Alvespimycin (17-DMAG) HCl

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

仅限科研使用

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。

Alvespimycin (17-DMAG) HCl Chemical Structure

CAS: 467214-21-7

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
大包装

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Alvespimycin (17-DMAG) HCl发表文献57篇:

产品安全说明书

HSP (HSP90)抑制剂选择性比较

相关HSP (HSP90)产品

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 NXXwNoN[S3m2b4TvfIlkcXS7IHHzd4F6 M2PtS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KFONQoKzJINmdGy|LDDJR|UxRTBwMEK0{txONg>? M4fjbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MU[1N|U1Lz5zNkG2OVM2PDxxYU6=
SKBR3 M3KyV2Z2dmO2aX;uJIF{e2G7 MnTZWZBz\We3bHH0bY9vKG:oIFjzdFcxKGmwIGPLRnI{KGOnbHzzMEBGSzVyPUCuNFA1|ryPLh?= MnjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6NUSwOlYoRjF4OEW0NFY3RC:jPh?=
SKBR3 NFHmU5BHfW6ldHnvckBie3OjeR?= MlnXSIVoemGmYYTpc44hd2ZiSHXyNkBqdiCVS1LSN{Bk\WyuczygSWM2OD1yLkCwPO69VS5? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2Okc,OTZ6NUSwOlY9N2F-
SKOV3 NHrMeFlHfW6ldHnvckBie3OjeR?= NVPEbZFiXXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHnuJHNMV1Z|IHPlcIx{NCCHQ{WwQVAvODF2zszNMi=> NGfQV3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNki1OFA3Pid-MU[4OVQxPjZ:L3G+
SKOV3 MnjDSpVv[3Srb36gZZN{[Xl? MonQSIVoemGmYYTpc44hd2ZiSHXyNkBqdiCVS1;WN{Bk\WyuczygSWM2OD1yLkC0Ou69VS5? NXnpVZRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjZpPkG2PFU1ODZ4PD;hQi=>
AGS Mo\YSpVv[3Srb36gZZN{[Xl? M{HhUVE3KGi{cx?= MVLJcohq[mm2aX;uJI9nKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBCT1NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgXCxeHnhMYlv\HWlZXSgcJVkcW[ncnHz[UBmgHC{ZYPzbY9vKGGodHXyJFE3KGi{czDifUBz\XCxcoTldkBie3OjeTygTWM2OD1yLkCzOu69VS5? NFH3XmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W4N|k2OCd-MUe1PFM6PTB:L3G+
Hep3B NH7IfYNHfW6ldHnvckBie3OjeR?= MUWxOkBpenN? NXrHXW91UW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG2JIhzeyCkeTDy[ZBwenSncjDhd5NigSxiSVO1NF0xNjB4Md88UU4> NYLrN5lpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1PFM6PTBpPkG3OVg{QTVyPD;hQi=>
AGS NYW0PGFjTnWwY4Tpc44h[XO|YYm= MUeyOEBpenN? NI\Fe29XcWGkaXzpeJkhd2ZiaIXtZY4hSUeVIHPlcIx{KHWwZHXyJI5wem2xeHnjJINwdmSrdHnvcpMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOu69VS5? M{m2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
NCI-H526 MXfGeY5kfGmxbjDhd5NigQ>? Mni0NUB2VQ>? MlziNlQhcHK| NHXIdoVDcW6maX7nJIFn\mmwaYT5JJRwKEiVUEmwJIlvKGi3bXHuJG5EUS2KNUK2JINmdGy|IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYm= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZyM{W0NEc,OTd4MEO1OFA9N2F-
NCI-H526 NGO0O4dHfW6ldHnvckBie3OjeR?= M3G5UVEhfU1? Ml;rPVYhcHK| MmXrTY5pcWKrdHnvckBw\iCKU2C5NE1u\WSrYYTl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGG2IEGgeW0h[W[2ZYKgPVYhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[Xl? M3fuRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkCzOVQxLz5zN{[wN|U1ODxxYU6=
AGS NH\JT4tHfW6ldHnvckBie3OjeR?= M{fUTWlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBCT1NiY3XscJMh[nlicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkCwN|bPxE1w NHXRZ4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
HeLa MWHGeY5kfGmxbjDhd5NigQ>? NYLKZ5dRUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCqdX3hckBJ\UyjIHPlcIx{NCCLQ{WwQVAvOTYQvF2u MmLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|NUm2N|EoRjF6M{W5OlMyRC:jPh?=
HeLa MUTDfZRwfG:6aXPpeJkh[XO|YYm= M{nYPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTJwMEdOwG0v NHmxfYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
AGS NYfxTm9DS3m2b4TvfIlkcXS7IHHzd4F6 M{HneGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGFIWyClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OTcQvF2u NFu0WJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO1PVY{OSd-MUizOVk3OzF:L3G+
A2058 MW\DfZRwfG:6aXPpeJkh[XO|YYm= NEf6Um5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFIy|ryPLh?= NF3ifHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
MDA-MB-231 MV\GeY5kfGmxbjDhd5NigQ>? MnO3TY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGinckKg[IVoemGmYYTpc44tKEmFNUC9NE4xODR3zszNMi=> MljCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
MDA-MB-231 NFnPdWtEgXSxdH;4bYNqfHliYYPzZZk> MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxPTkQvF2u MmnEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mkm0PFYoRjF6OUK5OFg3RC:jPh?=
A2058 M2TDVWZ2dmO2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJGEzODV6IHPlcIx{NCCHQ{WwQVAvODB5Od88UU4> M{OxeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
MDA-MB-231 MWDGeY5kfGmxbjDhd5NigQ>? NUjrS3psUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IFHreEBl\We{YXTheIlwdixiSVO1NF0xNjBzN{dOwG0v NE\Te2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyPVQ5Pid-MUi5Nlk1QDZ:L3G+
A2058 NV;qXZFZTnWwY4Tpc44h[XO|YYm= M3ztc2lvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNiYYPz[ZN{\WRiYYOgRYt1KGSnZ4Lh[IF1cW:wLDDJR|UxRTBwMEK0N:69VS5? M3THeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUK5OFg3Lz5zOEmyPVQ5PjxxYU6=
HuH7 MmjrRY51cX[rcnHsJIF{e2G7 NY\qZpJ3OyCmYYnz NVmwSFlTSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KENidnnyeZMh\2Wwb4T5dIUhOWJiQ3;uNUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IFfBVGRJKFKQQTDvdkAyQFNicmLORUBt\X[nbDDh[pRmeiB|IHThfZMh[nlicWLUMXBEWiCjbnHsfZNqeyxiRVO1NF0xNjByMUNOwG0v NVzjPIJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5N|YyQTFpPkG4PVM3OTlzPD;hQi=>
HuH7 M1L0UGFvfGm4aYLhcEBie3OjeR?= MoT5N{Bl[Xm| NX;iV4xMSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KENidnnyeZMh\2Wwb4T5dIUhOWJiQ3;uNUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IFfBVGRJKFKQQTDvdkAyQFNicmLORUBt\X[nbDDh[pRmeiB|IHThfZMhe2WuZXP0[YQhf2m2aDC0NEBvVSCKQ2[tO|k3KGGwZDC4NFAhdk1iYn;j[ZBz\X[rcjDifUByWlRvUFPSJIFv[Wy7c3nzMEBGSzVyPUCuNFA{Oc7:TT6= NX65TYtwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5N|YyQTFpPkG4PVM3OTlzPD;hQi=>
SKBR3 NVGxd3hITnWwY4Tpc44h[XO|YYm= M2rWXGJqdmSrbnegZYZncW6rdImgeI8hUHOyOUCgbY4hcHWvYX6gV2tDWjNiY3XscJMtKEmFNUC9NE4xOjUQvF2u Mn7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlyMUe1OlIoRjF7MEG3OVYzRC:jPh?=
Hep3B NWPjXGdLTnWwY4Tpc44h[XO|YYm= Ml3ON|AhdWmwcx?= MWTJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzYXzwbIEheHKxdHXpckBi[2O3bYXsZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgeJJm[XSnZDDmc5IhOzBibXnud{Bu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVAvODV5Mt88UU4> NWjqOW5VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwO|IzOTRpPkG5NFczOjF2PD;hQi=>
Hep3B M2PCR2Z2dmO2aX;uJIF{e2G7 MX2xOkBpenN? MnjHTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhXkWJRjDwdo91\WmwIIPlZ5JmfGmxbjDpckBpfW2jbjDI[ZA{SiClZXzsd{Bi\nSncjCxOkBpenNiYomgSWxKW0FuIFnDOVA:OC5yN{m1{txONg>? NFTCcFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUC3NlIyPCd-MUmwO|IzOTR:L3G+
HCT116 MYHDfZRwfG:6aXPpeJkh[XO|YYm= NGS1e5Y4OiCqcoO= NYL0ZY53S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2wMlA2P87:TT6= NInC[ZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
SKBR3 NWnwZWQ6S3m2b4TvfIlkcXS7IHHzd4F6 M{XD[|czKGi{cx?= M3[4V2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1yLkC1PO69VS5? NHy2WZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzNVg3PCd-MUmyN|E5PjR:L3G+
MCF7 MU\DfZRwfG:6aXPpeJkh[XO|YYm= MXe3NkBpenN? NYLLRpZ3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD6wO|HPxE1w MnLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
SKOV3 MlniR5l1d3SxeHnjbZR6KGG|c3H5 Ml\lO|IhcHK| NVu5WVBIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUCuNVIz|ryPLh?= Mnf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
SKBR3 NGXzcnlEgXSxdH;4bYNqfHliYYPzZZk> MUm3NkBpenN? M4nHZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDpckBxemW|ZX7j[UBw\iCQUV:xJIlvcGmkaYTvdkBlcWOxdX3hdo9tNCCLQ{WwQVAvOjQQvF2u MojXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{G4OlQoRjF7MkOxPFY1RC:jPh?=
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Assay
Methods Test Index PMID
Western blot HSP90 / HSP70 p-Akt / Survivin / MMP2 PARP / Cleaved caspase-3 / Cleaved caspase-8 / Cleaved caspase-9 / PUMA p-ALK / ALK / p-Akt / Akt / p-ERK / ERK α-Tax / α-IKKα / α-IKKβ/ α-NEMO / α-TBK1 / α-p65 / α-p50 28915605 26219569 24109220
Growth inhibition assay Cell proliferation 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]
  • 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]
  • 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。
动物实验:[5]
  • 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

溶解度(25°C)

体外

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 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
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

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

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