1. Apoptosis
  2. TNF-alpha

Lenalidomide (Synonyms: CC-5013)

Cat. No.: HY-A0003 Purity: 99.98%
Data Sheet SDS Handling Instructions

Lenalidomide is a potent inhibitor of TNF-α and has antiangiogenic effect.

For research use only. We do not sell to patients.
Lenalidomide Chemical Structure

Lenalidomide Chemical Structure

CAS No. : 191732-72-6

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Other Forms of Lenalidomide:

    Lenalidomide purchased from MCE. Usage Cited in: Nat Commun. 2017 May 22;8:15398.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Lenalidomide is a potent inhibitor of TNF-α and has antiangiogenic effect.

    IC50 & Target

    TNF-α[1]

    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].

    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].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 3.8571 mL 19.2857 mL 38.5713 mL
    5 mM 0.7714 mL 3.8571 mL 7.7143 mL
    10 mM 0.3857 mL 1.9286 mL 3.8571 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [3]

    Lenalidomide is solubilized in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[1].

    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.

    Animal Administration
    [4]

    Lenalidomide is prepared in sterile PBS containing 1% hydrochloric acid (HCl) (Mice)[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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    259.26

    Formula

    C₁₃H₁₃N₃O₃

    CAS No.

    191732-72-6

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 35 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.98%

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