Alvespimycin (17-DMAG) HCl

For research use only. Not for use in humans.

目录号：S1142 别名： NSC 707545,BMS 826476 HCl,KOS 1022 中文名称：阿螺旋霉素盐酸盐

Alvespimycin (17-DMAG) HCl Chemical Structure

CAS No. 467214-21-7

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2351.34 现货
RMB 794.94 现货
RMB 2432.56 现货
大剂量询单

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客户使用Selleck生产的Alvespimycin (17-DMAG) HCl发表文献50篇：

产品安全说明书

HSP (HSP90)抑制剂选择性比较

生物活性

产品描述 Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。
特性 17-DMAG是抗生素Geldanamycin 的合成衍生物，比现有抗生素具有较低的肝毒性，比相似衍生物17-AAG效果和有效性更强。
靶点
HSP90 [1]
(Cell-free assay)
62 nM
体外研究

荧光偏振（FP）为基础的竞争性结合实验中，17-DMAG作用于人类 Hsp90比 17-AAG（IC50 为 119 nM）效果高2倍，IC50为 62 nM。17-DMAG作用于过量表达Hsp90“服务蛋白” Her2的SKBR3和 SKOV3细胞,下调Her2，EC50分别为8 nM和 46 nM, 且诱导 Hsp70，EC50分别为 4 nM和 14 nM,结果产生显著的毒性，GI50分别为 29 nM 和32 nM。[1] 17-DMAG和 Vorinostat 联用，通过显著降低cyclin D1和CDK4, 及c-Myc, c-RAF 和AKT水平，协同诱导培养的MCL细胞和原发性 MCL 细胞凋亡。[3]17-AAG 只有效作用于慢性淋巴细胞白血病 (CLL) 细胞的IKKβ，而17-DMAG 处理，有效导致Hsp90 客户蛋白IKKα 和 IKKβ的消耗,导致 NF-κB p50/p65 DNA结合减少，NF-κB 靶基因转录降低，及caspase依赖性凋亡降低。通过靶向作用于NF-κB 家族，17-DMAG作用于CLL细胞而不是正常T细胞或NK细胞，选择性调节毒性，这种作用存在剂量和时间依赖性。[5]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKBr3 MWXDfZRwfG:6aXPpeJkh[XO|YYm= NWTTdlhKS3m2b4TvfIlkcXS7IHHnZYlve3RiU1vCdlMh[2WubIOsJGlEPTB;MD6wNlTPxE1w M{DSOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MU[1N|U1Lz5zNkG2OVM2PDxxYU6=
SKBR3 M1S1bmZ2dmO2aX;uJIF{e2G7 MV;VdJJm\3WuYYTpc44hd2ZiSIPwO|AhcW5iU1vCVlMh[2WubIOsJGVEPTB;MD6wNFTPxE1w Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6NUSwOlYoRjF4OEW0NFY3RC:jPh?=
SKBR3 M4HSR2Z2dmO2aX;uJIF{e2G7 MXHE[Ydz[WSjdHnvckBw\iCKZYKyJIlvKFONQmKzJINmdGy|LDDFR|UxRTBwMEC4{txONg>? MnrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6NUSwOlYoRjF4OEW0NFY3RC:jPh?=
SKOV3 NFHVe5dHfW6ldHnvckBie3OjeR?= NIjFc5pWeHKnZ4XsZZRqd25ib3[gTJNxPzBiaX6gV2tQXjNiY3XscJMtKEWFNUC9NE4xOTUQvF2u MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKOV3 M1LOUmZ2dmO2aX;uJIF{e2G7 MnjMSIVoemGmYYTpc44hd2ZiSHXyNkBqdiCVS1;WN{Bk\WyuczygSWM2OD1yLkC0Ou69VS5? M17xW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
AGS M1frNGZ2dmO2aX;uJIF{e2G7 M2\GelE3KGi{cx?= MUDJcohq[mm2aX;uJI9nKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBCT1NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgXCxeHnhMYlv\HWlZXSgcJVkcW[ncnHz[UBmgHC{ZYPzbY9vKGGodHXyJFE3KGi{czDifUBz\XCxcoTldkBie3OjeTygTWM2OD1yLkCzOu69VS5? NV;rZoxPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1PFM6PTBpPkG3OVg{QTVyPD;hQi=>
Hep3B M1\YTmZ2dmO2aX;uJIF{e2G7 NXLsTnI6OTZiaILz M2PtemlvcGmkaYTpc44hd2ZiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEincEPCJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzNjDodpMh[nlicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xPjIQvF2u NFPhO5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W4N|k2OCd-MUe1PFM6PTB:L3G+
AGS MX7GeY5kfGmxbjDhd5NigQ>? MmriNlQhcHK| MYrWbYFjcWyrdImgc4YhcHWvYX6gRWdUKGOnbHzzJJVv\GW{IH7vdo1wgGmlIHPvcoRqfGmxboOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zNt88UU4> NWXWb3JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1PFM6PTBpPkG3OVg{QTVyPD;hQi=>
NCI-H526 NWnac21JTnWwY4Tpc44h[XO|YYm= MWqxJJVO NUD5UYVFOjRiaILz M1fyXWJqdmSrbnegZYZncW6rdImgeI8hUFOSOUCgbY4hcHWvYX6gUmNKNUh3Mk[gZ4VtdHNiYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeR?= MojvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4MEO1OFAoRjF5NkCzOVQxRC:jPh?=
NCI-H526 NUfYdlNyTnWwY4Tpc44h[XO|YYm= NVLrUo1TOSC3TR?= NHrnSXQ6PiCqcoO= MnzzTY5pcWKrdHnvckBw\iCKU2C5NE1u\WSrYYTl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGG2IEGgeW0h[W[2ZYKgPVYhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[Xl? M1HxSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkCzOVQxLz5zN{[wN|U1ODxxYU6=
AGS MVPGeY5kfGmxbjDhd5NigQ>? NXO4WXJUUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCkeTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNFA{Ps7:TT6= M2i3V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{W5OlMyLz5zOEO1PVY{OTxxYU6=
HeLa MlvQSpVv[3Srb36gZZN{[Xl? NF;6WWhKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIlvKGi3bXHuJGhmVGFiY3XscJMtKEmFNUC9NE4yPc7:TT6= NEDBSpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
HeLa MojlR5l1d3SxeHnjbZR6KGG|c3H5 MlHMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5yNt88UU4> MlzZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
AGS MlTRR5l1d3SxeHnjbZR6KGG|c3H5 NV\DeFdHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSUeVIHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1zNt88UU4> MkPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
A2058 MU\DfZRwfG:6aXPpeJkh[XO|YYm= NXWxc4hJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJyNUigZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFAzOc7:TT6= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
MDA-MB-231 M2DWdWZ2dmO2aX;uJIF{e2G7 NYDsZlBWUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IHjldlIh\GWpcnHkZZRqd25uIFnDOVA:OC5yMES1{txONg>? NYHxUlg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
MDA-MB-231 MVHDfZRwfG:6aXPpeJkh[XO|YYm= NWfB[3dLS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMEW4{txONg>? NHnqOJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
A2058 MnnuSpVv[3Srb36gZZN{[Xl? NInYRpVKdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKEF{MEW4JINmdGy|LDDFR|UxRTBwMEC3Pe69VS5? NGnx[209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
MDA-MB-231 NEjFbZZHfW6ldHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMhSWu2IHTl[5Ji\GG2aX;uMEBKSzVyPUCuNFE4Ps7:TT6= NU\lcYY5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
A2058 NGr5dmlHfW6ldHnvckBie3OjeR?= NGfRcY5KdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKEF{MEW4JINmdGy|IHHzd4V{e2WmIHHzJGFsfCCmZXfyZYRifGmxbjygTWM2OD1yLkCyOFPPxE1w NYDHcXJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
HuH7 MVLBcpRqfmm{YXygZZN{[Xl? MUSzJIRigXN? MknpRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOg[4Vvd3S7cHWgNYIhS2:wMTDpcoZm[3SnZDDpckBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KEeDUFTIJHJPSSCxcjCxPHMhelKQQTDs[ZZmdCCjZoTldkA{KGSjeYOgZpkheVKWLWDDVkBidmGueYPpd{whTUN3ME2wMlAxOTMQvF2u NHHLXYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmzOlE6OSd-MUi5N|YyQTF:L3G+
HuH7 NFzW[4hCdnSrdnnyZYwh[XO|YYm= M2H2W|Mh\GG7cx?= MWDBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZkBEd25zIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhT0GSRFigVm5CKG:{IEG4V{BzWk6DIHzleoVtKGGodHXyJFMh\GG7czDz[Yxm[3SnZDD3bZRpKDRyIH7NJGhEXi15OU[gZY5lKDhyMDDuUUBjd2OncILleolzKGK7IIHSWE1RS1JiYX7hcJl{cXNuIFXDOVA:OC5yMEOx{txONg>? NYrvOm1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5N|YyQTFpPkG4PVM3OTlzPD;hQi=>
SKBR3 NGS4[JlHfW6ldHnvckBie3OjeR?= NGqwfoVDcW6maX7nJIFn\mmwaYT5JJRwKEi|cEmwJIlvKGi3bXHuJHNMSlJ|IHPlcIx{NCCLQ{WwQVAvODJ2zszNMi=> NF7qem49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUCxO|U3Oid-MUmwNVc2PjJ:L3G+
Hep3B MljkSpVv[3Srb36gZZN{[Xl? MUGzNEBucW6| MojTTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhUEmIMXHsdIhiKHC{b4TlbY4h[WOldX31cIF1cW:wIHnuJIh2dWGwIFjldFNDKGOnbHzzJJRz\WG2ZXSg[o9zKDNyIH3pcpMhdWWjc4Xy[YQh[W[2ZYKgNVIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0xNjB3N{NOwG0v MoLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlyN{KyNVQoRjF7MEeyNlE1RC:jPh?=
Hep3B M1fqOmZ2dmO2aX;uJIF{e2G7 NX3UfYlwOTZiaILz M13LZmlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKF[HR1[gdJJwfGWrbjDz[YNz\XSrb36gbY4hcHWvYX6gTIVxO0JiY3XscJMh[W[2ZYKgNVYhcHK|IHL5JGVNUVODLDDJR|UxRTBwMEe5Oe69VS5? NWOwV4F6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwO|IzOTRpPkG5NFczOjF2PD;hQi=>
HCT116 M4ThPWN6fG:2b4jpZ4l1gSCjc4PhfS=> MW[3NkBpenN? M1jWd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6wOVfPxE1w M1;5XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkOxPFY1Lz5zOUKzNVg3PDxxYU6=
SKBR3 MXrDfZRwfG:6aXPpeJkh[XO|YYm= NGDSUXU4OiCqcoO= MlzVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEW4{txONg>? MnHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
MCF7 Mn\ZR5l1d3SxeHnjbZR6KGG|c3H5 NH;oUXM4OiCqcoO= MkTFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OC5yN{JOwG0v M{HGUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkOxPFY1Lz5zOUKzNVg3PDxxYU6=
SKOV3 NEPTZo9EgXSxdH;4bYNqfHliYYPzZZk> NFTKfXE4OiCqcoO= M1X0S2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1yLkGyNu69VS5? NYfIRYFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN|E5PjRpPkG5NlMyQDZ2PD;hQi=>
SKBR3 M{TCNmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVm3NkBpenN? MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhVlGRMTDpcohq[mm2b4Kg[Ilkd3WvYYLvcEwhUUN3ME2wMlI{|ryPLh?= NYmyS|dlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN|E5PjRpPkG5NlMyQDZ2PD;hQi=>
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... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
HSP90 / HSP70 ; 

PubMed: 28915605     


Western blot analysis showing dose-dependent elevation of Hsp70 and HSP90 levels in AGS cells by 17-DMAG.

p-Akt / Survivin / MMP2 ; 

PubMed: 28915605     


Western blot analysis showing the dose-dependent reduction of the expression of HSP90 client proteins, such as p-Akt, survivin, and MMP2 by 17-DMAG.

PARP / Cleaved caspase-3 / Cleaved caspase-8 / Cleaved caspase-9 / PUMA ; 

PubMed: 28915605     


(C-D) 17-DMAG effects on the expression of apoptotic proteins (PARP, c-caspase 3, c-caspase-8, c-caspase-9, and PUMA) in AGS cells. Western blot analyses indicate that 17-DMAG significantly increased the expression of apoptotic proteins in AGS cells in a dose- (C) and time- (D) dependent manner (P < 0.05).

p-ALK / ALK / p-Akt / Akt / p-ERK / ERK ; 

PubMed: 26219569     


Modulation of ALK signaling in parental and 17-DMAG-resistant cells. Cells were treated with the indicated concentrations of 17-DMAG or AUY922 for 6 h. The molecules of ALK-related signaling activity were detected by western blot analysis.

α-Tax / α-IKKα / α-IKKβ/ α-NEMO / α-TBK1 / α-p65 / α-p50 ; 

PubMed: 24109220     


C8166, MT-2, and MT-4 cells were treated with 17-DMAG as indicated, and cell lysates were subjected to immunoblotting with the indicated antibodies.

