Thalidomide

Catalog No.S1193

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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In DMSO USD 190 In stock
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Thalidomide Chemical Structure

Thalidomide Chemical Structure
Molecular Weight: 258.23

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Thalidomide is available in the following compound libraries:

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Product Description

Biological Activity

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.
Targets TNF-alpha [2]
(Cell-free assay)
In vitro Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite. [1] 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. [2] Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. [3] 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. [4] 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. [5]
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%. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] D'Amato RJ, et al. Proc Natl Acad Sci U S A, 1994, 91(9), 4082-4085.

[2] Sampaio EP, et al. J Exp Med, 1991, 173(3), 699-703.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-05-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02387086 Not yet recruiting NSCLC Bai Jun|Shaanxi Provincial Peoples Hospital May 2015 Phase 2|Phase 3
NCT02387086 Not yet recruiting NSCLC Bai Jun|Shaanxi Provincial Peoples Hospital May 2015 Phase 2|Phase 3
NCT02410694 Not yet recruiting Multiple Myeloma Arbeitsgemeinschaft medikamentoese Tumortherapie April 2015 Phase 2
NCT02410694 Not yet recruiting Multiple Myeloma Arbeitsgemeinschaft medikamentoese Tumortherapie April 2015 Phase 2
NCT02301949 Not yet recruiting Gastrointestinal Bleeding of Unknown Origin|Gastrointestinal Vascular Malformation|Thalidomide Efficiency Zhizheng Ge|Shanghai Jiao Tong University School of Medicine December 2014 Phase 2

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Chemical Information

Download Thalidomide SDF
Molecular Weight (MW) 258.23
Formula

C13H10N2O4

CAS No. 50-35-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 52 mg/mL (201.37 mM)
Ethanol 2 mg/mL (7.74 mM)
Water <1 mg/mL (<1 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.
Chemical Name 2-​(2,​6-​dioxo-​3-​piperidinyl)​-1H-​isoindole-​1,​3(2H)​-​dione

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