Geldanamycin (NSC 122750)

目录号:S2713 中文名称:格尔德霉素

仅限科研使用

Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂,Kd为1.2 μM,特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。

Geldanamycin (NSC 122750) Chemical Structure

CAS: 30562-34-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3131.63 现货
RMB 1407.44 现货
RMB 5493.81 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Geldanamycin (NSC 122750)发表文献28篇:

产品安全说明书

Antineoplastic and Immunosuppressive Antibiotics抑制剂选择性比较

生物活性

产品描述 Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂,Kd为1.2 μM,特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。
靶点
p185 [4]
(SKBr3 cells)
HSP90 (N-terminal domain) [1]
(Cell-free assay)
HSP90 [1]
(Cell-free assay)
70 nM 0.78 μM(Kd) 1.2 μM(Kd)
体外研究

Geldanamycin结合于Hsp90s (残基1-220) N-末端结构域的ATP结合位点。Geldanamycin剂量依赖性抑制Hsp90的ATPase活性。[1] 在A2780人卵巢细胞系中,Geldanamycin引起剂量依赖性G2期阻滞,并可逆抑制其进入S期。该抑制作用伴随p53的增加,最终证明是p53依赖性的。[2] Geldanamycin引起p185受体蛋白-酪氨酸激酶的泛素化和蛋白酶体降解,IC50为70 nM。[3, 4] Geldanamycin是典型的抗肿瘤试剂,对一组60个人肿瘤细胞系的平均GI50为0.18 μM。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells M4X6OnBzd2yrZnXyZZRqd25iYYPzZZk> MlPQR49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJIxqdmViQUK3PFAtKEmFNUC9N{41KM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTVzNEG0OUc,OTF3MUSxOFU9N2F-
SW620 cell NYHp[nV3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrCVpFKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiClb3zvdoVkfGGuIHPhdoNqdm:vYTDTW|YzOCClZXzsJIxqdmW|LDDJR|UxRTZwMjDuUS=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTZ3OEi3PUc,OTV4NUi4O|k9N2F-
MCF-7 cell MlvTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIHjeFZKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiCkcnXhd5Qh[2GwY3XyJG1ETi15IHPlcIwhdGmwZYOsJGlEPTB;Nj61JI5O NHXjWo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNU[1PFg4QSd-MUW2OVg5Pzl:L3G+
K562 cell M3vtUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTLRYE2UW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5ibHX1b4VucWFiS{W2NkBk\WyuIHzpcoV{NCCLQ{WwQVIzNjFibl2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTZ3OEi3PUc,OTV4NUi4O|k9N2F-
HT-29 cell M2DZ[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHNTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4h[2:ub4LlZ5RidCClYYLjbY5wdWFiSGStNlkh[2WubDDsbY5meyxiSVO1NF0zPC53IH7N NHzoZm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNU[1PFg4QSd-MUW2OVg5Pzl:L3G+
SK-BR-3 NFnBXIxHfW6ldHnvckBie3OjeR?= M2LJUlUxKG2pL3vn NW\IbnA2UW6qaXLpeIlwdiCxZjDvcoNw\2WwZTDwdo9lfWO2IICxPFUh\XKkQj2yJIZzd21iaIXtZY4h[nKnYYP0JINidmOncjDj[YxteyiVSz3CVk0{KGOnbHzzLUBifCB3MDDt[{9s\yCmb4PlMEBKSzVyPUCuNFfPxE1? NHryRXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi95NU[yPVEyLz55NU[yPVEyRC:jPh?=
SK-BR-3 NUHFUlR2TnWwY4Tpc44h[XO|YYm= M3SyNmlvKH[rdILvJIlvcGmkaYTpc44hd2ZicEG4OUBmemKELUKgc45kd3C{b4TlbY4hcW5iaIXtZY4h[nKnYYP0JINidmOncjDTT{1DWi1|IHPlcIx{NCCLQ{WwQVAvODgQvF2= M2LzcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzd3NkK5NVIoRjd3NkK5NVI9N2F-
MCF-7 MVTGeY5kfGmxbjDhd5NigQ>? M1u4UmlvcGmkaYTpc44hd2Zic4TlZYR6NXO2YYTlJIV5eHKnc4Ppc44hd2ZiSFXSNkBqdiCPQ1[tO{BjemWjc4SgZ4Fv[2W{IHPlcIx{NCCLQ{WwQVAvODYQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODN2ME[wOUc,OTB|NEC2NFU9N2F-
MCF-7 MUPGeY5kfGmxbjDhd5NigQ>? NX;yc2NVUW6qaXLpeIlwdiCxZjDzeIVi\Hlvc4TheIUh\XiycnXzd4lwdiCxZjDFVkBqdiCPQ1[tO{BjemWjc4SgZ4Fv[2W{IHPlcIx{NCCLQ{WwQVAvODcQvF2= M4C4VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyM{SwOlA2Lz5zMEO0NFYxPTxxYU6=
MCF-7 MnrVSpVv[3Srb36gZZN{[Xl? MkXJTY5pcWKrdHnvckBw\iC|dHXh[Jkue3SjdHWg[ZhxemW|c3nvckBw\iCUYX[tNUBqdiCPQ1[tO{BjemWjc4SgZ4Fv[2W{IHPlcIx{NCCLQ{WwQVAvOs7:TR?= M1TYS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyM{SwOlA2Lz5zMEO0NFYxPTxxYU6=
SKBR-3 NXK1bodpTnWwY4Tpc44h[XO|YYm= NYq5ZVEyTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36g[o9zKEincj2yJIRm\3KjZHH0bY9vKGmwIGPLRnIuOyClZXzsd{whS2:wY3XueJJifGmxbk21{txO MknUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV5MUO0NVAoRjF3N{GzOFExRC:jPh?=
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LS174T Ml;ER5l1d3SxeHnjbZR6KGG|c3H5 M3;RVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxUOTd2VDDj[YxteyCkeTDNWHMh[XO|YYmsJGlEPTB;MD60Oe69VQ>? NF7ERno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{CzOFE{PSd-MUewN|QyOzV:L3G+
rat neuronal cells MUfDfZRwfG:6aXPpeJkh[XO|YYm= Mkj0NVAhfU1? MXWyOEBpenN? MmrqR5l1d3SxeHnjbZR6KGGpYXnud5QhemG2IH7leZJwdmGuIHPlcIx{KGG2IEGwJJVOKGGodHXyJFI1KGi{cx?= MormQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{N{[2O|koRjF5Mke2Olc6RC:jPh?=
P19 MYHDfZRwfG:6aXPpeJkh[XO|YYm= M2DINFE5KGi{cx?= NUXmWYJjS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDF7IHPlcIx{KGGodHXyJFE5KGi{czygTWM2OD1yLkJOwG0> NEjTdmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S0NlU3PSd-MUe0OFI2PjV:L3G+
MCF7 NXnKS|g4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1n4T2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKg[IF6eyCkeTDTVmIh[XO|YYmsJGdKPTB;M{WuOu69VQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzh4OUC5PEc,OTd6NkmwPVg9N2F-
HCT116 M3r2O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrzWopIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNuIFfJOVA:OC5yMkJOwG0> MnyxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NEO3NFMoRjF6MkSzO|A{RC:jPh?=
DLD1 Mn;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDEUGQyKGOnbHzzMEBIUTVyPUCuNFM4|ryP NU\yOFdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyOFM4ODNpPkG4NlQ{PzB|PD;hQi=>
KPL4 NInCNZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXLHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDLVGw1KGOnbHzzMEBIUTVyPUCuNFU6|ryP M36yUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkSzO|A{Lz5zOEK0N|cxOzxxYU6=
A549 NXWyVJJDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1PKb2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscJMtKEeLNUC9NE4xPjUQvF2= NHPZSJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK0N|cxOyd-MUiyOFM4ODN:L3G+
KPL4 NXfsfFFjTnWwY4Tpc44h[XO|YYm= MYC0NEBpenN? MlK4TY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBMWEx2IHPlcIx{KGG|c3Xzd4VlKGG|IHTldIxmfGmxbjDv[kBGemKEMjDs[ZZmdCCjZoTldkA1OCCqcoOsJG1GSz1yLkGx{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ2M{ewN{c,OTh{NEO3NFM9N2F-
KPL4 Mn\lSpVv[3Srb36gZZN{[Xl? NIiwc4Y1OCCqcoO= NGDjcFhKdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKEuSTESgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVxdGW2aX;uJI9nKFKjZj2xJIxmfmWuIHHmeIVzKDRyIHjyd{whVUWFPUCuN|PPxE1? M4nOTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkSzO|A{Lz5zOEK0N|cxOzxxYU6=
Jurkat M3H1emZ2dmO2aX;uJIF{e2G7 NETQ[2oyKHWP NGK4S3lKdmirYnn0bY9vKG:oIITvJGhUWDlyIHnuJGZCTERiZHXmbYNq\W62IHj1cYFvKEq3cnvheEBk\WyuczDhd5Nme3OnZDDhd{BTUVBicILveIVqdiCmZXfyZYRifGmxbjDheEAyKHWPIHL5JHdme3Sncn6gZoxwfA>? M1LSZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEC4O|E{Lz5zOESwPFcyOzxxYU6=
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SKBR3 M{j4dmZ2dmO2aX;uJIF{e2G7 NVvSelh1OjRiaILz NEjVTYhKdmirYnn0bY9vKG:oIFjzdFkxNW2nZHnheIVlKEiHUkKg[IVoemGmYYTpc44hcW5iaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhzNkGxNUc,OTh6MU[xNVE9N2F-
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体内研究 在FRE/erbB-2 小鼠体内,Geldanamycin (50 mg//kg)对pl85-相关的磷酸酪氨酸水平表现出30%的抑制。[6]

