Tanespimycin (17-AAG)

For research use only. Not for use in humans.

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

Tanespimycin (17-AAG) Chemical Structure

CAS No. 75747-14-7

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。

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
RMB 10950.03 现货

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客户使用Selleck生产的Tanespimycin (17-AAG)发表文献98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 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 NX34Tnk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMECwN|A{KM7:TR?= NVLBN|QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
IST-MEL1 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMECwOFA4KM7:TR?= NWj0SXdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-SNU-1 NUDSVpA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXu[FVKSzVyPUCuNFAzODdizszN NF60UFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
FADU MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;hPGJKSzVyPUCuNFAzODlizszN NVPGPHJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
C32 NEXsdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwMECzNFQh|ryP M1HQOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
D-566MG Mo\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HkZWlEPTB;MD6wNFM6KM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
LXF-289 NYruNI81T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMEC0NVkh|ryP MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
HGC-27 MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7QTWM2OD1yLkCwOVEh|ryP NYPubJlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
RPMI-7951 NH3Tb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMEC3NVch|ryP MoPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HSC-3 M2\MUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnlOpdKSzVyPUCuNFA6OjlizszN NEG3VYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
MIA-PaCa-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMEGwNFkh|ryP NUP2SnNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
KS-1 MoG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XtUGlEPTB;MD6wNVM2PSEQvF2= NYD3PIM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CAL-51 M2\Rcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPUW2d5UUN3ME2wMlAyPDB3IN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
MDA-MB-361 NFrmTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG4XlI5UUN3ME2wMlAyPDl3IN88US=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
TI-73 NGXGOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwMEG3PVYh|ryP MmPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
AGS M4DNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMEG5N|gh|ryP NX;vR4VCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-H460 NHixZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LL[2lEPTB;MD6wNVk4PCEQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
A204 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TBOGlEPTB;MD6wNlI1QSEQvF2= NGjlVmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
CHL-1 M1LsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPXTWM2OD1yLkCyNlUyKM7:TR?= Ml7CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
DU-4475 NH\sfo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLSXVlKSzVyPUCuNFIzPjFizszN NVzvUHJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CGTH-W-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXyTWM2OD1yLkCyN|Q6KM7:TR?= NF\2S5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
HCC2218 M4fhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrGTWM2OD1yLkCyOFk1KM7:TR?= M2rkd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
A2780 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37NS2lEPTB;MD6wNlU{OSEQvF2= Ml;hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-H720 NUHIVpBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f2e2lEPTB;MD6wNlU1PiEQvF2= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
NCI-N87 MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMEK1PVMh|ryP NVnjSGQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CHP-212 MoXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{G1d2lEPTB;MD6wNlYzQCEQvF2= MoHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-H23 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwMEK2OlUh|ryP NYm4SFlMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
D-263MG MmTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMEK3PFYh|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
ME-180 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P4NWlEPTB;MD6wNlg6OSEQvF2= MkT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SW982 NGnDRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTFdpFpUUN3ME2wMlAzQTl7IN88US=> M3XZSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
OE19 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMEOwO|ch|ryP M2n4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SK-LU-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrzdHZKSzVyPUCuNFMxQDJizszN NHrX[WI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
H4 MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT1eVFnUUN3ME2wMlA{ODlizszN M3;sbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
HT-144 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGGzcFhKSzVyPUCuNFMxQTNizszN NIHHfZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
SK-UT-1 M1LBO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fuNGlEPTB;MD6wN|E4QCEQvF2= M2XyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
D-336MG M1PUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX4WnUxUUN3ME2wMlA{OzB7IN88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
MDA-MB-175-VII MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\INJhpUUN3ME2wMlA{OzV2IN88US=> M4TiVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
GAMG NYjXXnlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nZWGlEPTB;MD6wN|Q{PSEQvF2= NEHse3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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OVCAR-5 NFLBVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL3elVRUUN3ME2wMlA{PDhizszN M1TDb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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CAL-39 MmO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Hyd2lEPTB;MD6wO|c3PiEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
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HT-1080 MnOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLsTWM2OD1yLkC4OFM6KM7:TR?= M4PodlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
OVCAR-8 NVzPSlNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfSTWM2OD1yLkC4OlIzKM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
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M059J Ml\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHGc5I6UUN3ME2wMlA6ODJ5IN88US=> NFnTZVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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EFO-27 NIX1NG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj2TWM2OD1yLkC5PVk4KM7:TR?= NX[1PWZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
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SN12C MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHLNGdKSzVyPUCuNVAyODdizszN M4\1[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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SiHa M33JVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[3cWlEPTB;MD6xNFQ5PiEQvF2= Mn:zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
U251 M1LIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvjWmpKSzVyPUCuNVA2OjVizszN M2TDWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
MMAC-SF NHnGdmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPyTWM2OD1yLkGwOVMyKM7:TR?= Mo\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
BB65-RCC M2nPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfDWGdKSzVyPUCuNVA2PTRizszN NGTZUWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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COLO-679 Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPXOWhKSzVyPUCuNVEzOTFizszN M3m1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
TE-8 NG[0eY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3tOHJKSzVyPUCuNVEzPjRizszN M2P6SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SK-MEL-28 MnO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LRVmlEPTB;MD6xNVMzOSEQvF2= NIfqbYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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MHH-PREB-1 NXTNZ5V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH35fFhKSzVyPUS5MlYxODdizszN MnjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
LATS1 / p-LATS1 / YAP / CTGF; 

PubMed: 25712415     


Effects of 17-AAG on the expression of LATS1, p-LATS1, YAP and CTGF.  The expression levels of YAP and CTGF proteins, indicated by Western blot assay, were down-regulated, while LATS1 was upregulated in a dose-dependent manner in 17-AAG treated groups compared to the untreated group.

Cleaved PARP / Survivin; 

PubMed: 18827603     


Western analysis of expression levels of cleaved PARP and Survivin in MM cell lines. β-Actin served as loading control.

pAKT / pMAPK / pRb; 

PubMed: 18682579     


The phosphorylated states of signaling proteins involved in glioma growth are also affected by 17-AAG treatment.

EGFR / PDGFR / AKT / MAPK / c-RAS; 

PubMed: 18682579     


17-AAG promotes the degradation of HSP90 client proteins that are involved in the pathology of glioblastoma multiforme (GBM). Glioma cell lines were treated with increasing concentrations of 17-AAG for 48 h, and protein lysates were run on Western blots. HSP90 client proteins known to be involved in gliomagenesis showed degradation while nonclient proteins remained unaffected by 17-AAG treatment.

α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin; 

PubMed: 20090920     


Immunoblot analysis of heat shock protein induction. Cells were treated with 17-AAG (1–200 nM, 24 h), or subjected to heat shock (HS: 44°C, 30 min, 24 h recovery) or to MG-132 (MG: 1 µM, 24 h). Cell lysates were prepared and immunoblot analysis was carried out with antibodies against the individual proteins as indicated on the right. Co, untreated control.

25712415 18827603 18682579 20090920
Immunofluorescence
β-catenin / E-cadherin; 

PubMed: 25290150     


Co-localization of β-catenin (Red) and E-cadherin (Green) was observed at the cell-cell junctions (white arrows) both in siCtrl and siCTGF cells after 17-AAG treatment. Scale bar is 20 µm.

YAP / TAZ; 

PubMed: 25290150     


Reduction in cytoplasmic distribution accompanied by increased nuclear localization of YAP/TAZ was more apparent in cells treated with 45 nM 17-AAG (red channel for YAP/TAZ and blue channel for nucleus). Statistical comparisons were performed using one-way Kruskal-Wallis multiple comparison, ***p<0.001 compared with control (0 nM).

STAT3; 

PubMed: 27279418     


Effects of 17-AAG on STAT3 expression of H446 cells. (A) Control group; (B) 3.125 mg/l; (C) 6.25 mg/l. 17-AAG, 17-allylamino-17-demethoxygel-danamycin; STAT3, signal transducer and activator of transcription 3; DAPI, 4′,6-diamidino-2-phenylindole.

25290150 27279418
Growth inhibition assay
Cell viability; 

PubMed: 18682579     


17-AAG inhibits the growth of human glioma cell lines. Human glioma cell lines and a nontumorigenic fibroblast cell line were treated with increasing concentrations of 17-AAG for 4 days, and the effect on cell growth was assessed by a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay. The 50% inhibitory concentration (IC50) of all glioma cell lines ranged from 0.05 to 0.5 μM 17-AAG, as compared to 1.5 μM for the nontumorigenic cells.

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[2]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (170.73 mM)
Water Insoluble
Ethanol ''5 mg/mL
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 粉状
溶于溶剂
别名 CP127374, NSC-330507, KOS 953

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
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

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID