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Lenalidomide (CC-5013)

Catalog No.
A4211
Antineoplastic agent,inhibits angiogenesis
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
Evaluation Sample
$28.00
In stock
50mg
$90.00
In stock
100mg
$120.00
In stock
250mg
$150.00
In stock
500mg
$180.00
In stock

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Background

Lenalidomide (also known as CC-5013), an oral derivative of thalidomide, is an antineoplastic agent exhibiting antitumor activity through a variety of mechanisms, including immune system activation, angiogenesis inhibition, and direct antineoplastic effects. It has been extensively studied for the treatment of multiple myeloma and myelodysplastic syndrome as well as lymphoproliferative disorders including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma. According to recent studies, Lnalidomide promotes and restores immune system function in CLL patients by inducing an overexpression of costimulatory molecules in leukemic lymphocytes to restore the humoral immunity and immunoglobulins production as well as improving the ability of T cells and leukemic cells to form synapses with T lymphocytes.

Reference

Ana Pilar Gonzalez-Rodriguez, Angel R. Payer, Andrea Acebes-Huerta, Leticia Hergo-Zapico, Monica Villa-Alvarez, Esther Gonzalez-Garcia, and Segundo Gonzalez. Lenalidomide and chronic lymphocytic leukemia. BioMed Research International 2013.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt259.3
Cas No.191732-72-6
FormulaC13H13N3O3
SynonymsRevlimid,IMiD3,CC 5013,CDC-501,CDC 501
Solubility≥100.8 mg/mL in DMSO,insoluble in EtOH,insoluble in H2O
Chemical Name3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione
SDFDownload SDF
Canonical SMILESC1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment: [1]

Cell lines

Peripheral blood mononuclear cells (PBMCs)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 7 days

Applications

The cells were incubated with the dye at 37°C for 10 min and treated for 7 days in RPMI culture medium with lenalidomide. Cells were surface stained with anti-CD4-PerCP and anti-CD25-APC, followed by intracellular staining with anti-FOXP3-PE. Lenalidomide inhibited the expression of CD4+CD25high CTLA-4+FOXP3+ cells. Incubation with lenalidomide significantly decreases expression of the T regulatory cell population after 7 days of culture. The drug decreased the percentage of CD4+CD25high cells expressing both CTLA-4 and FOXP3 from 25 to 12%.

Animal experiment: [2]

Animal models

Male Sprague–Dawley rats

Dosage form

Oral administration, 50 mg/kg or 250 mg/kg

Applications

In the rat mesenteric window assay (RMWA), representative differences between vehicle and 50 or 250 mg/kg lenalidomide-treated rats were visualized by staining with an antibody against rat endothelium in bFGF-induced angiogenic windows. The induction of angiogenesis by bFGF was significantly inhibited by oral treatment of lenalidomide in a dose-dependent manner. Lenalidomide significantly decreased the percentage of vascularized area from 5.16% in the control group to 2.58 and 1.69 in the 50 and 250 mg/kg group, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Galustian C, Meyer B, Labarthe M C, et al. The anti-cancer agents lenalidomide and pomalidomide inhibit the proliferation and function of T regulatory cells. Cancer Immunology, Immunotherapy, 2009, 58(7): 1033-1045.

[2] Dredge K, Horsfall R, Robinson S P, et al. Orally administered lenalidomide (CC-5013) is anti-angiogenic in vivo and inhibits endothelial cell migration and Akt phosphorylation in vitro. Microvascular research, 2005, 69(1): 56-63.

Biological Activity

Description Lenalidomide (CC-5013) is an inhibitor of TNF-α secretion with IC50 of 13 nM.
Targets TNF-α          
IC50 13 nM          

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