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)

激酶实验:

[1]

  • 核苷结合的等温滴定量热法(ITC):

    滴定实验使用MSC系统进行。在每个实验中,16等份15 μL geldanamycin (300 μM在1% DMSO中)在25 °C下注射到1.3 mL蛋白质(31 μM在20 mMTris-HCl中, pH 7.5, 1 mMEDTA),得到的数据减去稀释热后进行拟合。将geldanamycin加入缓冲液和缓冲液加入蛋白质的稀释热在单独实验中测定。在核苷酸结合位点没有观察到DMSO的结合。滴定数据使用非线性最小二乘法曲线拟合算法拟合,该算法有三个不固定变量:化学计量,结合常数(Kb) 1/Kd),和相互作用焓的变化(ΔH°)。Geldanamycin结合到完整酵母Hsp90和Hsp90 N-末端结构域,估计的解离常数分别为1.22 μM和0.78 μM。结合到C-末端片段时,没有观察到有意义的热量。

细胞实验:

[2]

  • Cell lines: A2780人卵巢癌细胞系
  • Concentrations: 0.001-10 μM
  • Incubation Time: 3小时
  • Method: 指数生长的细胞用Geldanamycin处理,不同时期的DNA合成通过溴脱氧尿苷(BrdUrd)的整合和流式细胞分析术评估。在此期间,处理的和未处理的细胞,总细胞数没有显著的差别。BrdUrd (10 μM)在37 °C下4小时的培育期间进行整合,将细胞采集并固定在70%乙醇中。DNA通过2 N HC1变性后,细胞用抗- BrdUrd小鼠单克隆抗体培育,随后用异硫氰酸荧光素(FITC)-连接的山羊抗-小鼠IgG培育。细胞在室温下用碘化丙啶着色30分钟,使用Coulter EPICS Profile分析器通过流式细胞术分析。
动物实验:

[6]

  • Animal Models: 负荷FRE/erbB-2肿瘤的nu/nu小鼠
  • Dosages: 50 mg/kg
  • Administration: 通过腹腔注射给药

溶解度(25°C)

体外

* 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 560.64
化学式

C29H40N2O9

CAS号 30562-34-6
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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

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,: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: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: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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00003969 Completed Drug: tanespimycin Unspecified Adult Solid Tumor Protocol Specific Cancer Research UK|National Cancer Institute (NCI) August 1998 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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