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
1
200mgIn Stock
$39.00
1
500mgIn Stock
$70.00
1
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Descripción (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.

Protocolo (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.

Documentos del producto (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
50-35-1
Sinónimos
N-Phthaloylglutamimide, NSC 66847, NSC 527179
Nombre químico
2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
SMILES
C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
Fórmula molecular
C13H10N2O4
Peso molecular
258.23
Solubilidad
≥ 11.8 mg/mL in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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