Thalidomide (K17)

For research use only. Not for use in humans.

目录号:S1193

Thalidomide (K17) Chemical Structure

CAS No. 50-35-1

沙利度胺作为一种镇静药,免疫调节剂,也用于研究治疗许多癌症的症状。沙利度胺抑制E3泛素连接酶(一种CRBN-DDB1-Cul4A复合物)。

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客户使用Selleck生产的Thalidomide (K17)发表文献26篇:

产品安全说明书

E3 ligase Ligand抑制剂选择性比较

生物活性

产品描述 沙利度胺作为一种镇静药,免疫调节剂,也用于研究治疗许多癌症的症状。沙利度胺抑制E3泛素连接酶(一种CRBN-DDB1-Cul4A复合物)。
靶点
E3 Ligase [6]
(Cell-free assay)
TNF-alpha [2]
(Cell-free assay)
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa NFm3T2FHfW6ldHnvckBie3OjeR?= NEPiVJpKdmirYnn0bY9vKG:oIFnMMVEu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJIJtd2OtaX7nJI9nKHB3MD;wOlUhdnWlbHXhdkB1emGwc3zvZ4F1cW:wLDDJR|UxRTJwMEVOwG0> Mm\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd6NEW4OVAoRjF5OES1PFUxRC:jPh?=
RAW264.7 NH;aWWpCdnSraX7mcIFudWG2b4L5JIF{e2G7 M3qyXFExKHWP MmGzN{BpenN? NXizZVJISW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCvb4Xz[UBNWFNvYXP0bZZifGWmIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IGLPV{B{[2G4ZX7nbY5oKGGldHn2bZR6KGG2IEGwJJVOKHC{ZYTy[YF1\WRiZn;yJFMhcHK|IHLl[o9z\SCOUGOgZ4hidGynbnflJI1m[XO3cnXkJIJ6KGSnY4LlZZNmKGmwIH\seY9z\XOlZX70JIlvfGWwc3n0fUBjgSClb37mc4NidCCvaXPyc5Nkd3C7 NFn5Z2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEeyN|M2Pyd-MUi3NlM{PTd:L3G+
RAW264.7 NWHjRoZ4TnWwY4Tpc44h[XO|YYm= MlLkNUB2VQ>? MUezJIhzew>? MWjS[YR2[3Srb36gbY4hcU6RUzDlfJBz\XO|aX;uJIlvKEySUz3hZ5RqfmG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[XRiMTD1UUBxemW2cnXheIVlKG[xcjCzJIhzeyCkZX\vdoUhVFCVIHPoZYxt\W6pZTDhd5Nme3OnZDDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0 MlTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5MkOzOVcoRjF6N{KzN|U4RC:jPh?=
RAW264.7 MlnySpVv[3Srb36gZZN{[Xl? MUCxNEB2VQ>? MX[zJIhzew>? MXrS[YR2[3Srb36gbY4hcU6RUzDlfJBz\XO|aX;uJIlvKEySUz3hZ5RqfmG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[XRiMUCgeW0heHKndILlZZRm\CCob4KgN{BpenNiYnXmc5JmKEySUzDjbIFtdGWwZ3WgZZN{\XO|ZXSgZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveC=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd{M{O1O{c,OTh5MkOzOVc9N2F-
RAW264.7 NYHl[XdLTnWwY4Tpc44h[XO|YYm= NWjWXlE1OTBidV2= M{jHblMhcHK| M1\IWHJm\HWldHnvckBqdiCyRWLLNU8zKGW6cILld5Nqd25iaX6gUHBUNWGldHn2ZZRm\CCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDheEAyOCC3TTDwdoV1emWjdHXkJIZweiB|IHjyd{Bj\W[xcnWgUHBUKGOqYXzs[Y5o\SCjc4Pld5Nm\CCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2 Mmq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5MkOzOVcoRjF6N{KzN|U4RC:jPh?=
Ehrlich ascites carcinoma cells NFXEU4pVd3irY3n0fUBie3OjeR?= M{LMSFEvOjVibV2vb4c> NGC0PGg4KGSjeYO= M1Pw[HRwgGmlaYT5JIlvKFO5aYPzJIFt[mmwbzDtc5V{\SCkZXHybY5oKG2xdYPlJGVpemyrY3igZZNkcXSnczDjZZJkcW6xbXGgZ4VtdHNiYYPz[ZN{\WRiYYOg[o9k[WxiZHXn[Y5memG2aX;uJI9nKGincHH0c4N6fGW|IITy[YF1\WRiYX\0[ZIhPyCmYYnzJJBwe3RvdIXtc5IhcW2ybHHueIF1cW:wIHH0JFEvOjVibV2vb4ctKHOlIH\vdkA2KGSjeYOgZpkhcGm|dH;wZZRpd2yxZ3njZYwh[W6jbInzbZM> M1;SOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUWxPFA1Lz5zOEm1NVgxPDxxYU6=
Ehrlich ascites carcinoma cells MlfEWI95cWOrdImgZZN{[Xl? M1XkUlEvOjVibV2vb4c> MmDmO{Bl[Xm| M{TUUXRwgGmlaYT5JIlvKFO5aYPzJIFt[mmwbzDtc5V{\SCkZXHybY5oKG2xdYPlJGVpemyrY3igZZNkcXSnczDjZZJkcW6xbXGgZ4VtdHNiYYPz[ZN{\WRiYYOg[o9k[WxibnXjdo9{cXNib3[gbIVx[XSxY4n0[ZMhfHKnYYTl[EBi\nSncjC3JIRigXNicH;zeE11fW2xcjDpcZBt[W62YYTpc44h[XRiMT6yOUBuVS:tZzygd4Mh\m:{IEWg[IF6eyCkeTDobZN1d3CjdHjvcI9ocWOjbDDhcoFtgXOrcx?= M1PEbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUWxPFA1Lz5zOEm1NVgxPDxxYU6=
BTI-TN-5B1-4 MXjGeY5kfGmxbjDhd5NigQ>? M{nifFMxKG2rboO= NIq4U29DcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJGNTSk5iKEGgeI8hPDR{IILld4llfWW|KT;OMZRmem2rbnHsJFZJcXNvdHHn[4VlKGi3bXHuJGRFSjFiKEGgeI8hOTF2MDDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIFLUTU1VVi13QkGtOEBqdnOnY4SgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCleUWgdJJw[mViYnHz[YQh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygT4Q:OC5{Nd88US=> MnO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFzMUe1NVgoRjNzMUG3OVE5RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38 / Acetyl-H4 ; 

