GLPBio

Thalidomide

Catalog No.: GC17054Purity:>99.50%Synonyms: N-Phthaloylglutamimide, NSC 66847, NSC 527179
COASDSData Sheet
Thalidomide is a non-addictive and non-barbiturate sedative that inhibits cereblon with anti-inflammatory and anti-angiogenic properties.

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Thalidomide
Cas No.: 50-35-1
10mM (in 1mL DMSO)In Stock
$43.00
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200mgIn Stock
$39.00
1
500mgIn Stock
$70.00
1
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Description

Thalidomide is a non-addictive and non-barbiturate sedative that inhibits cereblon with anti-inflammatory and anti-angiogenic properties [1]. Thalidomide binds to GC-rich promoter sites by intercalation and thereby decreases the transcription of IGF-1 and FGF-2 and inhibits angiogenesis to exert the teratogenic effects [2]. Thalidomide has been widely used to alleviate neural inflammation and inhibit the excessive vascularization, growth, and metastasis of tumors[3].

In vitro, Thalidomide treatment for 72 hours significantly inhibited the proliferation of MG-63 cells and U2OS cells, with IC50 values of 94.76µg/ml and 156.61µg/ml, respectively[4]. Thalidomide treatment (150µg/ml) for 12 hours significantly inhibited the formation of tubular structures in ECV 304 cells and induced cytoskeleton reorganization[5]. Thalidomide pretreatment (1mM) for 30 minutes inhibited the NFκB transcriptional activation induced by IL-1β in Caco-2 cells as well as the production of IL-8, and inhibited the nuclear translocation of NFκB and the degradation of IκB[6].

In vivo, Thalidomide treatment via oral administration at a dose of 200mg/kg/day for 30 days significantly inhibited the tumor growth and metastasis of A549 xenograft in mice [7].

References:
[1] Vargesson N. Thalidomide‐induced teratogenesis: History and mechanisms[J]. Birth Defects Research Part C: Embryo Today: Reviews, 2015, 105(2): 140-156.
[2] Stephens T D, Bunde C J W, Fillmore B J. Mechanism of action in thalidomide teratogenesis[J]. Biochemical pharmacology, 2000, 59(12): 1489-1499.
[3] Kim J H, Scialli A R. Thalidomide: the tragedy of birth defects and the effective treatment of disease[J]. Toxicological sciences, 2011, 122(1): 1-6.
[4] Zhu J, Yang Y, Liu S, et al. Anticancer effect of thalidomide in vitro on human osteosarcoma cells[J]. Oncology Reports, 2016, 36(6): 3545-3551.
[5] Tamilarasan K P, Kolluru G K, Rajaram M, et al. Thalidomide attenuates nitric oxide mediated angiogenesis by blocking migration of endothelial cells[J]. BMC Cell Biology, 2006, 7(1): 17.
[6] Jin S H, Kim T I, Han D S, et al. Thalidomide Suppresses the Interleukin 1β‐Induced NFκB Signaling Pathway in Colon Cancer Cells[J]. Annals of the New York Academy of Sciences, 2002, 973(1): 414-418.
[7] Lin Y C, Shun C T, Wu M S, et al. A novel anticancer effect of thalidomide: inhibition of intercellular adhesion molecule-1–mediated cell invasion and metastasis through suppression of nuclear factor-κB[J]. Clinical cancer research, 2006, 12(23): 7165-7173.

Protocol

Cell experiment [1]:

Cell lines

MG-63 cells

Preparation Method

MG-63 cells were grown in Dulbecco's Modified Eagle Medium (DMEM) with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. MG-63 cells (1×104) were seeded into each well of a 96-well plate overnight before Thalidomide treatment. Thalidomide was added to the cells at various concentrations (0, 12.5, 25, 50, 100, 200, and 400µg/ml), and incubated at 37°C in a 5% CO2 incubator for 72h. The cell viability was analyzed.

Reaction Conditions

0, 12.5, 25, 50, 100, 200, and 400µg/ml; 72h

Applications

Thalidomide treatment significantly decreased the cell viability of MG-63 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

BALB/c nude mice

Preparation Method

Female BALB/c nude mice were housed in a specialized animal care facility, in a room with constant temperature (25°C), humidity control, and a 12/12h light/dark cycle with free access to food and water. A549 cells were resuspended in PBS. Subsequently, 1×107 cells in 0.1ml of PBS were injected into the lateral tail vein of 6-week-old nude mice. Two weeks after administration, 100 to 200mm3 tumors were apparent in all mice. Mice were divided into two groups (n=6) and orally received either control vehicle (soy oil) or Thalidomide (200mg/kg/day) suspended in soy oil. Mice were treated every day for 30 days with thalidomide or control vehicle, and tumor growth was measured twice per week with calipers.

Dosage form

200mg/kg/day for 30 days; p.o.

Applications

Thalidomide treatment significantly reduced tumor growth in mice with A549 xenograft.

References:
[1] Zhu J, Yang Y, Liu S, et al. Anticancer effect of thalidomide in vitro on human osteosarcoma cells[J]. Oncology Reports, 2016, 36(6): 3545-3551.
[2] Lin Y C, Shun C T, Wu M S, et al. A novel anticancer effect of thalidomide: inhibition of intercellular adhesion molecule-1–mediated cell invasion and metastasis through suppression of nuclear factor-κB[J]. Clinical cancer research, 2006, 12(23): 7165-7173.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
50-35-1
Synonyms
N-Phthaloylglutamimide, NSC 66847, NSC 527179
Chemical Name
2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
SMILES
C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
Molecular Formula
C13H10N2O4
Molecular Weight
258.23
Solubility
≥ 11.8 mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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