Tanespimycin (17-AAG)

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

Tanespimycin (17-AAG) Chemical Structure

Molecular Weight(MW): 585.69

Tanespimycin (17-AAG) 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. Phase 2.

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Cited by 56 Publications

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Description Tanespimycin (17-AAG) 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. Phase 2.
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 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXDWpFKSzVyPUCuNFAxOzB|IN88US=> M3qxUHNCVkeHUh?=
IST-MEL1 M3jPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMECwOFA4KM7:TR?= NVv3NXp5W0GQR1XS
NCI-SNU-1 M3\JfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMECyNFch|ryP Ml7UV2FPT0WU
FADU MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwMECyNFkh|ryP M1fMTXNCVkeHUh?=
C32 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LCcmlEPTB;MD6wNFMxPCEQvF2= NYflO|I1W0GQR1XS
D-566MG MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\mOWdKUUN3ME2wMlAxOzlizszN MoT2V2FPT0WU
LXF-289 M{T2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwMEC0NVkh|ryP Mn\GV2FPT0WU
HGC-27 M3[5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrHZ3BKSzVyPUCuNFA2OSEQvF2= M4O0dnNCVkeHUh?=
RPMI-7951 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMEC3NVch|ryP MYHTRW5ITVJ?
HSC-3 M{L6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P2OmlEPTB;MD6wNFkzQSEQvF2= NUHu[lRnW0GQR1XS
MIA-PaCa-2 NYfHXmpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmriTWM2OD1yLkCxNFA6KM7:TR?= MoTIV2FPT0WU
KS-1 M3;qb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHITWM2OD1yLkCxN|U2KM7:TR?= MUDTRW5ITVJ?
CAL-51 NI\DbW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXUTndpUUN3ME2wMlAyPDB3IN88US=> M4i1THNCVkeHUh?=
MDA-MB-361 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwMEG0PVUh|ryP NH\UO3BUSU6JRWK=
TI-73 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPXTWM2OD1yLkCxO|k3KM7:TR?= MYHTRW5ITVJ?
AGS M1;Nbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XqPWlEPTB;MD6wNVk{QCEQvF2= M3jTd3NCVkeHUh?=
NCI-H460 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHHWHQ5UUN3ME2wMlAyQTd2IN88US=> NW\kT4tVW0GQR1XS
A204 NVGxcG9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDQTWM2OD1yLkCyNlQ6KM7:TR?= M36zcXNCVkeHUh?=
CHL-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTTTWM2OD1yLkCyNlUyKM7:TR?= M172SHNCVkeHUh?=
DU-4475 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDoTWM2OD1yLkCyNlYyKM7:TR?= Ml63V2FPT0WU
CGTH-W-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTiXJJpUUN3ME2wMlAzOzR7IN88US=> NIS0WVBUSU6JRWK=
HCC2218 M121bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPiR41KSzVyPUCuNFI1QTRizszN MV3TRW5ITVJ?
A2780 NHvX[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\jW4VKSzVyPUCuNFI2OzFizszN NH34V4pUSU6JRWK=
NCI-H720 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPRWJFSUUN3ME2wMlAzPTR4IN88US=> MlqxV2FPT0WU
NCI-N87 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PXNWlEPTB;MD6wNlU6OyEQvF2= MlHIV2FPT0WU
CHP-212 M3HNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwMEK2Nlgh|ryP NUOydpMzW0GQR1XS
NCI-H23 NX7ucoFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfCW2pKSzVyPUCuNFI3PjVizszN M2PnVHNCVkeHUh?=
D-263MG MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzPb2dXUUN3ME2wMlAzPzh4IN88US=> MmmxV2FPT0WU
ME-180 NWHF[mpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DDS2lEPTB;MD6wNlg6OSEQvF2= NYnNXlNTW0GQR1XS
SW982 NX:5XGhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TBPGlEPTB;MD6wNlk6QSEQvF2= NGrWe4lUSU6JRWK=
