Molecular Weight(MW): 258.23
Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.
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Thalidomide and lenalidomide increase the protein level of WT CRBN. Plasmids expressing FS-CRBN WT were transfected into HEK293T cells and then cells were equally divided into each well of a 6-well plate. The cells were treated with thalidomide (100 µM) or lenalidomide (10 µM) for indicated time.
FASEB Journal, 2015, fj.15-274050. Thalidomide purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
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|Description||Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.|
Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite.  Thalidomide selectively inhibits the production of human monocyte tumor necrosis factor alpha (TNF-alpha) when human monocytes are triggered with lipopolysaccharide and other agonists in culture.  Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation.  Thalidomide acts directly, by inducing apoptosis or G1 growth arrest, in MM cell lines and in patient MM cells that are resistant to melphalan, doxorubicin, and dexamethasone (Dex). Thalidomide enhances the anti-MM activity of Dex and, conversely, are inhibited by interleukin 6.  Thalidomide is a potent costimulator of primary human T cells in vitro, synergizing with stimulation via the T cell receptor complex to increase interleukin 2-mediated T cell proliferation and interferon gamma production. Thalidomide also increases the primary CD8+ cytotoxic T cell response induced by allogeneic dendritic cells in the absence of CD4+ T cells. 
|In vivo||Thalidomide (200 mg/kg) results in an inhibition of the area of vascularized cornea of rabbits that ranged from 30% to 51% in three experiments with a median inhibition of 36%. |
-  D'Amato RJ, et al. Proc Natl Acad Sci U S A, 1994, 91(9), 4082-4085.
-  Sampaio EP, et al. J Exp Med, 1991, 173(3), 699-703.
-  Moreira AL, et al. J Exp Med, 1993, 177(6), 1675-1680.
|In vitro||DMSO||52 mg/mL (201.37 mM)|
|Ethanol||2 mg/mL (7.74 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||5 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02844309||Recruiting||Waldenström Macroglobulinemia||Institute of Hematology & Blood Diseases Hospital||May 2016||Phase 4|
|NCT02733380||Recruiting||Diffuse Large B-cell Lymphoma||Henan Cancer Hospital||May 2016||Phase 2|
|NCT02778893||Recruiting||NSCLC||Henan Provincial Hospital||March 2016||Phase 4|
|NCT02707484||Not yet recruiting||Gastrointestinal Vascular Malformation||Shanghai Jiao Tong University School of Medicine||March 2016||Phase 3|
|NCT02748772||Recruiting||Colorectal Neoplasms||The First Peoples Hospital of Hefei|Anhui Cancer Hospital|Anhui Jimin Cancer Hospital|Simcere Pharmaceutical Co., Ltd||January 2016||Phase 3|
|NCT02301949||Withdrawn||Gastrointestinal Bleeding of Unknown Origin|Gastrointestinal Vascular Malformation|Thalidomide Efficiency||Zhizheng Ge|Shanghai Jiao Tong University School of Medicine||December 2015||Phase 2|
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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