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Thalidomide
| Product Name | Thalidomide |
| Price: | Inquiry |
| Catalog No.: | CN00218 |
| CAS No.: | 50-35-1 |
| Molecular Formula: | C13H10N2O4 |
| Molecular Weight: | 258.23 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C1CCC(C(=O)N1)N1C(=O)c2c(C1=O)cccc2 |
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| Description | Thalidomide is initially promoted as a sedative, inhibits ereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. |
| Target | Kd: ∼250 nM (CRL4CRBN)[1] |
| In Vitro | Thalidomide is initially promoted as a sedative, has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, and targets ereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM[1]. Thalidomide (50 μg/mL) potentiates the anti-tumor activity of icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells[3]. |
| In Vivo | Thalidomide (100 mg/kg, p.o.) inhibits the collagen deposition, down-regulates the mRNA expression level of α-SMA and collagen I, and significantly reduces the pro-inflammatory cytokines in RILF mice. Thalidomide alleviates RILF via suppression of ROS and down-regulation of TGF-β/Smad pathway dependent on Nrf2 status[2]. Thalidomide (200 mg/kg, p.o.) combined with icotinib shows synergistic anti-tumor effects in nude mice bearing PC9 cells, suppressing tumor growth and promoting tumor death[3]. |
| Cell Assay | THP-1 cells, A549 cells and KYSE30 cells are cultured in RPMI-1640 Medium supplemented with 10% fetal bovine serum and maintained at 37 °C in an atmosphere of 5% CO2 and 95% room air. THP-1 cells is irradiated with a single dose of 4 Gy 6-MV X-ray and treated with or without Thalidomide (0.2 μmol/mL)-containing medium for 48 h after radiation. The concentration of Thalidomide is selected based on the preliminary results[2]. |
| Animal Admin | Mice[2] A total of 24 WT C57BL/6 mice are randomly divided into 4 groups for the experiments (n = 6 in each group): a control group, an irradiated group, a group irradiated along with Thalidomide, and a Thalidomide only group. Based on the preliminary results, 100 mg/kg Thalidomide is used in the experiment. Thalidomide is dissolved in DMSO vehicle. The treatment group receives the indicated dose of Thalidomide in 200 μL by gavage every other day beginning on day 1 for six treatments. The control mice receives 200 μL 0.1% DMSO contained-saline only. The lungs are harvested at 12 weeks after irradiation for the analysis. A total of 20 Nrf2-/- mice are randomly divided into 4 groups for the experiments (n = 5 in each group). The experiment procedures of Nrf2-/- mice are the same as WT C57BL/6 mice. In addition, a total of 30 WT C57BL/6 mice are randomly divided into 5 groups for the subsequent experiments (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. 600 ng and 100 mg/kg are selected as the dose of CDDO-Me and Thalidomide for the experiment, respectively. The treatment group receives the indicated dose of CDDO-Me or Thalidomide in 200 μL by gavage every other day beginning on day 1 for six times. For the combined group of CDDO-Me and Thalidomide, CDDO-Me is delivered in 200 μL by gavage every other day beginning on day 1 for six treatments. Thalidomide is delivered in 200 μL by gavage every other day beginning on day 2 for six treatments[2]. |
| Density | 1.5±0.1 g/cm3 |
| Boiling Point | 509.7±43.0 °C at 760 mmHg |
| Flash Point | 262.1±28.2 °C |
| Exact Mass | 258.064056 |
| PSA | 83.55000 |
| LogP | 0.54 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Storage condition | Store at RT |