Lenalidomide
Based on 63 publication(s) in Google Scholar
Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 191732-72-6
- Fòrmula: C13H13N3O3
- Peso molecular:259.26
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Lenalidomide
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 15;6(4):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 Jun 17:158:114831. [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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Actividad biológica
|
Cereblon |
IKZF1 |
IKZF3 |
|
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 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] |
| 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] |
| 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] |
| MM.1S | 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] |
| MM.1S | 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] |
| MM.1S | 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] |
| MM.1S | 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: 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] |
| 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] |
| 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 |
>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] |
| 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] |
| 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] |
| 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] |
| 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] |
Lenalidomide (1-10 μM; 4-24 h) induces ubiquitination and degradation of CK1α in human del (5q) myeloid KG-1 cells[1].
Lenalidomide (0.01-10 μM; 0-24 h) induces CRBN-dependent post-translational degradation of CK1α in multiple human hematopoietic cell lines[1].
Lenalidomide (1-10 μM; 90 min-4 h) mediates the physical interaction between CK1α and CRBN, thereby enabling CRL4CRBN-dependent ubiquitination of CK1α in human hematopoietic cells and cell-free systems[1].
Lenalidomide (1 μM; 5-25 days) specifically depletes CD34+ cells derived from patients with del (5q) myelodysplastic syndrome (MDS), and this effect is reversed by CSNK1A1 overexpression; in contrast, CSNK1A1 downregulation sensitizes primary human CD34+ hematopoietic stem/progenitor cells to Lenalidomide[1].
Lenalidomide (0.01-10 μM; 4-24 h) induces the degradation of CK1α, IKZF1 and IKZF3 in mouse Ba/F3 cells carrying the mouse Crbn I391V mutation and human 293T cells[1].
Lenalidomide (0.3-10 μM; 6-72 h) selectively induces the degradation of CK1α in human MDS-L and KG-1 myeloid cells, and this effect is blocked by competition with the cereblon modulator CC-122 (HY-100507)[1].
Lenalidomide selectively destabilizes exogenous IKZF1 and IKZF3 (but not other Ikaros family members or IRF4) in a proteasome-dependent and cullin-dependent manner in 293FT embryonic kidney cells[4].
Lenalidomide induces proteasomal degradation of endogenous IKZF1 (in U937 leukemia cells) as well as endogenous IKZF1 and IKZF3 (in MM1S and L363 myeloma cells) via a post-transcriptional, cullin-dependent mechanism[4].
Lenalidomide-induced degradation of IKZF1 and IKZF3 in 293FT embryonic kidney cells, U937 leukemia cells, and MM1S, L363 and KMS34 myeloma cells is strictly dependent on functional cereblon[4].
Lenalidomide mediates direct and specific interactions between cereblon and IKZF1/IKZF3, thereby triggering cereblon-dependent ubiquitination of IKZF1[4].
Lenalidomide exerts antiproliferative effects on MM1S, KMS34 and L363 myeloma cells via cereblon-dependent degradation of IKZF1 and IKZF3, and this mechanism is both necessary and sufficient for its anti-myeloma activity[4].
Lenalidomide inhibits the TNF-α/HMGB1 pathway and reduces the pyroptosis level of THP-1 M1 macrophages differentiated by PMA and induced by LPS (HY-D1056)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human del(5q) myeloid KG-1 cells, human multiple myeloma MM1S cells, human chronic myelogenous leukemia K562 cells, human T-cell leukemia Jurkat cells, human embryonic kidney 293T cells
-
Concentration:1 μM (KG-1 cells); 0.01, 0.1, 1 and 10 μM (MM1S, K562, Jurkat cells); 10 μM (293T cells)
-
Incubation Time:0, 1, 2, 3, 5, 8, 24 h (KG-1 cells); 24 h (MM1S, K562, Jurkat cells); 5 h (293T cells)
-
Result:Caused time-dependent decreases in CK1α protein levels in KG-1 cells, with visible reduction by 2 hours and near-complete loss by 24 hours at 1 μM.
Decreased CK1α levels in MM1S, K562, and Jurkat cells, with no effect on CSNK1A1 mRNA expression at 0.01-10 μM for 24 h.
Eliminated lenalidomide-dependent CK1α degradation in 293T cells with homozygous CRBN inactivation at 10 μM for 5 h.
Lenalidomide (0.5-45 mg/kg; i.v., i.p., p.o.; single bolus) is well-tolerated at doses up to 15 mg/kg i.v., 22.5 mg/kg i.p., and 45 mg/kg p.o. in healthy ICR mice, with preferential distribution to lung, liver, heart, and spleen, and limited brain penetration detectable only at i.v. doses of 5 mg/kg and higher[5].
Lenalidomide (50 mg/kg; p.o.; daily; 21 days starting on day +14 after transplantation) synergizes with anti-TIGIT to induce CD8+ T cell-dependent antimyeloma activity, reduce T cell exhaustion, and expand memory T cells in the bone marrow of multiple myeloma-bearing mice after autologous stem cell transplantation; lenalidomide monotherapy shows no antimyeloma activity with suboptimal T cell dosing[2].
Lenalidomide (3 mg/kg; i.p.; single dose) reduces pathological damage, improves organ function, inhibits TNF-α/HMGB1 pathway activation, suppresses pyroptosis, and reduces M1 macrophage activation in mice with LPS/D-Gal-induced ALF and AKI[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (female)[1]
-
Dosage:10 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Did not alter CK1α protein levels in mouse bone marrow cells.
-
Animal Model:C57BL/6J; CRBN (female, 8-12 weeks of age, multiple myeloma model via Vk12653 myeloma cell injection 2 weeks prior to autologous stem cell transplantation with suboptimal donor T cell dose)[2]
-
Dosage:50 mg/kg
-
Administration:p.o.; daily; 21 days starting on day +14 after transplantation
-
Result:Showed no antimyeloma activity as monotherapy with suboptimal T cell dose.
Drove synergistic antimyeloma efficacy in combination with anti-TIGIT.
Reduced serum M-band progression in combination with anti-TIGIT.
Improved survival in combination with anti-TIGIT.
Reduced the frequency of exhausted CD8+ T cells in combination with anti-TIGIT.
Expanded central memory CD8+ T cell subsets in combination with anti-TIGIT.
Enhanced IFN-γ production from PD-1+ CD8+ T cells in combination with anti-TIGIT.
Increased expression of Il7r and Ikzf2 genes associated with memory T cell maintenance in bone marrow CD8+ T cells in combination with anti-TIGIT.
Fully protected long-term survivors against myeloma rechallenge in combination with anti-TIGIT.
-
Animal Model:C57/BL6 (male, 8-10 weeks old, 20-25 g, LPS and D-Gal induced)[3]
-
Dosage:3 mg/kg
-
Administration:i.p.; single dose (2 hours before LPS/D-Gal exposure)
-
Result:Reduced liver lobular structural damage, hepatocyte necrosis, and inflammatory cell infiltration in liver tissue.
Ameliorated renal tubular epithelial swelling, brush border loss, and vacuolar degeneration in kidney tissue.
Decreased serum levels of alanine aminotransferase, aspartate aminotransferase, total bilirubin, blood urea nitrogen, creatinine, TNF-α, HMGB1, IL-1β, and IL-18 compared to the model group.
Decreased protein levels of IL-1β, IL-18, NLRP3, caspase-1 p10+p12, and GSDMD in liver and kidney tissues.
Reduced expression of M1 macrophage markers CD68 and iNOS in liver and kidney tissues.
-
Animal Model:ICR mice (8-10 weeks of age)[5]
-
Dosage:0.5、1.5、5、10、15 mg/kg (i.v.);
0.5、10、22.5 mg/kg (i.p.);
45 mg/kg (p.o.) -
Administration:i.v.; single bolus; i.p.; single bolus; p.o.; single bolus
-
Result:Caused no observable toxicity up to 24 hours post-dose at 15 mg/kg i.v., 22.5 mg/kg i.p., and 45 mg/kg p.o., with one fatal event occurring immediately after 15 mg/kg i.v. administration.
Reached highest tissue concentrations at 2 minutes post-10 mg/kg i.v. dose in lung (15 μg/g), followed by liver (5 μg/g), heart (2.4 μg/g), and spleen (1.3 μg/g).
Decreased to less than 15 ng/g in all tissues by 8 hours post-10 mg/kg i.v. dose.
Was detectable in brain tissue only after i.v. doses of 5 and 10 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 191732-72-6
-
Appearance Solid
-
Peso molecular 259.26
-
Fòrmula C13H13N3O3
-
Color Off-white to light yellow
-
SMILES
O=C1C2=CC=CC(N)=C2CN1C(C(N3)=O)CCC3=O
-
Synonyms
CC-5013
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (63)
-
Journal Impact Factor
-
Most Recent
-
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 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.
-
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 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.
-
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 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 15;6(4):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 Jun 17:158:114831. 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 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 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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Solvente y solubilidad
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)
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.
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.
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 (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.
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.
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.
Pureza y Documentación
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Ficha de datos (300 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Krönke J, et al. Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS. Nature. 2015 Jul 9;523(7559):183-188. [Content Brief]
[3]. Wang Y, et al. TNF-α/HMGB1 inflammation signalling pathway regulates pyroptosis during liver failure and acute kidney injury. Cell Prolif. 2020 Jun;53(6):e12829. [Content Brief]
[4]. Lu G, et al. The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science (New York, N.Y.). 2014 Jan 17;343(6168):305-9. [Content Brief]
[5]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. The AAPS journal. 2012 Dec;14(4):872-82. [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, 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 |