Tanespimycin (17-AAG)

For research use only. Not for use in humans.

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

56 publications

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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Selleck's Tanespimycin (17-AAG) has been 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 Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f1PGlEPTB;MD6wNFA{ODNizszN NUfQXHBOW0GQR1XS
IST-MEL1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i1e2lEPTB;MD6wNFA1ODdizszN MXXTRW5ITVJ?
NCI-SNU-1 MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG0c5VTUUN3ME2wMlAxOjB5IN88US=> MlzXV2FPT0WU
FADU M2jFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rDSWlEPTB;MD6wNFIxQSEQvF2= MlfOV2FPT0WU
C32 NHTCO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\BcVBKSzVyPUCuNFA{ODRizszN NVfFRoNSW0GQR1XS
D-566MG MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnVTWM2OD1yLkCwN|kh|ryP MXLTRW5ITVJ?
LXF-289 NEHicW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXPTWM2OD1yLkCwOFE6KM7:TR?= MYXTRW5ITVJ?
HGC-27 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;rRY9KSzVyPUCuNFA2OSEQvF2= MWfTRW5ITVJ?
RPMI-7951 NUCzSFh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjlcWk4UUN3ME2wMlAxPzF5IN88US=> NUTPVHhzW0GQR1XS
HSC-3 M4XNXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzhTWM2OD1yLkCwPVI6KM7:TR?= NUnCNnRUW0GQR1XS
MIA-PaCa-2 NYnFWXhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwMEGwNFkh|ryP NVzwOplnW0GQR1XS
KS-1 NGrvdplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMEGzOVUh|ryP MX7TRW5ITVJ?
CAL-51 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPtVGJKSzVyPUCuNFE1ODVizszN M3fRd3NCVkeHUh?=
MDA-MB-361 M131d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr4TWM2OD1yLkCxOFk2KM7:TR?= MUfTRW5ITVJ?
TI-73 MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMEG3PVYh|ryP MoXWV2FPT0WU
AGS NX61RZl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH3TWM2OD1yLkCxPVM5KM7:TR?= NH\jOZFUSU6JRWK=
NCI-H460 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwMEG5O|Qh|ryP NYPlcFlKW0GQR1XS
A204 NXL2XFd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwMEKyOFkh|ryP NGnG[phUSU6JRWK=
CHL-1 M1nUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMEKyOVEh|ryP M320PHNCVkeHUh?=
DU-4475 MlHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XZXWlEPTB;MD6wNlI3OSEQvF2= MoXDV2FPT0WU
CGTH-W-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHZTWM2OD1yLkCyN|Q6KM7:TR?= MlnxV2FPT0WU
HCC2218 M32zTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTncYZGUUN3ME2wMlAzPDl2IN88US=> MnyxV2FPT0WU
A2780 Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;wNIlyUUN3ME2wMlAzPTNzIN88US=> NVuzOo9XW0GQR1XS
NCI-H720 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnRR3ZKSzVyPUCuNFI2PDZizszN M3vJOHNCVkeHUh?=
NCI-N87 M4ToVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSx[GFiUUN3ME2wMlAzPTl|IN88US=> NWS1c5J5W0GQR1XS
CHP-212 NXn2ZYhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzIXI1KSzVyPUCuNFI3OjhizszN NH3nVZhUSU6JRWK=
NCI-H23 NWLZUZRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1yLkCyOlY2KM7:TR?= NITQe5VUSU6JRWK=
D-263MG NF:y[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3XNZUyUUN3ME2wMlAzPzh4IN88US=> NVu0cIU5W0GQR1XS
ME-180 M1HBOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX0WpJLUUN3ME2wMlAzQDlzIN88US=> M1XheHNCVkeHUh?=
SW982 MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13uV2lEPTB;MD6wNlk6QSEQvF2= M3i3THNCVkeHUh?=
OE19 NVfk[5Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjOZpE3UUN3ME2wMlA{ODd5IN88US=> MonqV2FPT0WU
SK-LU-1 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTudWhXUUN3ME2wMlA{ODh{IN88US=> NHnUW3lUSU6JRWK=
H4 M{\ZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnoTWM2OD1yLkCzNFkh|ryP M1np[3NCVkeHUh?=
HT-144 NHfyeoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwMEOwPVMh|ryP NYeydlg2W0GQR1XS
SK-UT-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vFTmlEPTB;MD6wN|E4QCEQvF2= MmXjV2FPT0WU
D-336MG MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\OfGlEPTB;MD6wN|MxQSEQvF2= M16ySnNCVkeHUh?=
MDA-MB-175-VII MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\6VGlEPTB;MD6wN|M2PCEQvF2= NXXyNW1bW0GQR1XS
GAMG M2j0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUiwdXYzUUN3ME2wMlA{PDN3IN88US=> MVzTRW5ITVJ?
CP50-MEL-B NYnUSXQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX5VWJKSzVyPUCuNFM1PSEQvF2= MYfTRW5ITVJ?
OVCAR-5 NWO1cGZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLJTWM2OD1yLkCzOFgh|ryP MWPTRW5ITVJ?
SK-MES-1 NGrGeVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vJV2lEPTB;MD6wN|YxPiEQvF2= Mme4V2FPT0WU
VM-CUB-1 NXXVTpExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXuTWM2OD1yLkCzOlU4KM7:TR?= M{PLOHNCVkeHUh?=
WM-115 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLSTWM2OD1yLkCzO|YzKM7:TR?= NUXESGp3W0GQR1XS
DSH1 NYjn[WQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3pbJFvUUN3ME2wMlA{QDB5IN88US=> MmX3V2FPT0WU
Becker M4DQT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vuc2lEPTB;MD6wN|g5PSEQvF2= MV7TRW5ITVJ?
SW962 NHz1VnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrVZ214UUN3ME2wMlA{QTR3IN88US=> MlW0V2FPT0WU
TYK-nu MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwMEO5PFUh|ryP MoTtV2FPT0WU
HO-1-N-1 M1fZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHj2NpdKSzVyPUCuNFQxOjFizszN MnnkV2FPT0WU
T98G MlvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[0dmlEPTB;MD6wOFExOyEQvF2= M{LETnNCVkeHUh?=
ACN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwMESxOlIh|ryP MYjTRW5ITVJ?
SW780 M1eyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwMESyNFMh|ryP NGD2VJBUSU6JRWK=
Detroit562 M3H1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\vTWM2OD1yLkC0NlM6KM7:TR?= NFe3VnVUSU6JRWK=
BB49-HNC NXG0OY9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XGXWlEPTB;MD6wOFI1OyEQvF2= M171ZXNCVkeHUh?=
HN NWLoRpZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vvUWlEPTB;MD6wOFI4OiEQvF2= M3zFfHNCVkeHUh?=
H9 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwMESzO|Eh|ryP M2jXWnNCVkeHUh?=
VA-ES-BJ M4DiXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLETWM2OD1yLkC0OFQ4KM7:TR?= NVPIfGVxW0GQR1XS
MEL-JUSO NXrQNIdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\xTWM2OD1yLkC0OFc2KM7:TR?= NEHpc|hUSU6JRWK=
BT-474 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrRTWM2OD1yLkC0OUDPxE1? M4qwOnNCVkeHUh?=
CaR-1 Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkftTWM2OD1yLkC0OVQ6KM7:TR?= NX;FUmN1W0GQR1XS
PSN1 M1fUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrlXmdKSzVyPUCuNFQ3ODNizszN M1LjfXNCVkeHUh?=
KYSE-510 Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XJcWlEPTB;MD6wOFY1QSEQvF2= MV3TRW5ITVJ?