OE19 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXRTWM2OD1yLkCzNFc4KM7:TR?= MWnTRW5ITVJ?
SK-LU-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwMEOwPFIh|ryP M3LqTnNCVkeHUh?=
H4 M2DyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj3TWM2OD1yLkCzNFkh|ryP NIqx[pZUSU6JRWK=
HT-144 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEOwPVMh|ryP NIL5c4pUSU6JRWK=
SK-UT-1 NV\WSo1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDvNHNKSzVyPUCuNFMyPzhizszN MYjTRW5ITVJ?
D-336MG MmHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnNdlh7UUN3ME2wMlA{OzB7IN88US=> M{[wTXNCVkeHUh?=
MDA-MB-175-VII Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33qSGlEPTB;MD6wN|M2PCEQvF2= NIPrbZBUSU6JRWK=
GAMG MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMEO0N|Uh|ryP NXThS5gzW0GQR1XS
CP50-MEL-B NVL3Z5E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\vW2lEPTB;MD6wN|Q2KM7:TR?= Mmj6V2FPT0WU
OVCAR-5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jrW2lEPTB;MD6wN|Q5KM7:TR?= M4PafHNCVkeHUh?=
SK-MES-1 NX7p[GZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwMEO2NFYh|ryP NF20[HhUSU6JRWK=
VM-CUB-1 NELxc5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4GwU2lEPTB;MD6wN|Y2PyEQvF2= NXjV[|R1W0GQR1XS
WM-115 Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PXTmlEPTB;MD6wN|c3OiEQvF2= MoXsV2FPT0WU
DSH1 NGHpOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\TOHg6UUN3ME2wMlA{QDB5IN88US=> M4f2cnNCVkeHUh?=
Becker M332T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLweI8zUUN3ME2wMlA{QDh3IN88US=> NWXvWmpLW0GQR1XS
SW962 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwMEO5OFUh|ryP NUXPcGFJW0GQR1XS
TYK-nu MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DuNWlEPTB;MD6wN|k5PSEQvF2= NHjpeJFUSU6JRWK=
HO-1-N-1 NIXOR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPTTWM2OD1yLkC0NFIyKM7:TR?= MV\TRW5ITVJ?
T98G NE\3RW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K4XGlEPTB;MD6wOFExOyEQvF2= MVnTRW5ITVJ?
ACN NFjOU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofhTWM2OD1yLkC0NVYzKM7:TR?= MXPTRW5ITVJ?
SW780 MmnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHDTlNmUUN3ME2wMlA1OjB|IN88US=> NY\sOZd{W0GQR1XS
Detroit562 M3KzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMESyN|kh|ryP NHvhd4FUSU6JRWK=
BB49-HNC NEX6UoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jjT2lEPTB;MD6wOFI1OyEQvF2= M4Pye3NCVkeHUh?=
HN NVXaTG1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwMESyO|Ih|ryP MYrTRW5ITVJ?
H9 NGDuOmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvVVVBKSzVyPUCuNFQ{PzFizszN NH7uO5ZUSU6JRWK=
VA-ES-BJ NF;pUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\VN4pPUUN3ME2wMlA1PDR5IN88US=> M1u0NXNCVkeHUh?=
MEL-JUSO M3X6SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfROmhKSzVyPUCuNFQ1PzVizszN MVvTRW5ITVJ?
BT-474 M{K5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMES1JO69VQ>? Ml72V2FPT0WU
CaR-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S3N2lEPTB;MD6wOFU1QSEQvF2= NGi4ZpBUSU6JRWK=
PSN1 M3;WR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\NTWM2OD1yLkC0OlA{KM7:TR?= MlfOV2FPT0WU
KYSE-510 M1PLTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTBwMES2OFkh|ryP NUH5cppuW0GQR1XS
KP-4 NV:xSJVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojOTWM2OD1yLkC0O|U{KM7:TR?= MVzTRW5ITVJ?
KYSE-410 NYj1OlZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPpbo5[UUN3ME2wMlA1Pzd{IN88US=> M{LVNXNCVkeHUh?=
G-402 M3i5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVL6bWlPUUN3ME2wMlA1Pzh7IN88US=> M4H1PHNCVkeHUh?=
DOK M4Sxbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[0TWlEPTB;MD6wOFkxOiEQvF2= NF7HWI9USU6JRWK=
