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

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客户使用Selleck生产的Alvespimycin (17-DMAG) HCl发表文献48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 NGDuNGhEgXSxdH;4bYNqfHliYYPzZZk> NH3KT29EgXSxdH;4bYNqfHliYXfhbY5{fCCVS1LyN{Bk\WyuczygTWM2OD1yLkCyOO69VS5? MonaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZzNkWzOVQoRjF4MU[1N|U1RC:jPh?=
SKBR3 M3;RWmZ2dmO2aX;uJIF{e2G7 MYnVdJJm\3WuYYTpc44hd2ZiSIPwO|AhcW5iU1vCVlMh[2WubIOsJGVEPTB;MD6wNFTPxE1w NGPZR2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNki1OFA3Pid-MU[4OVQxPjZ:L3G+
SKBR3 NWPKWW5uTnWwY4Tpc44h[XO|YYm= M2HMR2Rm\3KjZHH0bY9vKG:oIFjldlIhcW5iU1vCVlMh[2WubIOsJGVEPTB;MD6wNFjPxE1w M1:3[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
SKOV3 M3TEUWZ2dmO2aX;uJIF{e2G7 M4jvO3VxemWpdXzheIlwdiCxZjDId5A4OCCrbjDTT29XOyClZXzsd{whTUN3ME2wMlAyPM7:TT6= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKOV3 MkL1SpVv[3Srb36gZZN{[Xl? NXXMNW1QTGWpcnHkZZRqd25ib3[gTIVzOiCrbjDTT29XOyClZXzsd{whTUN3ME2wMlA1Ps7:TT6= NXTQNJZvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjZpPkG2PFU1ODZ4PD;hQi=>
AGS M{nOXWZ2dmO2aX;uJIF{e2G7 NHjKdVAyPiCqcoO= NV\Lc3czUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iQVfTJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzNjDodpMh[nlicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xOzcQvF2u M{fnXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
Hep3B Mn7aSpVv[3Srb36gZZN{[Xl? NX\ldGxyOTZiaILz NILVV2NKdmirYnn0bY9vKG:oIFjJSlEh[WO2aY\heIlwdiCrbjDoeY1idiCKZYCzRkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCudXPp[oVz[XOnIHX4dJJme3Orb36gZYZ1\XJiMU[gbJJ{KGK7IILldI9zfGW{IHHzd4F6NCCLQ{WwQVAvODZzzszNMi=> NInXPGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W4N|k2OCd-MUe1PFM6PTB:L3G+
AGS MnLPSpVv[3Srb36gZZN{[Xl? MnXjNlQhcHK| MlqwWoli[mmuaYT5JI9nKGi3bXHuJGFIWyClZXzsd{B2dmSncjDuc5Jud3irYzDjc45lcXSrb37zJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUdOwG0v M4XZS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
NCI-H526 M2TIPGZ2dmO2aX;uJIF{e2G7 NVracZRGOSC3TR?= NIPyXpkzPCCqcoO= M{DBSGJqdmSrbnegZYZncW6rdImgeI8hUFOSOUCgbY4hcHWvYX6gUmNKNUh3Mk[gZ4VtdHNiYYSgNUB2VSCjZoTldkAzPCCqcoOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeR?= NVXQOHl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe2NFM2PDBpPkG3OlA{PTRyPD;hQi=>
NCI-H526 MkfiSpVv[3Srb36gZZN{[Xl? NWmzclRMOSC3TR?= NVfEZnNNQTZiaILz MXTJcohq[mm2aX;uJI9nKEiVUEmwMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25ib3[gbJVu[W5iTlPJMWg2OjZiY3XscJMh[XRiMTD1UUBi\nSncjC5OkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigQ>? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZyM{W0NEc,OTd4MEO1OFA9N2F-
AGS MWrGeY5kfGmxbjDhd5NigQ>? MVzJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzIHHjeIl3[XSrb36gbY4hcHWvYX6gRWdUKGOnbHzzJIJ6KHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMEO2{txONg>? NWS5d5ZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOVk3OzFpPkG4N|U6PjNzPD;hQi=>
HeLa M4TWSWZ2dmO2aX;uJIF{e2G7 NWK3dldsUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCqdX3hckBJ\UyjIHPlcIx{NCCLQ{WwQVAvOTYQvF2u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN3OU[zNUc,OTh|NUm2N|E9N2F-
HeLa MV;DfZRwfG:6aXPpeJkh[XO|YYm= NHHZe5ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjIHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1{LkC2{txONg>? NVzGUJN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOVk3OzFpPkG4N|U6PjNzPD;hQi=>
AGS MX3DfZRwfG:6aXPpeJkh[XO|YYm= MliyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRWdUKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPs7:TT6= NXfCOmxmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOVk3OzFpPkG4N|U6PjNzPD;hQi=>
A2058 M1XhUWN6fG:2b4jpZ4l1gSCjc4PhfS=> MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlA2QCClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMEKx{txONg>? M{jV[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
MDA-MB-231 NH7GXXlHfW6ldHnvckBie3OjeR?= NHy1N5ZKdmirYnn0bY9vKG:oIFjzdFkxKGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiaHXyNkBl\We{YXTheIlwdixiSVO1NF0xNjByNEZOwG0v NWO5c4N1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
MDA-MB-231 MX\DfZRwfG:6aXPpeJkh[XO|YYm= NVrJeXZ7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMEW4{txONg>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
A2058 MVPGeY5kfGmxbjDhd5NigQ>? M2L6SGlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNuIFXDOVA:OC5yMEe5{txONg>? MorUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
MDA-MB-231 Ml3WSpVv[3Srb36gZZN{[Xl? Mmm2TY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KEGtdDDk[Ydz[WSjdHnvckwhUUN3ME2wMlAyPzcQvF2u NH30UFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
A2058 NX3rS2ttTnWwY4Tpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJGEzODV6IHPlcIx{KGG|c3Xzd4VlKGG|IFHreEBl\We{YXTheIlwdixiSVO1NF0xNjB{NEROwG0v M{\QdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
HuH7 M{TtTWFvfGm4aYLhcEBie3OjeR?= NYPmN|N1OyCmYYnz MnzRRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOg[4Vvd3S7cHWgNYIhS2:wMTDpcoZm[3SnZDDpckBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KEeDUFTIJHJPSSCxcjCxPHMhelKQQTDs[ZZmdCCjZoTldkA{KGSjeYOgZpkheVKWLWDDVkBidmGueYPpd{whTUN3ME2wMlAxOTMQvF2u M2q3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
HuH7 MkLJRY51cX[rcnHsJIF{e2G7 M2Tpd|Mh\GG7cx?= MW\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZkBEd25zIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhT0GSRFigVm5CKG:{IEG4V{BzWk6DIHzleoVtKGGodHXyJFMh\GG7czDz[Yxm[3SnZDD3bZRpKDRyIH7NJGhEXi15OU[gZY5lKDhyMDDuUUBjd2OncILleolzKGK7IIHSWE1RS1JiYX7hcJl{cXNuIFXDOVA:OC5yMEOx{txONg>? M{DtRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
SKBR3 MlfOSpVv[3Srb36gZZN{[Xl? NFnr[IZDcW6maX7nJIFn\mmwaYT5JJRwKEi|cEmwJIlvKGi3bXHuJHNMSlJ|IHPlcIx{NCCLQ{WwQVAvODJ2zszNMi=> M4HrVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEG3OVYzLz5zOUCxO|U3OjxxYU6=
Hep3B M33EZ2Z2dmO2aX;uJIF{e2G7 MmjPN|AhdWmwcx?= NUDlTo9vUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNYFteGijIIDyc5RmcW5iYXPjeY12dGG2aX;uJIlvKGi3bXHuJGhmeDOEIHPlcIx{KHS{ZXH0[YQh\m:{IEOwJI1qdnNibXXhd5Vz\WRiYX\0[ZIhOTJiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1yLkC1O|LPxE1w M1fvV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEeyNlE1Lz5zOUC3NlIyPDxxYU6=
Hep3B NWXOXWJsTnWwY4Tpc44h[XO|YYm= Mmr5NVYhcHK| MYHJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBXTUeIIIDyc5RmcW5ic3XjdoV1cW:wIHnuJIh2dWGwIFjldFNDKGOnbHzzJIFnfGW{IEG2JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjB5OUZOwG0v NXTPZll6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwO|IzOTRpPkG5NFczOjF2PD;hQi=>
HCT116 NXHKTndpS3m2b4TvfIlkcXS7IHHzd4F6 M13Sc|czKGi{cx?= MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEW3{txONg>? NY\2XlRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyN|E5PjRpPkG5NlMyQDZ2PD;hQi=>
SKBR3 M4T1eWN6fG:2b4jpZ4l1gSCjc4PhfS=> Mm\VO|IhcHK| MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OC5yNUlOwG0v NFuxc249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
MCF7 NFzhRVVEgXSxdH;4bYNqfHliYYPzZZk> NGK0epI4OiCqcoO= NIjnOXVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1yLkC3Ne69VS5? NG[zVos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
SKOV3 MoLaR5l1d3SxeHnjbZR6KGG|c3H5 MYW3NkBpenN? NF6wbpZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6xNlLPxE1w Mn;MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
SKBR3 M1yzUGN6fG:2b4jpZ4l1gSCjc4PhfS=> M36y[|czKGi{cx?= M4\vc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDpckBxemW|ZX7j[UBw\iCQUV:xJIlvcGmkaYTvdkBlcWOxdX3hdo9tNCCLQ{WwQVAvOjQQvF2u M{jPbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkOxPFY1Lz5zOUKzNVg3PDxxYU6=
MCF7 M1i5W2N6fG:2b4jpZ4l1gSCjc4PhfS=> NYTFb5hzPzJiaILz MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCrbjDwdoV{\W6lZTDv[kBPWU9zIHnubIljcXSxcjDkbYNwfW2jcn;sMEBKSzVyPUCuPFYz|ryPLh?= NWTh[G01RGFidHHy[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
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

技术支持

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID