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
今日订购,明日送达 全国免运费 分装免费
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客户使用Selleck生产的Alvespimycin (17-DMAG) HCl发表文献56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 NInwcG5EgXSxdH;4bYNqfHliYYPzZZk> M3nifWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFONQoKzJINmdGy|LDDJR|UxRTBwMEK0{txONg>? NUfqSoZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[xOlU{PTRpPkG2NVY2OzV2PD;hQi=>
SKBR3 M4rlWmZ2dmO2aX;uJIF{e2G7 NEDybIhWeHKnZ4XsZZRqd25ib3[gTJNxPzBiaX6gV2tDWjNiY3XscJMtKEWFNUC9NE4xODUQvF2u M3zmOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
SKBR3 M{nidGZ2dmO2aX;uJIF{e2G7 NHzmdINF\We{YXTheIlwdiCxZjDI[ZIzKGmwIGPLRnI{KGOnbHzzMEBGSzVyPUCuNFA5|ryPLh?= M3e0UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY3Lz5zNki1OFA3PjxxYU6=
SKOV3 NXT1dHRkTnWwY4Tpc44h[XO|YYm= NYfx[GhJXXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHnuJHNMV1Z|IHPlcIx{NCCHQ{WwQVAvODF2zszNMi=> NWrFXHZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjZpPkG2PFU1ODZ4PD;hQi=>
SKOV3 M1rLTWZ2dmO2aX;uJIF{e2G7 NHywVXRF\We{YXTheIlwdiCxZjDI[ZIzKGmwIGPLU3Y{KGOnbHzzMEBGSzVyPUCuNFQ3|ryPLh?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
AGS NV\WPFl3TnWwY4Tpc44h[XO|YYm= Mny1NVYhcHK| NXz5SYFOUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iQVfTJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzNjDodpMh[nlicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xOzcQvF2u M3TURlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
Hep3B M1rLVmZ2dmO2aX;uJIF{e2G7 NWTEeFIyOTZiaILz MUnJcohq[mm2aX;uJI9nKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBJ\XB|QjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBtfWOrZnXyZZNmKGW6cILld5Nqd25iYX\0[ZIhOTZiaILzJIJ6KHKncH;yeIVzKGG|c3H5MEBKSzVyPUCuNFYy|ryPLh?= M3;iW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
AGS NES1bGNHfW6ldHnvckBie3OjeR?= MlrUNlQhcHK| NUW0U2d6XmmjYnnsbZR6KG:oIHj1cYFvKEGJUzDj[YxteyC3bnTldkBvd3Kvb4jpZ{Bkd26maYTpc45{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVbPxE1w M4\YelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
NCI-H526 NYXIV29RTnWwY4Tpc44h[XO|YYm= MV6xJJVO MXKyOEBpenN? MVTCbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gZZN{[Xl? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZyM{W0NEc,OTd4MEO1OFA9N2F-
NCI-H526 MV;GeY5kfGmxbjDhd5NigQ>? MWOxJJVO M{P2bVk3KGi{cx?= NIm4WJdKdmirYnn0bY9vKG:oIFjTVFkxNW2nZHnheIVlKHC{b3zp[oVz[XSrb36gc4YhcHWvYX6gUmNKNUh3Mk[gZ4VtdHNiYYSgNUB2VSCjZoTldkA6PiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeR?= NU\jUlMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe2NFM2PDBpPkG3OlA{PTRyPD;hQi=>
AGS M{fadWZ2dmO2aX;uJIF{e2G7 NUCzNIxIUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCkeTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNFA{Ps7:TT6= MnG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
HeLa M2f5V2Z2dmO2aX;uJIF{e2G7 MYTJcohq[mm2aX;uJI9nKFSQRj3hcJBp[S2rbnT1Z4VlKE6ILXvhdJBiSiCjY4TpeoF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOsJGlEPTB;MD6xOe69VS5? MlX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
HeLa Mn\MR5l1d3SxeHnjbZR6KGG|c3H5 Mm\uR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5yNt88UU4> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN3OU[zNUc,OTh|NUm2N|E9N2F-
AGS NX7TbpdGS3m2b4TvfIlkcXS7IHHzd4F6 MmS0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRWdUKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPs7:TT6= NVvnOVJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOVk3OzFpPkG4N|U6PjNzPD;hQi=>
A2058 NWfNO3dJS3m2b4TvfIlkcXS7IHHzd4F6 NHvGcY1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFIy|ryPLh?= NFnPW|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
MDA-MB-231 NG\OXHFHfW6ldHnvckBie3OjeR?= MlvhTY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGinckKg[IVoemGmYYTpc44tKEmFNUC9NE4xODR3zszNMi=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl{OUS4Okc,OTh7Mkm0PFY9N2F-
