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Thalidomide

別名: K17 中文名稱:沙利度胺

Thalidomide作為一種鎮(zhèn)靜藥,免疫調(diào)節(jié)劑,也用于研究治療許多癌癥的癥狀。沙利度胺能夠抑制cereblon (CRBN),它是cullin-4 E3 泛素連接酶復(fù)合物CUL4-RBX1-DDB1的一部分。

Thalidomide Chemical Structure

Thalidomide Chemical Structure

CAS: 50-35-1

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
200mg 658.37 現(xiàn)貨
1g 2211.3 現(xiàn)貨
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Thalidomide相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Thalidomide作為一種鎮(zhèn)靜藥,免疫調(diào)節(jié)劑,也用于研究治療許多癌癥的癥狀。沙利度胺能夠抑制cereblon (CRBN),它是cullin-4 E3 泛素連接酶復(fù)合物CUL4-RBX1-DDB1的一部分。
靶點(diǎn)
E3 Ligase [6]
(Cell-free assay)
TNF-alpha [2]
(Cell-free assay)
體外研究(In Vitro)
體外研究活性

Thalidomide必須通過肝臟代謝以形成環(huán)氧化物,可能是活性致畸代謝物。[1] Thalidomide選擇性地抑制脂多糖和其他激動(dòng)劑刺激人體單核細(xì)胞生產(chǎn)腫瘤壞死因子α(TNF-α)。[2] Thalidomide通過增強(qiáng)mRNA降解發(fā)揮其對(duì)腫瘤壞死因子α的抑制作用。[3] Thalidomide通過誘導(dǎo)細(xì)胞凋亡和G1期生長(zhǎng)停滯直接作用在MM細(xì)胞系以及抗melphalan, doxorubicin和dexamethasone 的病人的MM細(xì)胞。Thalidomide增強(qiáng)塞米松的抗MM活性,而白介素6會(huì)抑制其活性。[4] Thalidomide是原代人T細(xì)胞在體外的有力協(xié)同刺激分子,通過T細(xì)胞受體復(fù)合物以協(xié)同增加白細(xì)胞介素-2介導(dǎo)的T細(xì)胞增殖和干擾素γ生成。Thalidomide也增加在不存在的CD4 + T細(xì)胞的同種異體樹突狀細(xì)胞誘導(dǎo)初級(jí)CD8 +細(xì)胞毒性T細(xì)胞應(yīng)答。[5]

實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-p38 / p38 / Acetyl-H4 17620452
Immunofluorescence bFGF VCAM-1/CUL5 / NEDD8 25053990
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Thalidomide(200 毫克/千克)導(dǎo)致在兔子體內(nèi)血管化角膜區(qū)的抑制,抑制率在三個(gè)實(shí)驗(yàn)中從30%到51%,抑制率中位數(shù)為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

化學(xué)信息&溶解度

分子量 258.23 分子式

C13H10N2O4

CAS號(hào) 50-35-1 SDF Download Thalidomide SDF
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次:

DMSO : 51 mg/mL ( (197.49 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次:

現(xiàn)配現(xiàn)用,請(qǐng)按從左到右的順序依次添加,澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器(澄清溶液)

第一步:請(qǐng)輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過程中的損耗,建議多配一只動(dòng)物的藥量)

mg/kg g μL

第二步:請(qǐng)輸入動(dòng)物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果:

工作液濃度: mg/ml;

DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,:如該濃度超過該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

體內(nèi)配方配制方法:μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。

體內(nèi)配方配制方法:μL DMSO母液,加入μL Corn oil,混勻澄清。

注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。

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