Lenalidomide hydrochloride
Based on 63 publication(s) in Google Scholar
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) 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 hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
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- CAS. Nr.: 1243329-97-6
- Formel: C13H14ClN3O3
- Molecular Weight:295.72
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Publications Citing Use of MedChemExpress (MCE) Lenalidomide hydrochloride
More- Nature. 2024 Sep;633(8030):670-677. [Abstract]
- Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4. [Abstract]
- Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]
- Nat Cancer. 2022 May;3(5):595-613. [Abstract]
- Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1493. [Abstract]
- Nat Commun. 2025 Nov 6;16(1):9805. [Abstract]
- Nat Commun. 2025 Sep 1;16(1):8155. [Abstract]
- Nat Commun. 2017 May 22;8:15398. [Abstract]
- Nat Chem Biol. 2021 Jun;17(6):711-717. [Abstract]
- Microbiome. 2025 Feb 28;13(1):56. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(21):e18975. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Commun Signal. 2025 May 7;23(1):216. [Abstract]
- Acta Pharmacol Sin. 2025 Mar 25. [Abstract]
- Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- Leukemia. 2025 Mar;39(3):720-733. [Abstract]
- Int J Biol Macromol. 2026 Jan 7;340:150099.
- Mol Ther Oncol. 2025 Feb 20;33(1):200952. [Abstract]
- Free Radic Biol Med. 2023 Jul:203:86-101. [Abstract]
- Cell Rep. 2024 May 8;43(5):114211. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Med Chem. 2026 May 28;69(10):12669-12677. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
- Int Immunopharmacol. 2025 May 14:158:114831. [Abstract]
- Int J Mol Sci. 2023 Sep 14;24(18):14097. [Abstract]
- Front Cell Infect Microbiol. 2022 Jul 28;12:954814. [Abstract]
- Inflammation. 2019 Feb;42(1):221-234. [Abstract]
- ACS Omega. 2024 Dec 3;9(50):49739-49748. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2022 Oct 1;1868(10):166472. [Abstract]
- Cancer Sci. 2019 Dec;110(12):3802-3810. [Abstract]
- Am J Pathol. 2015 Jun;185(6):1783-94. [Abstract]
- Neoplasia. 2025 Oct 27:70:101243. [Abstract]
- Cancers (Basel). 2024 Mar 28;16(7):1319. [Abstract]
- Oncol Rep. 2018 Jun;39(6):2873-2880. [Abstract]
- iScience. 2022 Jul 19;25(8):104781. [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. [Abstract]
- Cancer Med. 2026 Jun;15(6):e71985. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Food Chem Toxicol. 2019 Mar:125:392-402. [Abstract]
- SSRN. 2026 Jun 16.
- Charles University. 2026.
- bioRxiv. 2026 Feb 8:2026.02.06.704516. [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. [Abstract]
- Patent. US20210379039A1.
- University of Washington. 2021 Aug 31.
- bioRxiv. April.
- Patent. US20180263995A1.
- Elife. 2018 Aug 1;7:e38430. [Abstract]
- Patent. US20170360780A1.
- Masaryk University. 2014.
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Cereblon |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1243329-97-6
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Molecular Weight 295.72
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Formel C13H14ClN3O3
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SMILES
O=C1C2=CC=CC(N)=C2CN1C(C(N3)=O)CCC3=O.[H]Cl
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Synonyms
CC-5013 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (63)
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Journal Impact Factor
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Most Recent
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Nature
2024 Sep;633(8030):670-677. PMID: 39198645 -
Cancer Cell
2022 Nov 14;40(11):1294-1305.e4. PMID: 36084652 -
Cell
Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. [Abstract]2018 Sep 20;175(1):171-185.e25. PMID: 30146162
Lenalidomide hydrochloride 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.
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Nat Cancer
IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia. [Abstract]2022 May;3(5):595-613. PMID: 35534777
Lenalidomide hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 May;3(5):595-613. [Abstract]
Western blot analysis for IKAROS, CK1α and MENIN protein following treatment of MV4;11 human MLL-r AML cell line for 5 hours with increasing doses of Thalidomide, lenalidomide, Pomalidomide and iberdomide (10,100, 1000 nM), using ACTIN as a loading control.
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Cancer Res
Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]2025 Jan 2;85(1):101-117. PMID: 39437162 -
Nat Commun
Tissue-resident macrophage survival depends on mitochondrial function regulated by SerpinB2 in chronic inflammation. [Abstract]2026 Feb 12;17(1):1493. PMID: 41680163 -
Nat Commun
PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]2025 Nov 6;16(1):9805. PMID: 41198675 -
Nat Commun
Multiple myeloma associated long non-coding RNA PLUM confers chemoresistance by enhancing PRC2 mediated UPR pathway activation. [Abstract]2025 Sep 1;16(1):8155. PMID: 40890111 -
Nat Commun
pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase. [Abstract]2017 May 22;8:15398. PMID: 28530236
Lenalidomide hydrochloride 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.
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Nat Chem Biol
2021 Jun;17(6):711-717. PMID: 34035522 -
Microbiome
2025 Feb 28;13(1):56. PMID: 40022244 -
Adv Sci (Weinh)
Targeting PRKCN, an Essential Driver Orchestrating mTOR-IRF4 Axis Independently of Kinase Activity, in Multiple Myeloma. [Abstract]2026 Apr;13(21):e18975. PMID: 41655233 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Cell Commun Signal
IKZF1 as a potential therapeutic target for dendritic cell-mediated immunotherapy in IgA nephropathy. [Abstract]2025 May 7;23(1):216. PMID: 40336063 -
Acta Pharmacol Sin
2025 Mar 25. PMID: 40133626 -
Acta Pharmacol Sin
The novel cereblon modulator CC-885 inhibits mitophagy via selective degradation of BNIP3L. [Abstract]2020 Sep;41(9):1246-1254. PMID: 32210356 -
J Transl Med
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]2024 Dec 3;22(1):1095. PMID: 39623468 -
Leukemia
2025 Mar;39(3):720-733. PMID: 39885295 -
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Mol Ther Oncol
Dual CARM1-and IKZF3-targeting: A novel approach to multiple myeloma therapy synergy between CARM1 inhibition and IMiDs. [Abstract]2025 Feb 20;33(1):200952. PMID: 40123976 -
Free Radic Biol Med
Targeting ABCB6 with nitidine chloride inhibits PI3K/AKT signaling pathway to promote ferroptosis in multiple myeloma. [Abstract]2023 Jul:203:86-101. PMID: 37044150 -
Cell Rep
Identification of WNK1 as a therapeutic target to suppress IgH/MYC expression in multiple myeloma. [Abstract]2024 May 8;43(5):114211. PMID: 38722741 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Med Chem
Real-Time NanoBRET Target Engagement Reveals Permeability-Activity Relationships in BET-Targeting Degraders. [Abstract]2026 May 28;69(10):12669-12677. PMID: 42139371 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Eur J Pharmacol
Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]2025 Dec 5:1008:178303. PMID: 41183585 -
Int Immunopharmacol
Pomalidomide promotes macrophage control of Mycobacterium tuberculosis via enhancing HDAC6-mediated autophagy. [Abstract]2025 May 14:158:114831. PMID: 40373598 -
Int J Mol Sci
Lenalidomide Promotes Thrombosis Formation, but Does Not Affect Platelet Activation in Multiple Myeloma. [Abstract]2023 Sep 14;24(18):14097. PMID: 37762399 -
Front Cell Infect Microbiol
Lenalidomide potentially reduced the level of cell- associated HIV RNA and improved persistent inflammation in patients with HIV-associated cryptococcal meningitis a pilot study. [Abstract]2022 Jul 28;12:954814. PMID: 35967862 -
Inflammation
Progranulin Promotes Regeneration of Inflammatory Periodontal Bone Defect in Rats via Anti-inflammation, Osteoclastogenic Inhibition, and Osteogenic Promotion. [Abstract]2019 Feb;42(1):221-234. PMID: 30187338 -
ACS Omega
Dynamic Detection of the E3-PROTAC-Target Protein Ternary Complex In Vitro and In Vivo via Bimolecular Fluorescence Complementation. [Abstract]2024 Dec 3;9(50):49739-49748. PMID: 39713624 -
Biochim Biophys Acta Mol Basis Dis
Dengue virus is involved in insulin resistance via the downregulation of IRS-1 by inducing TNF-α secretion. [Abstract]2022 Oct 1;1868(10):166472. PMID: 35752384 -
Cancer Sci
Activity of TAS4464, a novel NEDD8 activating enzyme E1 inhibitor, against multiple myeloma via inactivation of nuclear factor κB pathways. [Abstract]2019 Dec;110(12):3802-3810. PMID: 31583781 -
Am J Pathol
Pathophysiological function of endogenous calcitonin gene-related peptide in ocular vascular diseases. [Abstract]2015 Jun;185(6):1783-94. PMID: 25857228 -
Neoplasia
Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition. [Abstract]2025 Oct 27:70:101243. PMID: 41151153 -
Cancers (Basel)
Synergy between BRD9- and IKZF3-Targeting as a Therapeutic Strategy for Multiple Myeloma. [Abstract]2024 Mar 28;16(7):1319. PMID: 38610997 -
Oncol Rep
Microvesicles shed from bortezomib-treated or lenalidomide-treated human myeloma cells inhibit angiogenesis in vitro. [Abstract]2018 Jun;39(6):2873-2880. PMID: 29693175
Lenalidomide hydrochloride 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.
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iScience
Identification of a drug-response gene in multiple myeloma through longitudinal single-cell transcriptome sequencing. [Abstract]2022 Jul 19;25(8):104781. PMID: 35992084 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Clin Chim Acta
2024 Jan 15:553:117707. PMID: 38103853 -
ACS Pharmacol Transl Sci
General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]2021 Feb 26;4(2):941-952. PMID: 33860212 -
Cancer Med
Synergistic Antitumor Activity of HAT Inhibitor A485 and XPO1 Inhibitor KPT8602 in Multiple Myeloma. [Abstract]2026 Jun;15(6):e71985. PMID: 42231094 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Food Chem Toxicol
Inorganic arsenic induces pyroptosis and pancreatic β cells dysfunction through stimulating the IRE1α/TNF-α pathway and protective effect of taurine. [Abstract]2019 Mar:125:392-402. PMID: 30660605 -
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bioRxiv
Regulation of BCL11A DNA binding and expression in human erythrocyte precursor HUDEP-2 cells. [Abstract]2026 Feb 8:2026.02.06.704516. PMID: 41822826 -
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Oxid Med Cell Longev
TNF- α Induces Neutrophil Apoptosis Delay and Promotes Intestinal Ischemia-Reperfusion-Induced Lung Injury through Activating JNK/FoxO3a Pathway. [Abstract]2021 Dec 29:2021:8302831. PMID: 35003520 -
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Elife
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. [Abstract]2018 Aug 1;7:e38430. PMID: 30067223
Lenalidomide hydrochloride 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.
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Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
[1]. 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]
[2]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742. [Content Brief]
[3]. 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]
[4]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36. [Content Brief]
[5]. 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]
[6]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Lenalidomide hydrochloride Related Classifications
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