Thalidomide是一种非成瘾性、非巴比妥类镇静剂，可抑制cereblon蛋白，具有抗炎和抗血管生成特性。
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.
Thalidomide是一种非成瘾性、非巴比妥类镇静剂，可抑制cereblon蛋白，具有抗炎和抗血管生成特性[1]。Thalidomide通过嵌入方式结合到富含GC的启动子区域，从而降低IGF-1和FGF-2的转录，并通过抑制血管生成来发挥致畸作用[2]。Thalidomide已被广泛用于减轻神经炎症，抑制肿瘤的过度血管化、生长和转移[3]。
在体外，Thalidomide处理72小时显著抑制了MG-63细胞和U2OS细胞的增殖，IC50值分别为94.76µg/ml和156.61µg/ml[4]。150µg/ml的Thalidomide处理ECV 304细胞12小时，显著抑制了细胞管状结构的形成，并诱导了细胞骨架重组[5]。1mM的Thalidomide预处理Caco-2细胞30分钟，抑制了IL-1β诱导的NFκB转录激活及IL-8的产生，并抑制了NFκB的核转位和IκB的降解[6]。
在体内，每日口服200mg/kg剂量的Thalidomide，持续30天，显著抑制了小鼠A549异种移植瘤的生长和转移[7]。
| 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 | |
| 别名 | 沙利度胺 | ||
| 化学名 | 2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione | ||
| Canonical SMILES | C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O | ||
| 分子式 | C13H10N2O4 | 分子量 | 258.23 |
| 溶解度 | ≥ 11.8 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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