Thalidomide
别名: K17 中文名称：沙利度胺
Thalidomide作为一种镇静药，免疫调节剂，也用于研究治疗许多癌症的症状。沙利度胺能够抑制cereblon (CRBN)，它是cullin-4 E3 泛素连接酶复合物CUL4-RBX1-DDB1的一部分。
Thalidomide Chemical Structure
CAS: 50-35-1
产品质控
批次：
纯度：
99.98%
99.98
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| RAW264.7 | Antiinflammatory assay | 10 uM | 3 hrs | Antiinflammatory activity in mouse LPS-activated RAW264.7 cells assessed as ROS scavenging activity at 10 uM pretreated for 3 hrs before LPS challenge measured by decrease in fluorescent intensity by confocal microscopy | 18723357 |
| RAW264.7 | Function assay | 1 uM | 3 hrs | Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 1 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot | 18723357 |
| RAW264.7 | Function assay | 10 uM | 3 hrs | Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot | 18723357 |
| RAW264.7 | Function assay | 10 uM | 3 hrs | Reduction in pERK1/2 expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot | 18723357 |
| Ehrlich ascites carcinoma cells | Toxicity assay | 1.25 mM/kg | 7 days | Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal degeneration of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis | 18951804 |
| Ehrlich ascites carcinoma cells | Toxicity assay | 1.25 mM/kg | 7 days | Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal necrosis of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis | 18951804 |
| BTI-TN-5B1-4 | Function assay | 30 mins | Binding affinity to human CRBN (1 to 442 residues)/N-terminal 6His-tagged human DDB1 (1 to 1140 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells after 30 mins by cy5 probe based fluorescence polarization assay, Kd=0.25μM | 31117518 | |
| HeLa | Function assay | Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50=2.04μM | 17845850 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Thalidomide作为一种镇静药，免疫调节剂，也用于研究治疗许多癌症的症状。沙利度胺能够抑制cereblon (CRBN)，它是cullin-4 E3 泛素连接酶复合物CUL4-RBX1-DDB1的一部分。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Thalidomide必须通过肝脏代谢以形成环氧化物，可能是活性致畸代谢物。[1] Thalidomide选择性地抑制脂多糖和其他激动剂刺激人体单核细胞生产肿瘤坏死因子α（TNF-α）。[2] Thalidomide通过增强mRNA降解发挥其对肿瘤坏死因子α的抑制作用。[3] Thalidomide通过诱导细胞凋亡和G1期生长停滞直接作用在MM细胞系以及抗melphalan, doxorubicin和dexamethasone 的病人的MM细胞。Thalidomide增强塞米松的抗MM活性，而白介素6会抑制其活性。[4] Thalidomide是原代人T细胞在体外的有力协同刺激分子，通过T细胞受体复合物以协同增加白细胞介素-2介导的T细胞增殖和干扰素γ生成。Thalidomide也增加在不存在的CD4 + T细胞的同种异体树突状细胞诱导初级CD8 +细胞毒性T细胞应答。[5] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-p38 / p38 / Acetyl-H4 |
|
17620452 | |
| Immunofluorescence | bFGF VCAM-1/CUL5 / NEDD8 |
|
25053990 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Thalidomide（200 毫克/千克）导致在兔子体内血管化角膜区的抑制，抑制率在三个实验中从30％到51％，抑制率中位数为36％。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06146478 | Completed | Transfusion-dependent Beta-Thalassemia |
Blood Care Clinic|Khyber Medical University Peshawar |
January 25 2022 | Phase 3 |
| NCT04680195 | Unknown status | Chronic Radiation Proctitis |
Sixth Affiliated Hospital Sun Yat-sen University |
December 14 2020 | Phase 2 |
| NCT04469556 | Active not recruiting | Pancreatic Cancer Metastatic|Pancreatic Ductal Adenocarcinoma|Advanced Pancreatic Cancer |
University Health Network Toronto|Johns Hopkins University|Cold Spring Harbor Laboratory|Ontario Institute for Cancer Research|Dana-Farber Cancer Institute|Memorial Sloan Kettering Cancer Center|Stand Up To Cancer |
October 14 2020 | Phase 2 |
化学信息&溶解度
| 分子量 | 258.23 | 分子式 | C13H10N2O4 |
| CAS号 | 50-35-1 | SDF | Download Thalidomide SDF |
| Smiles | C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 51 mg/mL ( (197.49 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
mg/kg
g
μL
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Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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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