PubMed: 17620452     


Thalidomide induces activation of p38 MAPK and acetylation of histone H4. CD34+ cells were cultured in EPO alone medium for 7 days prior to the addition of thalidomide. (A) Cells were treated with different concentrations of thalidomide for 30 minutes. (B) Cells were treated with 100 μM thalidomide for the indicated times. Cellular protein (30 μg) was analyzed by Western blot using phosphorylated p38 MAPK and acetyl-histone H4 antibodies. The membranes were stripped and reprobed with total p38 MAPK and histone H4 antibodies as indicated to confirm that similar amounts of protein extracts were analyzed in each lane.

17620452
Immunofluorescence
bFGF; 

PubMed: 25053990     


Thalidomide regulates bFGF expression and cellular distribution in U266 cells. Immunofluorescence detection of bFGF in U266 cells treated with thalidomide for 4 h. Cellular distribution of bFGF was studied by fluorescence microscopy. DNA was stained with H33258 as a nuclear marker. Magnification, × 630.

VCAM-1/CUL5 / NEDD8 ; 

PubMed: 29746508     


CUL5 and NEDD8 colocalization in control cells treated with thalidomide (50 μg/mL) for 15 and 45 min, respectively. Immunostaining with anti- CUL5 and anti NEDD8 antibodies and nuclear DAPI staining was performed as described in the Methods. Images are of merged pictures from CUL5 staining (FITC-green) and NEDD8 staining (Texas red). Magnification is 40X.

25053990 29746508
体内研究

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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 51 mg/mL (197.49 mM)
Water Insoluble
Ethanol '2 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+1% Tween 80+ddH2O (suspension)
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 258.23
化学式

C13H10N2O4

CAS号 50-35-1
储存条件 粉状
溶于溶剂
别名 N/A

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)
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
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04680195 Not yet recruiting Drug: Thalidomide Chronic Radiation Proctitis Sixth Affiliated Hospital Sun Yat-sen University December 14 2020 Phase 2
NCT02956538 Unknown status Drug: Thalidomide|Drug: placebo(for thalidomide) Crohn Disease Sixth Affiliated Hospital Sun Yat-sen University October 2016 Early Phase 1
NCT02966522 Unknown status Drug: Thalidomide|Drug: Dexamethasone Cardiac Amyloidosis Seoul National University Hospital|CW pharmaceutical company October 2016 Phase 2
NCT02778893 Unknown status Drug: Conmana|Drug: Thalidomide NSCLC Henan Provincial People''s Hospital March 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID