Tanespimycin (17-AAG)

目录号:S1141 别名: CP127374, NSC-330507, KOS 953 中文名称:坦螺旋霉素

仅限科研使用

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。

Tanespimycin (17-AAG) Chemical Structure

CAS: 75747-14-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2350.91 现货
RMB 795.18 现货
RMB 2432.97 现货
RMB 6527.43 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Tanespimycin (17-AAG)发表文献115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 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。
特性 17-AAG对正常细胞的毒性很小。
靶点
HSP90 [1]
(Cell-free assay)
5 nM
体外研究

17-AAG是格尔德霉素类似物, 但是与过量表达HER-2的癌细胞 (BT474, N87, SKOV3 和SKBR3)或BT474乳腺细胞衍生的Hsp90亲和力高100多倍,IC50为5-6 nM, 而作用于正常人类原代细胞时,IC50为400-943 nM, 因为肿瘤Hsp90 处于多伴复合体状态,具有高ATP酶活性,而正常细胞Hsp90 处于潜在未结合状态, 且直接与那些细胞中17-AAG毒性相关。[1]17-AAG 引起HER2, HER3, Akt,突变和野生型雄激素受体(AR)降解,导致前列腺细胞如LNCaP, LAPC-4, DU-145,和PC-3中RB依赖的 G1 期生长停顿,IC50为25-45 nM。[2]除了诱导改变野生型BCR-ABL的Ba/F3细胞凋亡, IC50为5.2 μM, 17-AAG还通过诱导野生型和突变型 BCR-ABL蛋白降解,而诱导改变抗 Imatinib Mesylate的 T315I和 E255K BCR-ABL突变型细胞生长,IC50分别为2.3 μM 和 1.0 μM。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPKdHRUUUN3ME2wMlAxODNyMzFOwG0> NUKw[lg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
IST-MEL1 NHHaXHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHyVWRKSzVyPUCuNFAxPDB5IN88US=> NWDUZpl1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-SNU-1 NGfodItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K5Z2lEPTB;MD6wNFIxPyEQvF2= NHLxN4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
FADU M3vPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTDV4VKSzVyPUCuNFAzODlizszN NYjPb5Y4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
C32 NV\Le5FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLJSId{UUN3ME2wMlAxOzB2IN88US=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
D-566MG M4\ETmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofiTWM2OD1yLkCwN|kh|ryP Mn7lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
LXF-289 M4XkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK3TWM2OD1yLkCwOFE6KM7:TR?= MoDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HGC-27 MlP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nMOGlEPTB;MD6wNFUyKM7:TR?= M3yxO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
RPMI-7951 NHf4[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\yTWM2OD1yLkCwO|E4KM7:TR?= MmnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HSC-3 NHPoR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXkXlhKSzVyPUCuNFA6OjlizszN Mkn5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
MIA-PaCa-2 M{Xi[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonVTWM2OD1yLkCxNFA6KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
KS-1 MmXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPMTWM2OD1yLkCxN|U2KM7:TR?= M4HMdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CAL-51 NV\0ZotkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTqWnVKSzVyPUCuNFE1ODVizszN MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
MDA-MB-361 NIHYW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoWzTWM2OD1yLkCxOFk2KM7:TR?= MnLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
TI-73 NETqdItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj0UZZKSzVyPUCuNFE4QTZizszN MnHjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
AGS Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMEG5N|gh|ryP NH3tRWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
NCI-H460 NFPsVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkK5TWM2OD1yLkCxPVc1KM7:TR?= MlXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
A204 MlnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G2ZWlEPTB;MD6wNlI1QSEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CHL-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL0UodIUUN3ME2wMlAzOjVzIN88US=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
DU-4475 Mmn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF20dmFKSzVyPUCuNFIzPjFizszN Ml3nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
CGTH-W-1 M4rPb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLLUo1{UUN3ME2wMlAzOzR7IN88US=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
HCC2218 MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV6yZ3BzUUN3ME2wMlAzPDl2IN88US=> Mn71QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
A2780 M4Wyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMEK1N|Eh|ryP NHfJbYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
NCI-H720 MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHQTWM2OD1yLkCyOVQ3KM7:TR?= NV7nN|B3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-N87 NET1WoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMEK1PVMh|ryP M3nOS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CHP-212 NGfwNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfvO5hbUUN3ME2wMlAzPjJ6IN88US=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
NCI-H23 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYizVZk2UUN3ME2wMlAzPjZ3IN88US=> NIDyc4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
D-263MG Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwMEK3PFYh|ryP NH:5OWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
ME-180 M2PzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUOxeJRyUUN3ME2wMlAzQDlzIN88US=> M1L6RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SW982 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jybGlEPTB;MD6wNlk6QSEQvF2= NIC4SnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
OE19 M4jRZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfJTWM2OD1yLkCzNFc4KM7:TR?= M4DlW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SK-LU-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm1U3dKSzVyPUCuNFMxQDJizszN MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
H4 NFLQbI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3QTWM2OD1yLkCzNFkh|ryP NXj2PJAzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
HT-144 M2\5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMEOwPVMh|ryP MnjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SK-UT-1 M3jQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLETWM2OD1yLkCzNVc5KM7:TR?= MkLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
D-336MG NIT3[|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXwNnhKSzVyPUCuNFM{ODlizszN Ml3EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
MDA-MB-175-VII NVLMcJdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS1UGlKSzVyPUCuNFM{PTRizszN M4jSS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
GAMG MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3THbmlEPTB;MD6wN|Q{PSEQvF2= NFTiTYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
CP50-MEL-B MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXPUIFKSzVyPUCuNFM1PSEQvF2= NWi4OW05RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
OVCAR-5 M3nOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMEO0PEDPxE1? Mk\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SK-MES-1 NVu2RWhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HXUmlEPTB;MD6wN|YxPiEQvF2= MoL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
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PANC-03-27 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;5TWM2OD1yLkGwNlg3KM7:TR?= M{CyPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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MMAC-SF NF;oWHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT3TWM2OD1yLkGwOVMyKM7:TR?= NFrm[HM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
BB65-RCC MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnJXZNKUUN3ME2wMlExPTV2IN88US=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
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SK-MEL-28 NH7tV|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\Se29jUUN3ME2wMlEyOzJzIN88US=> MlnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
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MDA-MB-231 MknkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjKVHFKSzVyPUS1MlEyQTlizszN NH3GVGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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MHH-PREB-1 NIDvXm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXsbWxKSzVyPUS5MlYxODdizszN NGjxW|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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GCT NF3sWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\JUGlEPTB;NEmuOlk4PiEQvF2= NGPNXY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
Assay
Methods Test Index PMID
Western blot LATS1 / p-LATS1 / YAP / CTGF Cleaved PARP / Survivin pAKT / pMAPK / pRb EGFR / PDGFR / AKT / MAPK / c-RAS α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin 25712415 18827603 18682579 20090920
Immunofluorescence β-catenin / E-cadherin YAP / TAZ STAT3 25290150 27279418
Growth inhibition assay Cell viability 18682579
体内研究 17-AAG作用于携带3T3-src, B16或CT26移植瘤裸鼠,与Hsp90结合具有高亲和力,IC50为8-35 nM,而作用于正常组织时,IC50为200-600 nM。[1] 17-AAG按50 mg/kg左右剂量处理,引起AR, HER2, HER3, 和 Akt表达明显降低,降低达50%以上,这种作用存在剂量依赖性,结果导致雄激素依赖型 (CWR22)和非依赖型(CWR22R 和CWRSA6) 前列腺移植瘤生长受抑制,抑制率分别为67%, 80%和 68%。[2]

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]
  • Hsp90结合实验:

    纯化的Hsp90蛋白或过量表达HER-2的癌细胞(BT474, N87, SKOV3 和 SKBR3) 裂解物或BT474乳腺癌细胞溶于溶解buffer(20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) ,与不同浓度17-AAG在4oC下温育30分钟,然后和生物素-GM链接的BioMag链霉亲和素磁珠在4oC下温育1小时。试管放置于磁架上,除去未结合的上清液。在溶解buffer中清洗三次磁珠,然后在SDS–PAGE 样本缓冲液中在95oC下加热5分钟。在SDS蛋白凝胶上进行样本分析,使用特点抗体进行Western Blotting。使用Bio-rad Fluor-S 多重图像测量Western Blot条带,计算抑制Hsp90与生物素-GM结合的百分数。测定IC50。

细胞实验:[1]
  • Cell lines: BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, 和 PBMC
  • Concentrations: 溶于DMSO, 终浓度为10 μM 左右
  • Incubation Time: 5天
  • Method: 细胞按每孔2000个接种在96孔板上,终培养体积为100 μL,培养24小时, 然后加入浓度不断增高的17-AAG,温育5天。使用 Celltiter 96 AQueous 非放射性细胞增殖检测试剂盒测定存活细胞数。测定IC50。
动物实验:[2]
  • Animal Models: 皮下注射雄激素依赖性CWR22移植瘤的雄性 nu/nu 无胸腺小鼠, 皮下注射雄激素非依赖性的CWR22R和CWRSA6移植瘤的雌性nu/nu 无胸腺小鼠。
  • Dosages: 50 mg/kg 左右
  • Administration: 腹膜注射

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):
5%DMSO+corn oil

10mg/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 585.69
化学式

C31H43N3O8

CAS号 75747-14-7
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
NCT00103272 Terminated Drug: tanespimycin|Drug: bortezomib Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia National Cancer Institute (NCI) April 2005 Phase 1
NCT00098488 Terminated Drug: tanespimycin|Biological: rituximab B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia National Cancer Institute (NCI) April 2005 Phase 1
NCT00118248 Completed Drug: tanespimycin Recurrent Thyroid Cancer|Stage IV Follicular Thyroid Cancer|Stage IV Papillary Thyroid Cancer|Thyroid Gland Medullary Carcinoma National Cancer Institute (NCI) December 2004 Phase 2
NCT00098423 Completed Drug: tanespimycin|Drug: cytarabine Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts in Transformation|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes National Cancer Institute (NCI) November 2004 Phase 1

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

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常见问题及建议解决方法

问题 1:
What kind of subtypes does this compound inhibit? HSP90α or HSP90β ?

回答:
17-AAG can inhibit both HSP90α and HSP90β, but it is unclear how much are they affected respectively. You should note that Hsp90 derived from tumor cells has a 100-fold higher binding affinity for 17-AAG than that from normal cells according to this paper. http://www.nature.com.ezp-prod1.hul.harvard.edu/nature/journal/v425/n6956/full/nature01913.html

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