Lenalidomide (CC-5013) | Immunomodulator - MedChemExpress
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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 Chemical Structure
CAS No. : 191732-72-6
Size | Price | Stock | Quantity |
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Free Sample (0.1 - 0.5 mg) | Apply Now | ||
Solid + Solvent (Highly Recommended) | |||
10 mM * 1 mL in DMSO ready for reconstitution | USD 73 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
Solution | |||
10 mM * 1 mL in DMSO | USD 73 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
Solid | |||
100 mg | USD 66 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
500 mg | USD 119 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
1 g | USD 198 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
5 g | USD 495 | In-stock | 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31 |
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Based on 43 publication(s) in Google Scholar
Other Forms of Lenalidomide:
- Lenalidomide hemihydrate In-stock
- Lenalidomide-d5 Get quote
- Lenalidomide-13C5,15N Get quote
- rac-Lenalidomide-13C5 Get quote
- Lenalidomide hydrochloride Get quote
- Lenalidomide sodium Get quote
- Lenalidomide (Standard) Get quote
Lenalidomide Related Antibodies
39 Publications Citing Use of MCE Lenalidomide
- •Nature. 2024 Sep;633(8030):670-677. [Abstract]
- •Cancer Cell. 2022 Aug 26;S1535-6108(22)00372-5. [Abstract]
- •Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]
- •Nat Cancer. 2022 May;3(5):595-613. [Abstract]
- •Nat Commun. 2017 May 22;8:15398. [Abstract]
- •Cancer Res. 2024 Oct 22. [Abstract]
- •Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- •Nat Chem Biol. 2021 Jun;17(6):711-717. [Abstract]
- •Cell Rep. 2024 May 8;43(5):114211. [Abstract]
- •Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254. [Abstract]
- •Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- •Free Radic Biol Med. 2023 Apr 10;S0891-5849(23)00373-8. [Abstract]
- •Biochim Biophys Acta Mol Basis Dis. 2022 Jun 22;166472. [Abstract]
- •Elife. 2018 Aug 1;7:e38430. [Abstract]
- •Cancers (Basel). 2024 Mar 28, 16(7), 1319.
- •Clin Chim Acta. 2023 Dec 14:117707. [Abstract]
- •Cancer Sci. 2019 Dec;110(12):3802-3810. [Abstract]
- •Int J Mol Sci. 2023 Sep 14, 24(18), 14097.
- •Front Cell Infect Microbiol. 2022 Jul 28;12:954814. [Abstract]
- •iScience. 19 July 2022, 104781.
- •ACS Pharmacol Transl Sci. 2021 Feb 26.
- •Food Chem Toxicol. 2019 Mar;125:392-402. [Abstract]
- •Inflammation. 2019 Feb;42(1):221-234. [Abstract]
- •Oncol Rep. 2018 Jun;39(6):2873-2880. [Abstract]
- •Am J Pathol. 2015 Jun;185(6):1783-94. [Abstract]
- •Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- •Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- •Patent. US20240261246A1.
- •bioRxiv. 2024 June 12.
- •Universidad de Navarra. 2024 Feb 28.
- •Patent. US20220332776A1.
- •Oxid Med Cell Longev. 29 Dec 2021.
- •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
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 BiozFeatured Recommendations
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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]. | ||||||||||||
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IC50 & Target[5] |
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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 |
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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
* 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.
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 pMC1 × Volume (start) L mL μLV1 = Concentration (final) M mM μM nM pMC2 × Volume (final) L mL μLV2 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.
Dosage mg/kgAnimal weight (per animal) gDosing volume (per animal) μLNumber 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-A0003-05010 HY-A0003-90881 HY-A0003-20918 HY-A0003-66714 HY-A0003-00999 HY-A0003-85873 HY-A0003-116210 HY-A0003-44023 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 |
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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. |
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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 |
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[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 |
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DMSO | 1 mM | 3.8571 mL | 19.2856 mL | 38.5712 mL | 96.4281 mL |
5 mM | 0.7714 mL | 3.8571 mL | 7.7142 mL | 19.2856 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 | 6.4285 mL | |
20 mM | 0.1929 mL | 0.9643 mL | 1.9286 mL | 4.8214 mL | |
25 mM | 0.1543 mL | 0.7714 mL | 1.5428 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
- Inflammation/Immunology Cancer
- Cancer Targeted Therapy Cancer Immunotherapy Cancer Metabolism and Metastasis
- PROTAC Apoptosis
- Ligands for E3 Ligase Molecular Glues Apoptosis
- Do most proteins show cross-species activity?
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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