COR-L88 M2\PWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMES5NVIh|ryP NE\Pe|dUSU6JRWK=
SKG-IIIa NWPYWIpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfVZo9KSzVyPUCuNFQ6QDZizszN MlTIV2FPT0WU
AN3-CA NVrhcJlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f4RWlEPTB;MD6wOUDPxE1? NIHRN3VUSU6JRWK=
SW48 M2Dldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3nUGFEUUN3ME2wMlA2ODN7IN88US=> NX:5dFhoW0GQR1XS
YKG-1 NVjwc4djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXKTWM2OD1yLkC1NFcyKM7:TR?= M4\p[HNCVkeHUh?=
KYSE-150 Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LtVmlEPTB;MD6wOVI{PSEQvF2= M3\4c3NCVkeHUh?=
HuO-3N1 M4XXbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwMEWyN|ch|ryP MX3TRW5ITVJ?
LB1047-RCC NFjWbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVeyfpRPUUN3ME2wMlA2Ojl4IN88US=> M4G1UnNCVkeHUh?=
NCI-H2030 Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDkTWM2OD1yLkC1OFE1KM7:TR?= NF6yVYRUSU6JRWK=
YH-13 M{HTdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMEW3NlIh|ryP MofpV2FPT0WU
5637 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMEW3OEDPxE1? MnPlV2FPT0WU
LOXIMVI M2nSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rkSGlEPTB;MD6wOVg4OiEQvF2= NV;FXGhxW0GQR1XS
GT3TKB MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe1T3BKSzVyPUCuNFU6PDJizszN MkjXV2FPT0WU
TCCSUP MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwMEW5OlQh|ryP MY\TRW5ITVJ?
EPLC-272H NYOwbVFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDseod{UUN3ME2wMlA3OjB3IN88US=> MkeyV2FPT0WU
LU-99A MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwME[yN|ch|ryP M2HURnNCVkeHUh?=
NCI-H1755 NV3GU|NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwME[zOFEh|ryP NW\PR|dKW0GQR1XS
KM12 NHuzPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4iyXWlEPTB;MD6wOlM1QCEQvF2= M{TQUnNCVkeHUh?=
SF295 MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwME[0OVIh|ryP NWDMZ2dWW0GQR1XS
MZ2-MEL M4\0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDlTpFsUUN3ME2wMlA3PTV|IN88US=> MkP6V2FPT0WU
HEC-1 NXzxdZhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDNTWM2OD1yLkC2OVg5KM7:TR?= NGD6eGZUSU6JRWK=
SW684 NGTSdIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Tw[WlEPTB;MD6wOlU6OSEQvF2= M2rMe3NCVkeHUh?=
SF539 M2rCTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3tSmZKSzVyPUCuNFY3QDFizszN NYnhV5M{W0GQR1XS
GMS-10 NIXFWI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\iXWlEPTB;MD6wOlY6QSEQvF2= NVTVOGt6W0GQR1XS
MV-4-11 NF\NVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvFfJRwUUN3ME2wMlA3QDB|IN88US=> NE\DbpJUSU6JRWK=
HT-29 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PFVWlEPTB;MD6wOlkyQSEQvF2= NIDn[|FUSU6JRWK=
23132-87 Ml:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXWPYZKSzVyPUCuNFY6PSEQvF2= Mn72V2FPT0WU
SW620 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLmTWM2OD1yLkC3NFI3KM7:TR?= NXnHepBnW0GQR1XS
HCC1806 NWGzNppyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjKUmVKSzVyPUCuNFcyOzFizszN M1[5OHNCVkeHUh?=
Hs-578-T MoKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnITWM2OD1yLkC3NlA5KM7:TR?= NUnkVWtTW0GQR1XS
A2058 NIXpcpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DmdmlEPTB;MD6wO|IzQCEQvF2= MlX5V2FPT0WU
MEL-HO MnfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37pNGlEPTB;MD6wO|I2PSEQvF2= NEfORWxUSU6JRWK=
HCC2998 MnW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwMEezOFch|ryP M4P1O3NCVkeHUh?=
HuO9 Mn[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TsOWlEPTB;MD6wO|U5QSEQvF2= M{[xOXNCVkeHUh?=
CAL-39 M4TUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMEe3OlYh|ryP NIDyNpRUSU6JRWK=
M14 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTBwMEe5NVMh|ryP MnPRV2FPT0WU
BFTC-909 MlfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XCOWlEPTB;MD6wO|k3QSEQvF2= M3TFe3NCVkeHUh?=
TE-11 M4LDPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwMEe5PVYh|ryP NEHj[lVUSU6JRWK=
TGBC1TKB MnTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLnTWM2OD1yLkC4NFQ{KM7:TR?= MoDnV2FPT0WU
L-363 NIjacW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInKfnVKSzVyPUCuNFgzODZizszN M{i2ZnNCVkeHUh?=
A431 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTrTWM2OD1yLkC4NlEh|ryP NFHTe4dUSU6JRWK=
MKN45 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwMEiyNVkh|ryP MkDlV2FPT0WU
HT-1080 M3HmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwMEi0N|kh|ryP NFfadIFUSU6JRWK=
OVCAR-8 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMEi2NlIh|ryP NV\PVJd{W0GQR1XS
LCLC-97TM1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq1TWM2OD1yLkC4O|I5KM7:TR?= MnPGV2FPT0WU
M059J MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLlRox6UUN3ME2wMlA6ODJ5IN88US=> NETwbnRUSU6JRWK=
SK-MEL-2 NUfJZWJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMEmwOkDPxE1? NVLwOplQW0GQR1XS
TE-1 M1W1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmezTWM2OD1yLkC5NlA1KM7:TR?= NYH0elBnW0GQR1XS
KYSE-180 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\pOHJKSzVyPUCuNFkzPjJizszN MVrTRW5ITVJ?
D-247MG M{jI[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXhSlNKSzVyPUCuNFk1PTVizszN NGjHem5USU6JRWK=
8-MG-BA MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXLdoFKSzVyPUCuNFk1PzJizszN MkjlV2FPT0WU
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NCI-H82 MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO1SHVKSzVyPUeuOFU4ODFizszN Mo\vV2FPT0WU
NCI-H1993 NE\ZVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTdwOEOwOlMh|ryP NEHx[I9USU6JRWK=
RH-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\MXmlEPTB;Nz64OVI1PCEQvF2= M37SZ3NCVkeHUh?=
SW948 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTdwOU[wOFkh|ryP MVfTRW5ITVJ?
CAL-33 M2rYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\GcFk2UUN3ME23Mlk6QTN6IN88US=> Mlr4V2FPT0WU
U-266 MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITmOVRKSzVyPUiuNVU4PzdizszN NWO5VWViW0GQR1XS
CAL-72 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRThwMkCzNkDPxE1? Mm\SV2FPT0WU
SNU-423 MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTlwM{[2OlYh|ryP NGHyVmtUSU6JRWK=
KG-1 NX;TNYh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[5eohxUUN3ME25MlU5PDV4IN88US=> Mlz2V2FPT0WU
HCC1395 MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3vN3FKSzVyPUmuPVI{PTJizszN MUDTRW5ITVJ?
BE-13 NIjYXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfDTWM2OD1zMD64PFkzKM7:TR?= Mmq4V2FPT0WU
MKN7 M3O5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD1TWM2OD1zMD65O|Y2KM7:TR?= MYTTRW5ITVJ?
697 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe2UlJoUUN3ME2xNU4yPDd{IN88US=> MXHTRW5ITVJ?
LU-135 NFrmcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFzLkKzNFch|ryP NYXaXoVYW0GQR1XS
ES7 NV3vWpBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\TXWlEPTB;MUGuN|MyOyEQvF2= MkXkV2FPT0WU
SK-HEP-1 M2XT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfJcFdKSzVyPUGxMlc3PDZizszN NWX0ZVJFW0GQR1XS
BEN NGPJNG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFzLki1NUDPxE1? M121SnNCVkeHUh?=
NCI-H1770 Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF{LkGyOkDPxE1? NF3MNXBUSU6JRWK=
SW13 M4SxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v6ZmlEPTB;MUKuNVU1OSEQvF2= Ml[5V2FPT0WU
MZ1-PC MmTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fhbWlEPTB;MUKuOVQ2OiEQvF2= M4\uNXNCVkeHUh?=
Mo-T MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\yTWM2OD1zMj63OFIyKM7:TR?= M{mwSHNCVkeHUh?=
HLE M{fMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF{LkiyNVUh|ryP NX3mUI9mW0GQR1XS
RCC10RGB M{LnWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\KWmlEPTB;MUOuOlcyKM7:TR?= Mm\RV2FPT0WU
COLO-320-HSR NE[1OZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vt[mlEPTB;MUOuO|M5OSEQvF2= MX;TRW5ITVJ?
BHT-101 MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PkSmlEPTB;MUOuPFM1PSEQvF2= NEnEWm1USU6JRWK=
OCUB-M MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTmTWM2OD1zND6xOlAzKM7:TR?= NVv4SGVSW0GQR1XS
MEG-01 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v6dmlEPTB;MUSuN|cxQCEQvF2= MX\TRW5ITVJ?
RS4-11 NELEeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2e2RmlEPTB;MUSuO|QzKM7:TR?= NYT0cXB6W0GQR1XS
MN-60 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nSTGlEPTB;MUSuO|g6PCEQvF2= MXnTRW5ITVJ?
NCI-H1304 NUGyenNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnybJBKSzVyPUG1MlA1OjVizszN M1P2fHNCVkeHUh?=
Ramos-2G6-4C10 NI\wbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TEWGlEPTB;MUWuNFU5OSEQvF2= MXTTRW5ITVJ?
NCI-H2342 M1vTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF3LkKwOFQh|ryP NVnJe2FYW0GQR1XS
LAN-6 NHPPVFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PsTWlEPTB;MUWuOFQyPCEQvF2= M3LER3NCVkeHUh?=
JVM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP2VnVKSzVyPUG1MlU4PDhizszN M1:ySXNCVkeHUh?=
P30-OHK MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF4LkC2NVQh|ryP NWDMTIpYW0GQR1XS
C-33-A NYDQeXlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF4Lk[yNVQh|ryP NEi1V2ZUSU6JRWK=
RPMI-8866 NVjEXZozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ruT2lEPTB;MU[uPFQ6PiEQvF2= MVzTRW5ITVJ?
NCI-H630 NXHUV45FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjMbIhKSzVyPUG2Mlg2OzdizszN NGrLOlFUSU6JRWK=
KYSE-140 NGHj[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjJTWM2OD1zNz6yNFI5KM7:TR?= M1rDVXNCVkeHUh?=
T84 M4G1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HmbmlEPTB;MUiuPFY6PSEQvF2= M13icXNCVkeHUh?=
KU-19-19 NELHZlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TrPWlEPTB;MUiuPVYxQCEQvF2= NIfjZ5ZUSU6JRWK=
BALL-1 NGTQOWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmwTWM2OD1zOT6zN|k6KM7:TR?= MknmV2FPT0WU
Calu-6 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTF7LkS5NkDPxE1? MknwV2FPT0WU
EGI-1 NYHxXoF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnHT5Y5UUN3ME2xPU42QThizszN MnHqV2FPT0WU
MFH-ino Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF7Lke0OVQh|ryP NH;ySXBUSU6JRWK=
GB-1 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFr6SZdKSzVyPUKwMlM2OzVizszN NF;Tc49USU6JRWK=
NCI-H1693 NWrFNJI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJyLk[1NFUh|ryP MYDTRW5ITVJ?
SW1116 NEjENXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXDTWM2OD1{MD65N|YzKM7:TR?= NHLseZRUSU6JRWK=
H-EMC-SS M2P0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ{LkC0OUDPxE1? NH;a[JpUSU6JRWK=
D-502MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH4Z4lkUUN3ME2yNk45OjZzIN88US=> M1LtNnNCVkeHUh?=
IA-LM MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HQ[GlEPTB;MkOuNlQ6OyEQvF2= M{jxWnNCVkeHUh?=
SW1463 NE\zS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJ|Lke5JO69VQ>? MVLTRW5ITVJ?
JAR NVL5RXFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ2LkOyPVMh|ryP NYXCfJV[W0GQR1XS
HT MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLUTWM2OD1{ND60O|U{KM7:TR?= MYLTRW5ITVJ?
LCLC-103H NY\URmpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XNNmlEPTB;MkSuPFQ1QSEQvF2= MWfTRW5ITVJ?
SNU-449 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTSTWM2OD1{ND64O|QyKM7:TR?= NGjjPGlUSU6JRWK=
KE-37 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TiemlEPTB;MkWuNFkzQCEQvF2= MUDTRW5ITVJ?
NCI-H1623 M1rC[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjHeXpKSzVyPUK3MlE{ODNizszN M13mbnNCVkeHUh?=
MOLT-13 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC3WYFyUUN3ME2yO{4{PTF4IN88US=> NUfkSGV3W0GQR1XS
COLO-741 M2HoNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNzLkOzN|Mh|ryP MlvDV2FPT0WU
NB6 NE[4cm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjIRVNKSzVyPUOyMlI5PzZizszN M4fJO3NCVkeHUh?=
MOLT-16 NVzB[|dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTN|LkCwOVUh|ryP MljBV2FPT0WU
IST-MES1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGCwXZVKSzVyPUO0MlA2PDFizszN M2GyR3NCVkeHUh?=
A4-Fuk MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7zVJc6UUN3ME2zOU4xPjZizszN NHj5e|dUSU6JRWK=
CAL-85-1 NYjMe5V[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vETWlEPTB;M{WuNlgyPyEQvF2= NILrZZRUSU6JRWK=
CCRF-CEM M2nweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXmelJKSzVyPUO3MlE2OzZizszN MWnTRW5ITVJ?
HAL-01 MlvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTN6LkS4PFkh|ryP NU[0dIJpW0GQR1XS
HEL M4PCdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEC5TXdKSzVyPUSzMlM1ODlizszN MnHpV2FPT0WU
EW-1 NFS1VGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH0ZmY1UUN3ME20N{41PzZ6IN88US=> MlfWV2FPT0WU
MDA-MB-231 MoLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\U[2lEPTB;NEWuNVE6QSEQvF2= NEXxN|lUSU6JRWK=
ABC-1 MmDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR4Lki1N|gh|ryP NEHvNHJUSU6JRWK=
NCI-H446 MlHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR6LkWwOVgh|ryP NFnv[ZRUSU6JRWK=
MHH-PREB-1 M3PZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTR7Lk[wNFch|ryP MWHTRW5ITVJ?
DOHH-2 NI[3SHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\GSVZKSzVyPUS5MlY3PTZizszN NFn2TXJUSU6JRWK=
GCT MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzTfZRKSzVyPUS5MlY6PzZizszN MlfoV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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.

pAKT / pMAPK / pRb; 

PubMed: 18682579     


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

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.

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.

20090920 18682579 18827603 25712415
Immunofluorescence
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.

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).

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.

27279418 25290150
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
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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • 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
  • Formulation: Dissolved in DMSO, and diluted in egg phospholipids (EPL) vehicle
  • Dosages: ~50 mg/kg
  • Administration: Injection i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (170.73 mM)
Ethanol 5 mg/mL (8.53 mM)
Water Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 585.69
Formula

C31H43N3O8

CAS No. 75747-14-7
Storage powder
in solvent
Synonyms CP127374,NSC-330507, KOS 953

Bio Calculators

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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

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

HSP (e.g. HSP90) Signaling Pathway Map

HSP (e.g. HSP90) Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID