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Purity: ≥98%
Thalidomide (trade names Immunoprin, Contergan and Thalomid among others) is a potent immunomodulatory agent and a drug approved in the 1950s. It is frequently employed as the E3 ligase's ligand in the protein degradation technology known as PROTACs (proteolysis targeting chimeras). The drug thalidomide is the representative of the thalidomide class, which is mainly used to treat leprosy complications as well as some cancers, such as multiple myeloma. By the German pharmaceutical company Grunenthal, it was first made available as a sedative and immunomodulatory agent in the 1950s. It is also being researched for use in the treatment of various cancer symptoms. Thalidomide is now frequently utilized as a PROTAC (Proteolysis Targeting Chimera) building block that functions as a ligand for the cereblon E3 ubiquitin ligase. A hetero-bifunctional small molecule is used in the PROTAC technology, and one end of the molecule attracts an E3 ubiquitin ligase while the other end interacts with the target protein. Thalidomide blocks the activity of the CRBN-DDB1-Cul4A complex, an E3 ubiquitin ligase. Thalidomide is an effective costimulator of primary human T cells when used in vitro, enhancing stimulation by the T cell receptor complex and interleukin 2-mediated T cell proliferation as well as interferon gamma production.
| Targets |
E3 Ligase; TNF-alpha
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| Cell Assay |
THP-1 cells, A549 cells, and KYSE30 cells are cultured in RPMI-1640 Medium with 10% fetal bovine serum supplement and kept at 37 °C in a 5% CO2 and 95% room air environment. A single dose of 4 Gy 6-MV X-rays is used to irradiate THP-1 cells, and the cells are then treated for 48 hours with or without medium containing thalidomide 0.2 μmol/mL). Based on the preliminary results[2,] the concentration of Thalidomide is chosen.
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| Animal Protocol |
Mice: For the experiments, a total of 24 WT C57BL/6 mice are divided into 4 groups (n = 6 in each group): a control group, an irradiated group, an irradiated group plus Thalidomide, and a Thalidomide only group. The experiment uses 100 mg/kg of Thalidomide based on the preliminary findings. In a DMSO vehicle, thalidomide is dissolved. Every other day starting on day 1 for six treatments, the treatment group is gavaged with the recommended dose of thalidomide in 200 μL. 200 μL of 0.1% DMSO-containing saline is all that is given to the control mice. For the analysis, the lungs are removed 12 weeks after the radiation treatment. For the experiments, a total of 20 Nrf2-/- mice are divided into 4 groups at random (n = 5 per group). The same as with WT C57BL/6 mice, Nrf2-/- mice undergo the same experimental procedures. For the following experiments, 30 WT C57BL/6 mice are additionally randomly assigned to 5 groups (n = 6 in each group): a control group, an irradiated group, a group irradiated along with CDDO-Me and Thalidomide, a group irradiated along with CDDO-Me, and a group irradiated along with Thalidomide. The experimental CDDO-Me and Thalidomide doses are chosen to be 600 ng and 100 mg/kg, respectively. Every other day starting on day 1, for a total of six times, the treatment group is gavaged with the recommended dose of CDDO-Me or thalidomide in 200 μL. For the combined group receiving CDDO-Me and thalidomide, 200 L of CDDO-Me is administered by gavage every other day starting on day 1 for six treatments. Every other day starting on day 2 for six treatments, thalidomide is administered by gavage in 200 μL .
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| References |
| Molecular Formula |
C13H10N2O4
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| Molecular Weight |
258.23
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| Exact Mass |
258.06406
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| Elemental Analysis |
C, 60.47; H, 3.90; N, 10.85; O, 24.78
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| CAS # |
50-35-1
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| Related CAS # |
(S)-Thalidomide;841-67-8;Thalidomide-d4;1219177-18-0;(R)-Thalidomide;2614-06-4
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| Appearance |
Solid powder
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| SMILES |
C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
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| InChi Key |
UEJJHQNACJXSKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10N2O4/c16-10-6-5-9(11(17)14-10)15-12(18)7-3-1-2-4-8(7)13(15)19/h1-4,9H,5-6H2,(H,14,16,17)
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| Chemical Name |
2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
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| Synonyms |
Nphthaloylglutamimide; alphaphthalimidoglutarimide; Nphthalylglutamic acid imide; US brand names: Synovir; Thalomid; Foreign brand names: Distaval; Contergan; Kevadon; Neurosedyn; Pantosediv; Softenon Talimol; Sedoval K17; Abbreviation: THAL
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol : 5 mg/mL Solubility in Formulation 4: 20 mg/mL (77.45 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 20 mg/mL (77.45 mM) in 10% Tween80 in PBS (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8725 mL | 19.3626 mL | 38.7252 mL | |
| 5 mM | 0.7745 mL | 3.8725 mL | 7.7450 mL | |
| 10 mM | 0.3873 mL | 1.9363 mL | 3.8725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03069326 | Active Recruiting |
Drug: Ruxolitinib Drug: Thalidomide |
Myelofibrosis | Memorial Sloan Kettering Cancer Center |
February 27, 2017 | Phase 2 |
| NCT00098475 | Active Recruiting |
Drug: Thalidomide Drug: Lenalidomide |
DS Stage I Multiple Myeloma DS Stage II Multiple Myeloma |
National Cancer Institute (NCI) |
October 26, 2004 | Phase 3 |
| NCT02891811 | Active Recruiting |
Drug: Carfilzomib Drug: Thalidomide |
Multiple Myeloma | Arbeitsgemeinschaft medikamentoese Tumortherapie |
March 10, 2017 | Phase 2 |
| NCT01661400 | Active Recruiting |
Drug: Thalidomide Drug: Metronomic Cyclophosphamide |
Glioma Wilms Tumor Osteosarcoma |
Washington University School of Medicine |
October 26, 2012 | Phase 1 |
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