868(10):166472. [Abstract]
                                • Inflammation. 2019 Feb;42(1):221-234. [Abstract]
                                • Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
                                • Clin Chim Acta. 2024 Jan 15:553:117707. [Abstract]
                                • ACS Pharmacol Transl Sci. 2021 Feb 26;4(2):941-952.
                                • Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
                                • Food Chem Toxicol. 2019 Mar:125:392-402. [Abstract]
                                • Oncol Rep. 2018 Jun;39(6):2873-2880. [Abstract]
                                • Am J Pathol. 2015 Jun;185(6):1783-94. [Abstract]
                                • Chemrxiv. 2025 Nov 17.
                                • Harvard University. 2025.
                                • bioRxiv. 2024 October 19.
                                • Patent. US20240261246A1.
                                • bioRxiv. 2024 June 12.
                                • Universidad de Navarra. 2024 Feb 28.
                                • Patent. US20220332776A1.
                                • Oxid Med Cell Longev. 2021 Dec 29:2021:8302831.
                                • Patent. US20210379039A1.
                                • University of Washington. The Columbian College of Arts and Sciences. August 31, 2021.
                                • bioRxiv. April.
                                • Patent. US20180263995A1.
                                • Patent. US20170360780A1.
                                • Faculty of Science, Masaryk University. Department of Experimental Biology.2014.
                                • Harvard Medical School LINCS LIBRARY
                                WB

                                Lenalidomide purchased from MedChemExpress. Usage Cited in: Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]

                                WB analysis of MV4-11 cells treated for 6.5 hr with Lenalidomide, BTX161, A51, or A86 at the indicated concentrations or DMSO.

                                Lenalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430. [Abstract]

                                H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

                                Lenalidomide purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Jun;39(6):2873-2880. [Abstract]

                                Representative western blot membranes showing the expression levels of NF-κB p-p65 and H3 in nuclear protein and of NF-κB p65 and β-actin in total protein. β-actin and H3 are used as internal controls.

                                Lenalidomide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 May 22;8:15398. [Abstract]

                                HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6 h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting. Powered by Bioz See more details on Bioz

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                                Related Small Molecules:

                                Related Proteins:

                                View All Ligands for E3 Ligase Isoform Specific Products:

                                View All Isoforms von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21
                                • Biological Activity

                                • Protocol

                                • Purity & Documentation

                                • References

                                • Customer Review

                                Description

                                Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

                                IC50 & Target[5]

                                Cereblon

                                Cellular Effect
                                Cell Line Type Value Description References
                                EC9706 IC50 340.3 μg/mL Compound: Lenalidomide Antiproliferative activity against human EC9706 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human EC9706 cells after 48 hrs by CCK-8 assay [PMID: 28757066]
                                G-401 IC50 > 10 μM Compound: Lenalidomide Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay [PMID: 39132814]
                                HCC827 IC50 > 10 μM Compound: Lenalidomide Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay [PMID: 31951960]
                                HEK293 IC50 5.19 μM Compound: Lenalidomide Inhibition of BRD4 bromodomain 2 (unknown origin) in HEK293 cells cotransfected with eGFP by flow cytometry based mCherry reporter gene analysis Inhibition of BRD4 bromodomain 2 (unknown origin) in HEK293 cells cotransfected with eGFP by flow cytometry based mCherry reporter gene analysis [PMID: 32550984]
                                JeKo-1 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human JeKo1 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human JeKo1 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                JeKo-1 IC50 > 20000 nM Compound: Lenalidomide Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay [PMID: 35635954]
                                JeKo-1 IC50 > 20000 nM Compound: Lenalidomide Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay [PMID: 35635954]
                                K562 IC50 > 10 μM Compound: Lenalidomide Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay [PMID: 34217059]
                                K562 IC50 > 10 μM Compound: Lenalidomide Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay [PMID: 36306539]
                                Kasumi 1 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human Kasumi-1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human Kasumi-1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                MCF-10A IC50 > 20 μM Compound: Lenalidomide Cytotoxicity against human MCF10A cells after 72 hrs by MTS assay Cytotoxicity against human MCF10A cells after 72 hrs by MTS assay [PMID: 29795767]
                                MCF7 IC50 > 100 μM Compound: Len Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay [PMID: 37619298]
                                MDA-MB-231 IC50 > 100 μM Compound: Len Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay [PMID: 37619298]
                                MDA-MB-468 IC50 > 100 μM Compound: Len Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay [PMID: 37619298]
                                MM1.S IC50 0.081 μM Compound: Lenalidoamide Antiproliferative activity against human MM1.S cells assessed as reduction in cell growth measured after 7 days culturing by CellTiter 96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human MM1.S cells assessed as reduction in cell growth measured after 7 days culturing by CellTiter 96 Aqueous non-radioactive cell proliferation assay [PMID: 33328101]
                                MM1.S IC50 50 nM Compound: 1 Antiproliferative activity against human MM1S cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human MM1S cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                MM1.S IC50 70.17 nM Compound: Lenalidomide Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay [PMID: 35635954]
                                MM1.S IC50 > 20000 nM Compound: Lenalidomide Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay [PMID: 35635954]
                                MV4-11 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human MV411 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human MV411 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                MV4-11 IC50 > 20000 nM Compound: Lenalidomide Antiproliferative activity against human MV411 cells after 72 hrs by MTS assay Antiproliferative activity against human MV411 cells after 72 hrs by MTS assay [PMID: 29795767]
                                MX1 IC50 > 100 μM Compound: Len Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay [PMID: 37619298]
                                NAMALVA IC50 0.36 μM Compound: 1 Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting [PMID: 23168019]
                                PBMC IC50 0.1 μM Compound: 1 Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA [PMID: 23168019]
                                PBMC IC50 100 nM Compound: 1 Antiinflammatory activity in human PBMC cells assessed as reduction in LPS-induced TNF-alpha production preincubated for 1 hr followed by LPS addition and measured after 18 to 20 hrs by ELISA Antiinflammatory activity in human PBMC cells assessed as reduction in LPS-induced TNF-alpha production preincubated for 1 hr followed by LPS addition and measured after 18 to 20 hrs by ELISA [PMID: 31125896]
                                PBMC IC50 100 nM Compound: 11; CC-5013 Inhibition of TNF-alpha release in LPS stimulated human PBMC Inhibition of TNF-alpha release in LPS stimulated human PBMC [PMID: 33906050]
                                PBMC IC50 > 20000 nM Compound: 1 Cytotoxicity against human PBMC cells by CellTiter96 Aqueous non-radioactive cell proliferation assay Cytotoxicity against human PBMC cells by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                RPMI-8226 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                Raji IC50 > 20000 nM Compound: 1 Antiproliferative activity against human Raji cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human Raji cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                T-cell EC50 0.15 μM Compound: 1 Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA [PMID: 23168019]
                                THP-1 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human THP1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human THP1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                U-266 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human U266 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human U266 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                WI-38 IC50 > 20 μM Compound: Lenalidomide Cytotoxicity against human WI38 cells after 72 hrs by MTS assay Cytotoxicity against human WI38 cells after 72 hrs by MTS assay [PMID: 29795767]
                                Z-138 IC50 > 20000 nM Compound: 1 Antiproliferative activity against human Z138 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human Z138 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay [PMID: 31125896]
                                In Vitro

                                Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells[2]. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM[3]. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation[5].

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

                                Lenalidomide Related Antibodies

                                In Vivo

                                The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes[4].

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

                                Clinical Trial
                                Molecular Weight

                                259.26

                                Formula

                                C13H13N3O3

                                CAS No.

                                191732-72-6

                                Appearance

                                Solid

                                Color

                                Off-white to light yellow

                                SMILES

                                O=C1C2=CC=CC(N)=C2CN1C(C(N3)=O)CCC3=O

                                Shipping

                                Room temperature in continental US; may vary elsewhere.

                                Storage
                                Powder -20°C 3 years
                                4°C 2 years
                                In solvent -80°C 1 year
                                -20°C 6 months
                                Solvent & Solubility In Vitro:

                                DMSO : 100 mg/mL (385.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

                                Preparing Stock Solutions
                                Concentration Solvent Mass 1 mg 5 mg 10 mg
                                1 mM 3.8571 mL 19.2857 mL 38.5713 mL
                                5 mM 0.7714 mL 3.8571 mL 7.7143 mL
                                10 mM 0.3857 mL 1.9286 mL 3.8571 mL
                                View the 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

                                • Molarity Calculator

                                • Dilution Calculator

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

                                Mass kg g mg μg ng pg = Concentration M mM μM nM pM × Volume L mL μL × Molecular Weight *

                                Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

                                This equation is commonly abbreviated as: C1V1 = C2V2

                                Concentration (start) M mM μM nM pM

                                C1

                                × Volume (start) L mL μL

                                V1

                                = Concentration (final) M mM μM nM pM

                                C2

                                × Volume (final) L mL μL

                                V2

                                In Vivo:

                                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.

                                • Protocol 1

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

                                  Solubility: ≥ 2.5 mg/mL (9.64 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 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.
                                • Protocol 2

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

                                  Solubility: ≥ 2.5 mg/mL (9.64 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.
                                • Protocol 3

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

                                  Solubility: ≥ 2.5 mg/mL (9.64 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

                                mg/kg

                                Animal weight (per animal)

                                g

                                Dosing volume (per animal)

                                μL

                                Number of animals

                                Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Please enter your animal formula composition: % DMSO + % + % Tween-80 + % Saline Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak. 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). Calculation results: Working solution concentration: mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL). The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE). Tel: 609-228-6898 E-mail: [email protected] Technical Support: [email protected] Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline. Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution If the continuous dosing period exceeds half a month, please choose this protocol carefully. 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.
                                Purity & Documentation

                                Purity: 99.95%

                                Select Batch: HY-A0003-253589 HY-A0003-90881 HY-A0003-05010 HY-A0003-20918 HY-A0003-66714 HY-A0003-00999 HY-A0003-85873 HY-A0003-44023 HY-A0003-823405 HY-A0003-116210 HY-A0003-07964 HY-A0003-568402 Data Sheet (283 KB) SDS (418 KB)

                                COA (251 KB) HNMR (271 KB) LCMS (93 KB)

                                Handling Instructions (2659 KB)
                                References
                                • [1]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742. [Content Brief]

                                  [2]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36. [Content Brief]

                                  [3]. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35. [Content Brief]

                                  [4]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82. [Content Brief]

                                  [5]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25. [Content Brief]

                                  [6]. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

                                  [7]. Omran A, et al. Effects of MRP8, LPS, and lenalidomide on the expressions of TNF-α , brain-enriched, and inflammation-related microRNAs in the primary astrocyte culture. ScientificWorldJournal. 2013 Sep 21;2013:208309. [Content Brief]

                                Cell Assay [3]

                                Cell lines NCI-H929 and U266, and DF15 cells are grown in RPMI-I640 medium containing 10% (V/V) heat-inactivated fetal bovine serum supplemented with 2 mM glutamine. To produce Lenalidomide resistant cell lines, NCI-H929 cells are treated continuously (fresh Lenalidomide is added every 3-4 days) with control (final 0.1% DMSO) or low-dose Lenalidomide (1 μM) for 2 months until the proliferation of cells is no longer inhibited by Lenalidomide (1 μM), as determined by cell viability (Vi-cell XR cell viability analyzer), cell proliferation by flow cytometry and cell cycle analysis (propidium iodide staining). After acquisition of resistance to 1 μM, the resistant H929 cell lines are treated with Lenalidomide (10 μM) for a further 4 months. After this period of time, the cell cultures achieved fully establish resistance up to high-dose Lenalidomide (30 μM). Prior to the experiments described here, H929 Lenalidomide-resistant cells are taken out of culture with compounds for 5-7 days before use[3].

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

                                Animal Administration [4]

                                Mice[4] Imprinting control region (ICR) mice 8-10 weeks of age are used. Lenalidomide is incompletely soluble at 3.5 mg/mL and above in PBS containing 1% HCl, as visible particulates remained after thorough mixing. Therefore 3 mg/mL is selected as the maximum dosing solution concentration (with no visible particulates). Single, individual mice are initially dosed with 3, 10, or 15 mg/kg IV; 4.5, 15, or 22.5 mg/kg IP; and 9, 30, or 45 mg/kg PO. Additional mice (n=4) are then evaluated at the maximum dose achievable by volume and solubility of Lenalidomide in the dosing solution. All mice are monitored closely for 1 h and re-evaluated for toxicities 3, 6, and 24 h postdose[4].

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

                                References
                                • [1]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742. [Content Brief]

                                  [2]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36. [Content Brief]

                                  [3]. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35. [Content Brief]

                                  [4]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82. [Content Brief]

                                  [5]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25. [Content Brief]

                                  [6]. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

                                  [7]. Omran A, et al. Effects of MRP8, LPS, and lenalidomide on the expressions of TNF-α , brain-enriched, and inflammation-related microRNAs in the primary astrocyte culture. ScientificWorldJournal. 2013 Sep 21;2013:208309. [Content Brief]

                                • [1]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742.

                                  [2]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36.

                                  [3]. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35.

                                  [4]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82.

                                  [5]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.

                                  [6]. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

                                  [7]. Omran A, et al. Effects of MRP8, LPS, and lenalidomide on the expressions of TNF-α , brain-enriched, and inflammation-related microRNAs in the primary astrocyte culture. ScientificWorldJournal. 2013 Sep 21;2013:208309.

                                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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

                                Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
                                DMSO 1 mM 3.8571 mL 19.2857 mL 38.5713 mL 96.4283 mL
                                5 mM 0.7714 mL 3.8571 mL 7.7143 mL 19.2857 mL
                                10 mM 0.3857 mL 1.9286 mL 3.8571 mL 9.6428 mL
                                15 mM 0.2571 mL 1.2857 mL 2.5714 mL 6.4286 mL
                                20 mM 0.1929 mL 0.9643 mL 1.9286 mL 4.8214 mL
                                25 mM 0.1543 mL 0.7714 mL 1.5429 mL 3.8571 mL
                                30 mM 0.1286 mL 0.6429 mL 1.2857 mL 3.2143 mL
                                40 mM 0.0964 mL 0.4821 mL 0.9643 mL 2.4107 mL
                                50 mM 0.0771 mL 0.3857 mL 0.7714 mL 1.9286 mL
                                60 mM 0.0643 mL 0.3214 mL 0.6429 mL 1.6071 mL
                                80 mM 0.0482 mL 0.2411 mL 0.4821 mL 1.2054 mL
                                100 mM 0.0386 mL 0.1929 mL 0.3857 mL 0.9643 mL
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                                Lenalidomide Related Classifications

                                • Disease Areas
                                • Cancer Infection Inflammation or Immune System Disease Blood or Cardiovascular Disease Digestive System Disease Urogenital Disease Neurological, Eye or Ear Disease
                                • Coronavirus Infection Blood Disease Prostate Cancer Urogenital Cancer Leukemia/Lymphoma/Myeloma Pancreatic Cancer Digestive System Cancer Viral Infection Digestive System Inflammation
                                • SARS-CoV-2 Infection Leukemia/Lymphoma/Myeloma
                                • Inflammation/Immunology Cancer
                                • Cancer Targeted Therapy Cancer Immunotherapy Cancer Metabolism and Metastasis
                                • PROTAC Apoptosis
                                • Ligands for E3 Ligase Molecular Glues Apoptosis
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                                  Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

                                Keywords:

                                Lenalidomide191732-72-6CC-5013CC5013CC 5013Ligands for E3 LigaseMolecular GluesApoptosisE3 ligase-recruiting MoietydegradationIKZF1IKZF3multiplemyelomaanalogimmunomodulatoryE3ligasecereblonCRL4ligandInhibitorinhibitorinhibit

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