MDA-MB-231 MnjQR5l1d3SxeHnjbZR6KGG|c3H5 NVPxfHFLS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMEW4{txONg>? NX6zcmR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
A2058 MX;GeY5kfGmxbjDhd5NigQ>? M17SUGlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNuIFXDOVA:OC5yMEe5{txONg>? M1GzVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
MDA-MB-231 Mn3sSpVv[3Srb36gZZN{[Xl? NXPBSYNvUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IFHreEBl\We{YXTheIlwdixiSVO1NF0xNjBzN{dOwG0v NY\iV4hQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5Nlk1QDZpPkG4PVI6PDh4PD;hQi=>
A2058 M1W3PWZ2dmO2aX;uJIF{e2G7 M{i2N2lvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOgRYt1KGSnZ4Lh[IF1cW:wLDDJR|UxRTBwMEK0N:69VS5? NHPPdJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
HuH7 NIrj[HhCdnSrdnnyZYwh[XO|YYm= MWCzJIRigXN? NYrmRWRtSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KENidnnyeZMh\2Wwb4T5dIUhOWJiQ3;uNUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IFfBVGRJKFKQQTDvdkAyQFNicmLORUBt\X[nbDDh[pRmeiB|IHThfZMh[nlicWLUMXBEWiCjbnHsfZNqeyxiRVO1NF0xNjByMUNOwG0v NInnTo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmzOlE6OSd-MUi5N|YyQTF:L3G+
HuH7 MWDBcpRqfmm{YXygZZN{[Xl? NIHpTnM{KGSjeYO= NFr6cmxCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJ\XCjdHn0bZMhSyC4aYL1d{Bo\W6xdInw[UAy[iCFb36xJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNiR1HQSGghWk6DIH;yJFE5WyC{Ul7BJIxmfmWuIHHmeIVzKDNiZHH5d{B{\WynY4Tl[EB4cXSqIESwJI5OKEiFVj23PVYh[W6mIEiwNEBvVSCkb3PldJJmfmm{IHL5JJFTXC2SQ2KgZY5idHm|aYOsJGVEPTB;MD6wNFMy|ryPLh?= M1PmOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUO2NVkyLz5zOEmzOlE6OTxxYU6=
SKBR3 MVHGeY5kfGmxbjDhd5NigQ>? MlKwRolv\GmwZzDh[oZqdmm2eTD0c{BJe3B7MDDpckBpfW2jbjDTT2JTOyClZXzsd{whUUN3ME2wMlAzPM7:TT6= NXS0fXNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwNVc2PjJpPkG5NFE4PTZ{PD;hQi=>
Hep3B MnuzSpVv[3Srb36gZZN{[Xl? NVvG[3ZSOzBibXnudy=> MWDJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzYXzwbIEheHKxdHXpckBi[2O3bYXsZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgeJJm[XSnZDDmc5IhOzBibXnud{Bu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVAvODV5Mt88UU4> M1XucVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEeyNlE1Lz5zOUC3NlIyPDxxYU6=
Hep3B Mn7HSpVv[3Srb36gZZN{[Xl? MojTNVYhcHK| NFq0W|JKdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCYRVfGJJBzd3SnaX6gd4VkemW2aX;uJIlvKGi3bXHuJGhmeDOEIHPlcIx{KGGodHXyJFE3KGi{czDifUBGVEmVQTygTWM2OD1yLkC3PVXPxE1w M1\qelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MEeyNlE1Lz5zOUC3NlIyPDxxYU6=
HCT116 M3fTV2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1XHS|czKGi{cx?= NWTiXJd2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2wMlA2P87:TT6= NE[zVW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
SKBR3 MlfCR5l1d3SxeHnjbZR6KGG|c3H5 M3nHVlczKGi{cx?= MkjSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMEW4{txONg>? NETYW4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
MCF7 MWrDfZRwfG:6aXPpeJkh[XO|YYm= NX\UVWJmPzJiaILz NVTZcpc5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6wO|HPxE1w MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|MUi2OEc,OTl{M{G4OlQ9N2F-
SKOV3 M2\LcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1P0R|czKGi{cx?= MnW1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTBwMUKy{txONg>? NIL1cIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
SKBR3 M3v4PWN6fG:2b4jpZ4l1gSCjc4PhfS=> MVq3NkBpenN? NHvWeZlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgbY4heHKnc3XuZ4Uhd2ZiTmHPNUBqdmirYnn0c5Ih\Gmlb4XtZZJwdCxiSVO1NF0xNjJ|zszNMi=> NHz3dog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
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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、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
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

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID