Thalidomide (Synonyms: N-Phthaloylglutamimide, NSC 66847, NSC 527179) |
Katalog-Nr.GC17054
One-Click Copy Product Info
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Thalidomide is a non-addictive and non-barbiturate sedative that inhibits cereblon with anti-inflammatory and anti-angiogenic properties.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 50-35-1
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 50-35-1 | SDF | |
| Überlieferungen | N-Phthaloylglutamimide, NSC 66847, NSC 527179 | ||
| Chemical Name | 2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione | ||
| Canonical SMILES | C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O | ||
| Formula | C13H10N2O4 | M.Wt | 258.23 |
| Löslichkeit | ≥ 11.8 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8725 mL | 19.3626 mL | 38.7252 mL |
| 5 mM | 774.5 μL | 3.8725 mL | 7.745 mL |
| 10 mM | 387.3 μL | 1.9363 mL | 3.8725 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)