28915605 26219569 24109220
Growth inhibition assay
Cell proliferation ; 

PubMed: 28915605     


Proliferation assay of AGS cells treated with graded concentrations of 17-DMAG for 24 h or 48 h. 17-DMAG resulted in significant dose- and time-dependent reduction of AGS cell proliferation (P < 0.05)

28915605
体内研究 17-DMAG按5 mg/kg 或 25 mg/kg处理，每周三次，显著降低 TMK-1 移植瘤生长，通过显著降低血管面积和增殖肿瘤细胞数。[2]与抑制FAK信号一致，17-DMAG 按 25 mg/kg剂量处理小鼠，每周三次，显著抑制肿瘤生长，及ME180 和SiHa 移植瘤的转移。[4]17-DMAG 按10 mg/kg 剂量处理TCL1-SCID移植鼠模型，处理16天，显著降低白细胞数，且延长寿命。[5]

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]
- 合并

荧光偏振（FP）为基础的竞争性结合实验:

实验使用氟化硼亚甲基二吡咯(BODIPY)标记的Geldanamycin类似物 (BODIPY-AG) 作为探针，根据探针与蛋白结合情况，测定荧光偏振。从 HeLa细胞中分离活性人类Hsp90 蛋白 (α + β 亚型)。 BODIPY-AG 溶液在FP 实验 buffer (20 mM HEPES-KOH, pH 7.3, 1.0 mM EDTA, 100 mM KCl, 5.0 mM MgCl2, 0.01% NP-40, 0.1 mg/mL 新鲜牛γ-球蛋白 (BGG), 1.0 mM 新鲜DTT,和蛋白酶抑制剂，溶于)中新鲜制备。通过10 μL每组含 BODIPY-AG 和Hsp90的溶液，与连续稀释的 17-DMAG（在 FP 实验 buffer中新鲜制备）混合，而获得竞争性曲线。终浓度为10 nM BODIPY-AG, 40 或 60 nM Hsp90,不同浓度 17-DMAG (0.10 nM-10 μM), 和 ≤0.25% DMSO 在384孔板中混合。30oC下温育3小时后, 在EnVision 2100多标记酶标仪上测定荧光 各向异性(γEx = 485 nm, γEm = 535 nm) 。从竞争曲线中获得17-DMAG的IC50值。
细胞实验：[5]
- 合并
  • Cell lines: 慢性淋巴细胞白血病(CLL)
  • Concentrations: 溶于DMSO,终浓度为~1 μM
  • Incubation Time: 24, 或48小时
  • Method: 使用不同浓度17-DMAG 处理细胞24,或48小时。为了测量毒性, 加如MTT试剂，实验板再温育24小时，然后使用分光光度法测量。通过膜联蛋白 V-异硫氰酸荧光素和碘化丙啶(PI)染色测定凋亡。
    (Only for Reference)
动物实验：[5]
- 合并
  • Animal Models: 移植TCL1 白血病细胞的SCID小鼠
  • Dosages: 10 mg/kg
  • Administration: 腹腔注射，每周5次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 131 mg/mL (200.54 mM)
Water Insoluble
Ethanol Insoluble
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)：
1% DMSO+30% polyethylene glycol+1% Tween 80
 30 mg/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 653.21
化学式

C32H48N4O8•HCl
CAS号 467214-21-7
储存条件 粉状
溶于溶剂
别名 NSC 707545,BMS 826476 HCl,KOS 1022

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 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
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、MSDS / 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、MSDS / 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
NCT00780000 Terminated Drug: Alvespimycin Breast Cancer Bristol-Myers Squibb April 2008 Phase 2
NCT00248521 Unknown status Drug: alvespimycin hydrochloride Unspecified Adult Solid Tumor Protocol Specific Institute of Cancer Research United Kingdom|National Cancer Institute (NCI) October 2005 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

  • 选择性强的HSP90抑制剂

    NVP-BEP800 : HSP90β-selective, IC50=58 nM.

  • 活性最高的HSP90抑制剂

    KW-2478 : HSP90, IC50=3.8 nM.

  • 用于临床的HSP90抑制剂

    17-AAG (Tanespimycin) : Phase III for Gastrointestinal Stromal Tumors.

  • 最新的HSP90抑制剂

    XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

相关HSP (HSP90)产品

  • PU-H71 New

    PU-H71 (NSC 750424)是有效的选择性HSP90抑制剂，IC50为51 nM。

  • KNK437 New

    KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。

  • VER155008 New

    VER155008 (C07)是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78 (HSPA5, Bip) 的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。VER155008 可抑制自噬并导致HSP90客户蛋白水平降低。

  • Tanespimycin (17-AAG)

    Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。

    Features:17-AAG对正常细胞的毒性很小。

  • Luminespib (NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922, VER-52296)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。

  • Ganetespib (STA-9090)

    Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。

  • Geldanamycin (NSC 122750)

    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)。

  • HSP990 (NVP-HSP990)

    HSP990 (NVP-HSP990) 是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。

  • Elesclomol (STA-4783)

    Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。

  • Onalespib (AT13387)

    Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID