Tanespimycin (17-AAG)

Catalog No.S1141 Synonyms: CP127374, NSC-330507, KOS 953

For research use only.

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Tanespimycin (17-AAG) Chemical Structure

CAS No. 75747-14-7

Selleck's Tanespimycin (17-AAG) has been cited by 110 publications

Purity & Quality Control

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Biological Activity

Description Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Features Displays very low toxicity toward normal cells.
Targets
HSP90 [1]
(Cell-free assay)
5 nM
In vitro

17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. [1] 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. [2] In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 NV[z[md5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDZPYZKSzVyPUCuNFAxOzB|IN88US=> NFXYZ4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
IST-MEL1 NYLvbIxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjOTWM2OD1yLkCwNFQxPyEQvF2= NEjnOJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
NCI-SNU-1 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwMECyNFch|ryP MoXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
FADU NVrZW|FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm3bm1KSzVyPUCuNFAzODlizszN M2nUWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
C32 M3PCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXkTWM2OD1yLkCwN|A1KM7:TR?= NFnkSlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
D-566MG NFnZXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzaWVBKSzVyPUCuNFA{QSEQvF2= MnHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
LXF-289 MlvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPjSpdmUUN3ME2wMlAxPDF7IN88US=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
HGC-27 M3TZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC1SGZKSzVyPUCuNFA2OSEQvF2= M2L0e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
RPMI-7951 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwMEC3NVch|ryP MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HSC-3 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\2eGlEPTB;MD6wNFkzQSEQvF2= NFq3VZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
MIA-PaCa-2 NF36e3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z0XGlEPTB;MD6wNVAxQSEQvF2= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
KS-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMEGzOVUh|ryP M{D4XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CAL-51 NFjiUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\ETWhKSzVyPUCuNFE1ODVizszN M3PkS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
MDA-MB-361 NH:1TnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTJRW0xUUN3ME2wMlAyPDl3IN88US=> MmTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
TI-73 NIrrPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm5cGtKSzVyPUCuNFE4QTZizszN Mn\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
AGS MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwMEG5N|gh|ryP NVrrV5hLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-H460 NEe2RphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3qS4kzUUN3ME2wMlAyQTd2IN88US=> MljFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
A204 M1[3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMEKyOFkh|ryP MlrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
CHL-1 M2jBc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O2fGlEPTB;MD6wNlI2OSEQvF2= M1[4TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
DU-4475 NFjCUJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXhTWM2OD1yLkCyNlYyKM7:TR?= M4LXRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CGTH-W-1 NXj2OnJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnuZWNKSzVyPUCuNFI{PDlizszN M1PqVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
HCC2218 MnLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULwXVBCUUN3ME2wMlAzPDl2IN88US=> MmmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
A2780 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor5TWM2OD1yLkCyOVMyKM7:TR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
NCI-H720 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;ZO45KSzVyPUCuNFI2PDZizszN NW\vcJNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-N87 NF:3d4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXoWGhDUUN3ME2wMlAzPTl|IN88US=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CHP-212 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfmVYRKSzVyPUCuNFI3OjhizszN M4C5RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
NCI-H23 NVLKfpZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjwTWM2OD1yLkCyOlY2KM7:TR?= MkXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
D-263MG NGPqNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPRTWM2OD1yLkCyO|g3KM7:TR?= MlPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
ME-180 NWTEbGl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfCfm5CUUN3ME2wMlAzQDlzIN88US=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
SW982 NVHYXnRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXPTWM2OD1yLkCyPVk6KM7:TR?= MojOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
OE19 M2XIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X0bmlEPTB;MD6wN|A4PyEQvF2= NWDOZ29QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
SK-LU-1 NHL2dlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTnT4dzUUN3ME2wMlA{ODh{IN88US=> NVfkUVJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
H4 MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwMEOwPUDPxE1? NX;aOW55RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
HT-144 MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzzVFZ3UUN3ME2wMlA{ODl|IN88US=> NUXBSFc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
SK-UT-1 M{flWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDL[WlKSzVyPUCuNFMyPzhizszN MkXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
D-336MG NXPlPHdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHvTWM2OD1yLkCzN|A6KM7:TR?= NWnwSWhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MDA-MB-175-VII M4LUZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rJVGlEPTB;MD6wN|M2PCEQvF2= MmfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
GAMG MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHlTWM2OD1yLkCzOFM2KM7:TR?= M13XSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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OVCAR-5 M2fsWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMEO0PEDPxE1? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
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VM-CUB-1 NFryOVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMEO2OVch|ryP NWfrPGJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
WM-115 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPrTWM2OD1yLkCzO|YzKM7:TR?= M2nIcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
DSH1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwMEO4NFch|ryP NIXmS4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
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BB65-RCC MoLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[0SY1KSzVyPUCuNVA2PTRizszN MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
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TGBC11TKB M2fsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjROJk4UUN3ME2wMlExQTB|IN88US=> NVrJNnhFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
COLO-679 NHzGfo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwMUGyNVEh|ryP M17aUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
TE-8 NYPVZoJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M12y[2lEPTB;MD6xNVI3PCEQvF2= MoHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SK-MEL-28 NXHqVVBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HZSmlEPTB;MD6xNVMzOSEQvF2= MoXJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SH-4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwMUGzOVYh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
KALS-1 M3nxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHXWZVKUUN3ME2wMlEyOzl|IN88US=> M17pSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
RKO NVK5NXpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXiTWM2OD1yLkGxO|Y1KM7:TR?= NYLOdZlKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
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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
In vivo 17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. [1] Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Hsp90 binding assays:

    Purified native Hsp90 protein or cell lysates from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells in lysis buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) are incubated with various concentrations of 17-AAG for 30 minutes at 4 °C, and then incubated with biotin-GM linked to BioMag streptavidin magnetic beads for 1 hour at 4 °C. Tubes are placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads are washed three times in lysis buffer and heated for 5 minutes at 95 °C in SDS–PAGE sample buffer. Samples are analysed on SDS protein gels, and western blots done using indicated antibodies. Bands in the western blots are quantified using the Bio-rad Fluor-S MultiImager, and the percentage inhibition of binding of Hsp90 to the biotin-GM is calculated. The IC50 reported is the concentration of 17-AAG needed to cause half-maximal inhibition of binding.

Cell Research:[1]
  • Cell lines: BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 5 days
  • Method: Cells are seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μL for 24 hours before the addition of increasing concentrations of 17-AAG that is incubated for 5 days. Viable cell number is determined using the Celltiter 96 AQueous Nonradioactive Cell Proliferation Assay. The value of the background absorbance at 490 nm (A490) of wells not containing cells is subtracted. Percentage of viable cells = (A490 of 17-AAG treated sample/A490 untreated cells) × 100. The IC50 is defined as the concentration that gave rise to 50% viable cell number.
Animal Research:[2]
  • Animal Models: Male nu/nu athymic mice inoculated s.c. with androgen-dependent CWR22 xenograft, and female nu/nu athymic mice inoculated s.c. with androgen-independent xenografts CWR22R and CWRSA6
  • Dosages: ~50 mg/kg
  • Administration: Injection i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+corn oil
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 585.69
Formula

C31H43N3O8

CAS No. 75747-14-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

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

Answer:
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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