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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Thalidomide Chemical Structure

Thalidomide Chemical Structure
Molecular Weight: 258.23

Validation & Quality Control

Quality Control & MSDS

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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.
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

Protocol(Only for Reference)

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02203253 Recruiting Neoplasms China Medical University, China|The First Hospital of Lia  ...more China Medical University, China|The First Hospital of Liaoning Medical University|The First Affiliated Hospital of Dalian Medical University|Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region|Liaoyang Central Hospital|Third Peoples hospital Liaoyang|Petrochemical General Hospital of Liaoyang city| Anshan Tumor Hospital July 2014 Phase 3
NCT01356290 Recruiting Medulloblastoma Medical University of Vienna|Medical University of Graz|M  ...more Medical University of Vienna|Medical University of Graz|Medical University Innsbruck|General Hospital Linz|Salzburger Landeskliniken April 2014 Phase 2
NCT01998971 Recruiting Multiple Myeloma Janssen Research & Development, LLC February 2014 Phase 1
NCT01927718 Recruiting Myeloma M.D. Anderson Cancer Center|Celgene Corporation January 2014 --
NCT01638078 Not yet recruiting Coronary Artery Disease University of Roma La Sapienza January 2014 Phase 4

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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 DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 52 mg/mL (201 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (7 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.

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