Home Ubiquitin E3 ligase Ligand chemical - TNF-alpha inhibitor - E3 Ligase inhibitor - VEGFR inhibitor - Caspase activator - Apoptosis related activator Lenalidomide For research use only.

Lenalidomide

Synonyms: CC-5013

Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. 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 promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

Lenalidomide Chemical Structure

Lenalidomide Chemical Structure

CAS: 191732-72-6

Selleck's Lenalidomide has been cited by 155 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Lenalidomide Related Products

Choose Selective E3 ligase Ligand Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LB771-HNC Growth Inhibition Assay IC50=2.15038 μM SANGER
L-363 Growth Inhibition Assay IC50=2.92212 μM SANGER
JAR Growth Inhibition Assay IC50=2.97001 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=4.10515 μM SANGER
BT-549 Growth Inhibition Assay IC50=6.21849 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=7.89512 μM SANGER
BV-173 Growth Inhibition Assay IC50=8.67585 μM SANGER
HMV-II Growth Inhibition Assay IC50=10.0172 μM SANGER
HCC1806 Growth Inhibition Assay IC50=11.4467 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=11.571 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=11.9764 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=12.6241 μM SANGER
T47D Growth Inhibition Assay IC50=13.2099 μM SANGER
HOP-62 Growth Inhibition Assay IC50=13.48 μM SANGER
A2058 Growth Inhibition Assay IC50=13.8199 μM SANGER
SW620 Growth Inhibition Assay IC50=14.2473 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=14.4892 μM SANGER
HAL-01 Growth Inhibition Assay IC50=14.5796 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=14.9108 μM SANGER
COLO-684 Growth Inhibition Assay IC50=15.3979 μM SANGER
DEL Growth Inhibition Assay IC50=15.499 μM SANGER
K5 Growth Inhibition Assay IC50=16.1486 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=16.4652 μM SANGER
ACN Growth Inhibition Assay IC50=16.5297 μM SANGER
H9 Growth Inhibition Assay IC50=16.626 μM SANGER
EM-2 Growth Inhibition Assay IC50=17.143 μM SANGER
HSC-4 Growth Inhibition Assay IC50=17.6601 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=17.783 μM SANGER
TE-1 Growth Inhibition Assay IC50=17.9968 μM SANGER
LN-405 Growth Inhibition Assay IC50=19.9076 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=20.3573 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=20.5759 μM SANGER
RS4-11 Growth Inhibition Assay IC50=22.1563 μM SANGER
ES3 Growth Inhibition Assay IC50=22.6963 μM SANGER
SBC-1 Growth Inhibition Assay IC50=23.8696 μM SANGER
CTV-1 Growth Inhibition Assay IC50=25.0149 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=25.4009 μM SANGER
HCC2218 Growth Inhibition Assay IC50=25.5407 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=28.2026 μM SANGER
ABC-1 Growth Inhibition Assay IC50=29.6974 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=29.7317 μM SANGER
WM-115 Growth Inhibition Assay IC50=30.3099 μM SANGER
SW1990 Growth Inhibition Assay IC50=30.33 μM SANGER
HCC70 Growth Inhibition Assay IC50=30.7346 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=30.8839 μM SANGER
JEG-3 Growth Inhibition Assay IC50=31.1614 μM SANGER
C8166 Growth Inhibition Assay IC50=31.2274 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=31.6755 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=32.683 μM SANGER
NKM-1 Growth Inhibition Assay IC50=32.9568 μM SANGER
ECC10 Growth Inhibition Assay IC50=34.7443 μM SANGER
A2780 Growth Inhibition Assay IC50=35.3601 μM SANGER
KY821 Growth Inhibition Assay IC50=35.7681 μM SANGER
MKN1 Growth Inhibition Assay IC50=36.2137 μM SANGER
EKVX Growth Inhibition Assay IC50=37.4212 μM SANGER
EW-16 Growth Inhibition Assay IC50=38.3885 μM SANGER
CTB-1 Growth Inhibition Assay IC50=39.7789 μM SANGER
COR-L105 Growth Inhibition Assay IC50=40.4746 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=41.2069 μM SANGER
Mewo Growth Inhibition Assay IC50=41.9871 μM SANGER
BCPAP Growth Inhibition Assay IC50=43.7917 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=44.2776 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=46.6986 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=48.3224 μM SANGER
697 Growth Inhibition Assay IC50=50.3545 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=52.3142 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=52.7024 μM SANGER
NOS-1 Growth Inhibition Assay IC50=52.8559 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=53.0508 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=53.6364 μM SANGER
LU-135 Growth Inhibition Assay IC50=55.1853 μM SANGER
OE33 Growth Inhibition Assay IC50=55.818 μM SANGER
ML-2 Growth Inhibition Assay IC50=55.9489 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=56.2893 μM SANGER
Daoy Growth Inhibition Assay IC50=56.3204 μM SANGER
KNS-62 Growth Inhibition Assay IC50=57.0142 μM SANGER
NBsusSR Growth Inhibition Assay IC50=57.5705 μM SANGER
UACC-257 Growth Inhibition Assay IC50=58.6264 μM SANGER
LU-139 Growth Inhibition Assay IC50=58.826 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=58.8643 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=58.8942 μM SANGER
MLMA Growth Inhibition Assay IC50=59.091 μM SANGER
A3-KAW Growth Inhibition Assay IC50=59.2809 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=59.6287 μM SANGER
A388 Growth Inhibition Assay IC50=60.449 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=60.9905 μM SANGER
GCT Growth Inhibition Assay IC50=61.0786 μM SANGER
K-562 Growth Inhibition Assay IC50=61.5333 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=61.875 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=63.4043 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=65.0121 μM SANGER
NB6 Growth Inhibition Assay IC50=65.988 μM SANGER
HCE-T Growth Inhibition Assay IC50=67.0798 μM SANGER
DOK Growth Inhibition Assay IC50=67.4948 μM SANGER
HT-1376 Growth Inhibition Assay IC50=69.8314 μM SANGER
NEC8 Growth Inhibition Assay IC50=70.1243 μM SANGER
G-402 Growth Inhibition Assay IC50=70.9395 μM SANGER
GR-ST Growth Inhibition Assay IC50=71.172 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=71.4434 μM SANGER
CHP-212 Growth Inhibition Assay IC50=71.965 μM SANGER
KU812 Growth Inhibition Assay IC50=72.9702 μM SANGER
Becker Growth Inhibition Assay IC50=73.1489 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=74.7486 μM SANGER
A498 Growth Inhibition Assay IC50=74.9308 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=75.7663 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=78.6147 μM SANGER
CAL-33 Growth Inhibition Assay IC50=78.9939 μM SANGER
COLO-680N Growth Inhibition Assay IC50=79.1007 μM SANGER
D-283MED Growth Inhibition Assay IC50=79.812 μM SANGER
ATN-1 Growth Inhibition Assay IC50=81.1187 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=81.7296 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=81.8849 μM SANGER
HEL Growth Inhibition Assay IC50=82.4134 μM SANGER
NB69 Growth Inhibition Assay IC50=83.0033 μM SANGER
MPP-89 Growth Inhibition Assay IC50=83.2575 μM SANGER
COLO-829 Growth Inhibition Assay IC50=85.4912 μM SANGER
ONS-76 Growth Inhibition Assay IC50=85.7908 μM SANGER
EW-3 Growth Inhibition Assay IC50=86.2032 μM SANGER
EW-11 Growth Inhibition Assay IC50=86.4336 μM SANGER
SW900 Growth Inhibition Assay IC50=87.2053 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=87.2243 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=91.0405 μM SANGER
HCC1419 Growth Inhibition Assay IC50=91.6374 μM SANGER
CAL-72 Growth Inhibition Assay IC50=92.0219 μM SANGER
Mo-T Growth Inhibition Assay IC50=92.7697 μM SANGER
OC-314 Growth Inhibition Assay IC50=92.8821 μM SANGER
BHT-101 Growth Inhibition Assay IC50=93.1 μM SANGER
EW-18 Growth Inhibition Assay IC50=93.8462 μM SANGER
TE-12 Growth Inhibition Assay IC50=94.3055 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=96.0516 μM SANGER
DF15 Function assay 4 hrs Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF15 cells expressing pLOC-ePL-tagged aiolos after 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay, EC50 = 0.053 μM. 28358507
DF15 Function assay 4 hrs Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis, EC50 = 0.067 μM. 28425720
DF15 Function assay 4 hrs Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing ePL-tagged aiolos after 4 hrs by luminometric analysis, EC50 = 0.087 μM. 28425720
T-cells Function assay 2 to 3 days Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA, EC50 = 0.15 μM. 23168019
NAMALWA Antiproliferative assay 72 hrs Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.36 μM. 23168019
CD34+ progenitor cells Function assay 14 days Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD36 expression after 14 days 17576924
CD34+ progenitor cells Function assay 14 days Decrease in myeloid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as CD33 expression after 14 days 17576924
CD34+ progenitor cells Function assay 14 days Decrease in erythroid differentiation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient assessed as glycophorin A expression after 14 days 17576924
CD34+ progenitor cells Growth inhibition assay 14 days Inhibition of cell proliferation of CD34+ progenitor cells from myelodysplastic syndrome del(5q) patient after 14 days 17576924
CD34+ progenitor cells Growth inhibition assay 14 days Growth inhibition of CD34+ progenitor cells from non-del(5q) myelodysplastic syndrome patient after 14 days 17576924
DF15 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
OPM2 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
DF15 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
OPM2 Function assay 0.1 to 10 uM 5 hrs Induction of cereblon-mediated ikaros degradation in human OPM2 cells at 0.1 to 10 uM after 5 hrs by immunoblot analysis 28425720
EC9706 Antiproliferative assay 150 ug/mL 48 hrs Antiproliferative activity against human EC9706 cells at 150 ug/mL after 48 hrs by CCK-8 assay 28757066
Click to View More Cell Line Experimental Data

Biological Activity

Description Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. 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 promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Targets
CRBN [3] VEGF [1] TNF-α [1]
(PBMCs)
13 nM
In vitro
In vitro

Lenalidomide strongly induces IL-2 and sIL-2R production. Lenalidomide-induced tyrosine phosphorylation of CD28 on T cells is followed by a down-stream activation of NF-κB. [2]

Lenalidomide and pomalidomide inhibits autoubiquitination of CRBN in HEK293 T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA). Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for Lenalidomide resistance in H929 myeloma cell lines is accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and Lenalidomide, CRBN protein is undetectable. [3]

Lenalidomide prevents induction of defects by down-regulating tumor cell inhibitory molecule expression. Lenalidomide prevents induction of tumor-induced T cell lytic synapse dysfunction. Lenalidomide treatment blocks CLL cell-induced T cell actin synapse dysfunction, mimicks antibody blockade, and down-regulates expression of CLL inhibitory ligands and their receptors on T cells. Lenalidomide treatment prevents tumor-induced immune suppression in FL, DLBCL, HL, MM, SCC, and OC and down-regulates immunosuppressive ligand expression on all tumor cells examined. CTL killing function significantly increases following antibody blockade of CLL inhibitory ligands or Lenalidomide treatment compared to control treatments. Treatment of autologous CLL-T cell co-cultures with Lenalidomide reverses impaired CD8+ T cell lytic synapse formation and granzyme B trafficking. [4]
Kinase Assay Assay for inhibition of TNF synthesis by human PBMCs
Human PBMCs from normal donors are obtained by Ficoll−Hypaque density centrifugation. Cells (106 cells/mL) are cultured in RPMI supplemented with 10 AB+ serum, 2 mM l-glutamine, 100 U/mL penicillin, and 100 μg/mL streptomycin. Lenalidomide is dissolved in DMSO at 20 mg/mL; further dilution is done with culture medium. The final DMSO concentration in all assays including the controls is 0.25%. Lenalidomide is added to cells 1 hour prior to the addition of LPS. PBMCs (106 cells/mL) are stimulated with 1 μg/mL of LPS from Salmonella minnesota R595. Cells, in triplicate, are incubated with LPS for 18−20 hours at 37 °C in 5% CO2. Supernatants are then harvested and assayed for cytokine levels. In some experiments, supernatants are kept frozen at −70 °C until use. Cell viability is assayed by Trypan blue exclusion dye method. The concentration of TNFα in the culture supernatants is determined by ELISA. Lenalidomide is assayed in a minimum of three separate experiments. Percent inhibition is determined as 100 × [1 − (cytokine(experimental)/cytokine(control))].
Experimental Result Images Methods Biomarkers Images PMID
Western blot MDM2 / p-MDM2 / p-p53 / p53 phospho-IKKβ / IKKβ 22525275
Growth inhibition assay Cell viability 22698399
In Vivo
In vivo

The induction of angiogenesis by bFGF is significantly inhibited by oral treatment of Lenalidomide in a dose-dependent manner. Lenalidomide significantly decreases the percentage of vascularized area from 5.16% (control group) to 2.58% (50 mg/kg). Lenalidomide significantly reduces the calculated total MVL from 21.07 (control) to 8.11 (50 mg/kg). Lenalidomide significantly inhibites HUVEC migration through the fibronectin-coated membranes towards 0.1 ng/mL of bFGF at 100 μM, 1 ng/mL of VEGF at concentrations of 10 μM and 100 μM. [5]
Animal Research Animal Models Adult male Sprague-Dawley rats bearing HUVECs cells
Dosages 50 mg/kg and 250 mg/kg
Administration Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06177028 Not yet recruiting
Cognitive Impairment Mild|Cognitive Dysfunction|Amyloid Plaque|Neurodegenerative Disease Hereditary|Inflammation Brain
St. Joseph''s Hospital and Medical Center Phoenix|Texas Tech University
 January 2 2024 Phase 2
NCT06149286 Recruiting
Relapsed/Refractory Follicular Lymphoma|Marginal Zone Lymphoma (MZL)
Regeneron Pharmaceuticals
 December 28 2023 Phase 3
NCT06087653 Recruiting
Multiple Myeloma
Starton Therapeutics Inc
 October 2 2023 Phase 1|Phase 2
NCT05626322 Recruiting
Diffuse Large B-Cell Lymphoma
Pfizer|MorphoSys AG|Incyte Corporation
 August 4 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 259.26 Formula

C13H13N3O3
CAS No. 191732-72-6 SDF Download Lenalidomide SDF
Smiles C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 51 mg/mL ( (196.71 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
What is the formulation for mouse injection(i.p.)?

Answer:
This paper has the information you need: http://link.springer.com/article/10.1208/s12248-012-9401-2. Add lenalidomide to the appropriate volume of sterile phosphate-buffered saline (PBS) containing 1% hydrochloric acid (HCl). the pH of this preparation was adjusted to 7.0–7.6 using sodium hydroxide and sterile filtered using a 0.22 μm Steriflip filter.

Question 2:
what is the procedure to resuspend this compound？

Answer:
You can resuspend this compund by DMSO, the solubility is about 52 mg/mL (200.57 mM). For in vivo study, you can prepare the working solution with the vehicle of: 30% PEG400/0.5% Tween80/5% propylene glycol for oral administration.

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