KP-4 M2XT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHsN|JKSzVyPUCuNFQ4PTNizszN NVvtfFBxW0GQR1XS
KYSE-410 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMES3O|Ih|ryP NHX5Z2ZUSU6JRWK=
G-402 M{[yfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jtfmlEPTB;MD6wOFc5QSEQvF2= M4\YTnNCVkeHUh?=
DOK MkPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7iTWM2OD1yLkC0PVAzKM7:TR?= M1HxS3NCVkeHUh?=
COR-L88 MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n4NmlEPTB;MD6wOFkyOiEQvF2= NU\NS5Y2W0GQR1XS
SKG-IIIa NFW1[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLudmhKSzVyPUCuNFQ6QDZizszN MoruV2FPT0WU
AN3-CA NVLCb5hmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHxSXJOUUN3ME2wMlA2KM7:TR?= M1\xPHNCVkeHUh?=
SW48 NEX6SG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXrPWRKSzVyPUCuNFUxOzlizszN NXjmfohuW0GQR1XS
YKG-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vRTGlEPTB;MD6wOVA4OSEQvF2= MlvoV2FPT0WU
KYSE-150 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLlTWM2OD1yLkC1NlM2KM7:TR?= NUL0PXpWW0GQR1XS
HuO-3N1 Mlu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7HfJAyUUN3ME2wMlA2OjN5IN88US=> MW\TRW5ITVJ?
LB1047-RCC NGDhc3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3OTWM2OD1yLkC1Nlk3KM7:TR?= MYXTRW5ITVJ?
NCI-H2030 MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILJb3dKSzVyPUCuNFU1OTRizszN NWT5Uo1[W0GQR1XS
YH-13 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjhTWM2OD1yLkC1O|IzKM7:TR?= M3fScXNCVkeHUh?=
5637 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjSW|Z2UUN3ME2wMlA2PzRizszN M{[3TnNCVkeHUh?=
LOXIMVI NH34WIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf2TWM2OD1yLkC1PFczKM7:TR?= NWTpfIIxW0GQR1XS
GT3TKB M1HNemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrE[phKSzVyPUCuNFU6PDJizszN MVzTRW5ITVJ?
TCCSUP MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rMUmlEPTB;MD6wOVk3PCEQvF2= MmnyV2FPT0WU
EPLC-272H M4LQfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nUfWlEPTB;MD6wOlIxPSEQvF2= MUfTRW5ITVJ?
LU-99A NX:4VFBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXQTWM2OD1yLkC2NlM4KM7:TR?= MXjTRW5ITVJ?
NCI-H1755 NWnyTmVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITScY1KSzVyPUCuNFY{PDFizszN NHzZSJlUSU6JRWK=
KM12 MknIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\yTWM2OD1yLkC2N|Q5KM7:TR?= NIi3NXNUSU6JRWK=
SF295 M4jkVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PCR2lEPTB;MD6wOlQ2OiEQvF2= MWjTRW5ITVJ?
MZ2-MEL NG\lcoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;K[nJKSzVyPUCuNFY2PTNizszN MnPKV2FPT0WU
HEC-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3hTWM2OD1yLkC2OVg5KM7:TR?= NHHKNplUSU6JRWK=
SW684 NVXyWYhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPqfpdFUUN3ME2wMlA3PTlzIN88US=> NIPuU29USU6JRWK=
SF539 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnG[WdKSzVyPUCuNFY3QDFizszN MU\TRW5ITVJ?
GMS-10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPnTWM2OD1yLkC2Olk6KM7:TR?= MV\TRW5ITVJ?
MV-4-11 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPEO5lKSzVyPUCuNFY5ODNizszN M3fWdXNCVkeHUh?=
HT-29 NIDRPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnMcoxKSzVyPUCuNFY6OTlizszN MmfsV2FPT0WU
23132-87 MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnqem1nUUN3ME2wMlA3QTVizszN MUnTRW5ITVJ?
SW620 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3q2d2lEPTB;MD6wO|AzPiEQvF2= Mnv5V2FPT0WU
HCC1806 NGjic3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPBRW9KSzVyPUCuNFcyOzFizszN M{j5SXNCVkeHUh?=
Hs-578-T NEHrNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXflb4NYUUN3ME2wMlA4OjB6IN88US=> MYfTRW5ITVJ?
A2058 M1;pXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;hV4I1UUN3ME2wMlA4OjJ6IN88US=> MkjTV2FPT0WU
MEL-HO Ml[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjlW25zUUN3ME2wMlA4OjV3IN88US=> M{PRXXNCVkeHUh?=
HCC2998 NVLMPG5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3noS2lEPTB;MD6wO|M1PyEQvF2= MkXOV2FPT0WU
HuO9 NYfld2dPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3HOYY{UUN3ME2wMlA4PTh7IN88US=> NXTMT401W0GQR1XS
CAL-39 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\ueYZKSzVyPUCuNFc4PjZizszN M1HHc3NCVkeHUh?=
M14 NVXt[Xk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMEe5NVMh|ryP M{XN[HNCVkeHUh?=
BFTC-909 NVfQ[3VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwMEe5Olkh|ryP MnvPV2FPT0WU
TE-11 NVvRZo5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DINmlEPTB;MD6wO|k6PiEQvF2= NFHCWGlUSU6JRWK=
TGBC1TKB MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwMEiwOFMh|ryP NGLBcJFUSU6JRWK=
L-363 NWq4T3NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMEiyNFYh|ryP M1H5dHNCVkeHUh?=
A431 NV\NcoxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\1NmlEPTB;MD6wPFIyKM7:TR?= Mme0V2FPT0WU
MKN45 M2WzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTsOYxGUUN3ME2wMlA5OjF7IN88US=> MXnTRW5ITVJ?
HT-1080 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXYPXJyUUN3ME2wMlA5PDN7IN88US=> M3PqdHNCVkeHUh?=
OVCAR-8 NUHMdWc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX36RXpZUUN3ME2wMlA5PjJ{IN88US=> MoDnV2FPT0WU
LCLC-97TM1 MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXYeXNKSzVyPUCuNFg4OjhizszN M1Hi[3NCVkeHUh?=
M059J MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwMEmwNlch|ryP M3TONnNCVkeHUh?=
SK-MEL-2 NI\TT4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMEmwOkDPxE1? MVrTRW5ITVJ?
TE-1 MmDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DxZWlEPTB;MD6wPVIxPCEQvF2= NELLUXBUSU6JRWK=
KYSE-180 NIjYRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fMcGlEPTB;MD6wPVI3OiEQvF2= Mn3XV2FPT0WU
D-247MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCTWM2OD1yLkC5OFU2KM7:TR?= NHi1bZhUSU6JRWK=
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D-423MG NUPleGdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jE[WlEPTB;Nj60NFI5PCEQvF2= NWC1eXZSW0GQR1XS
ECC10 NYfGPFF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTdwMUCxNFEh|ryP M{\oPHNCVkeHUh?=
TE-5 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TSfGlEPTB;Nz60NVI6QCEQvF2= NUPvToJwW0GQR1XS
P12-ICHIKAWA NUPVOm9UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTdwNEW1NlMh|ryP NIqyeZJUSU6JRWK=
NCI-H82 NHjhO5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfVTWM2OD15LkS1O|AyKM7:TR?= NGHmSYJUSU6JRWK=
NCI-H1993 M{PXXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHm1[mtKSzVyPUeuPFMxPjNizszN NFPScZNUSU6JRWK=
RH-1 M1n2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TxW2lEPTB;Nz64OVI1PCEQvF2= NIPvTWtUSU6JRWK=
SW948 M37sXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTdwOU[wOFkh|ryP NFHzfoNUSU6JRWK=
CAL-33 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTQdWtKSzVyPUeuPVk6OzhizszN Mmi2V2FPT0WU
U-266 NXv2XXJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHRdZFmUUN3ME24MlE2Pzd5IN88US=> MUXTRW5ITVJ?
CAL-72 NFrPfXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjw[npKSzVyPUiuNlA{OiEQvF2= MmjzV2FPT0WU
SNU-423 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTlwM{[2OlYh|ryP NVHkfmpJW0GQR1XS
KG-1 NV3MVJFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fn[WlEPTB;OT61PFQ2PiEQvF2= MYfTRW5ITVJ?
HCC1395 M1rwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPXTWM2OD17LkmyN|UzKM7:TR?= M2nzfXNCVkeHUh?=
BE-13 NF;lSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFyLki4PVIh|ryP MnmyV2FPT0WU
MKN7 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDySWlnUUN3ME2xNE46PzZ3IN88US=> M2\m[nNCVkeHUh?=
697 NXLGNolUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTpTWM2OD1zMT6xOFczKM7:TR?= NFvsbnBUSU6JRWK=
LU-135 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TFUWlEPTB;MUGuNlMxPyEQvF2= NX25eHU{W0GQR1XS
ES7 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj1TGlRUUN3ME2xNU4{OzF|IN88US=> MoPHV2FPT0WU
SK-HEP-1 NI\qWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF23fWdKSzVyPUGxMlc3PDZizszN MkGyV2FPT0WU
BEN MkHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2W1TmlEPTB;MUGuPFUyKM7:TR?= MV7TRW5ITVJ?
NCI-H1770 NIDwbW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjYeHVKSzVyPUGyMlEzPiEQvF2= MXLTRW5ITVJ?
SW13 NEjESGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrOOllKSzVyPUGyMlE2PDFizszN NVzzS5Y4W0GQR1XS
MZ1-PC NUf6bJhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF{LkW0OVIh|ryP MnS2V2FPT0WU
Mo-T MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf1TWM2OD1zMj63OFIyKM7:TR?= NHzHcmJUSU6JRWK=
HLE NFniW2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jp[WlEPTB;MUKuPFIyPSEQvF2= Mo\YV2FPT0WU
RCC10RGB MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPwXlB4UUN3ME2xN{43PzFizszN M3PT[nNCVkeHUh?=
COLO-320-HSR NVfaXmNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET5bJRKSzVyPUGzMlc{QDFizszN M3LnNHNCVkeHUh?=
BHT-101 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTF|LkizOFUh|ryP MmK0V2FPT0WU
OCUB-M MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHze|k3UUN3ME2xOE4yPjB{IN88US=> M{e4fXNCVkeHUh?=
MEG-01 NVTCXnVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF2LkO3NFgh|ryP M4\CcHNCVkeHUh?=
RS4-11 M2rmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzlTWM2OD1zND63OFIh|ryP M1HWNnNCVkeHUh?=
MN-60 NWKxPI9PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KwXGlEPTB;MUSuO|g6PCEQvF2= MXvTRW5ITVJ?
NCI-H1304 NWS0OFFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF3LkC0NlUh|ryP NWHVdpNMW0GQR1XS
Ramos-2G6-4C10 NILt[W5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF3LkC1PFEh|ryP MXPTRW5ITVJ?
NCI-H2342 Ml[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPsUo1KSzVyPUG1MlIxPDRizszN MVLTRW5ITVJ?
LAN-6 M4S0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrNV4VlUUN3ME2xOU41PDF2IN88US=> M2KzPXNCVkeHUh?=
JVM-2 NF:yUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTF3LkW3OFgh|ryP NX;TSnFKW0GQR1XS
P30-OHK NVG2b5pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnFT2NKSzVyPUG2MlA3OTRizszN M2HpcHNCVkeHUh?=
C-33-A MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTF4Lk[yNVQh|ryP NVHibHQ3W0GQR1XS
RPMI-8866 NVzSTXlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnlbYtCUUN3ME2xOk45PDl4IN88US=> MX7TRW5ITVJ?
NCI-H630 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF4Lki1N|ch|ryP MWnTRW5ITVJ?
KYSE-140 M4jvSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;NTWM2OD1zNz6yNFI5KM7:TR?= NVK5NmNlW0GQR1XS
T84 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrJfmJbUUN3ME2xPE45Pjl3IN88US=> NFXOd3NUSU6JRWK=
KU-19-19 NIPoSJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXwTnlKSzVyPUG4Mlk3ODhizszN M37PS3NCVkeHUh?=
BALL-1 NYfwSWJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTF7LkOzPVkh|ryP MUDTRW5ITVJ?
Calu-6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3EPYZKSzVyPUG5MlQ6OiEQvF2= MnPLV2FPT0WU
EGI-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rKRmlEPTB;MUmuOVk5KM7:TR?= MofYV2FPT0WU
MFH-ino M1\u[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TQOWlEPTB;MUmuO|Q2PCEQvF2= NFf4TWtUSU6JRWK=
GB-1 M{XFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJyLkO1N|Uh|ryP MoLSV2FPT0WU
NCI-H1693 M{jYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG3d3pwUUN3ME2yNE43PTB3IN88US=> NEHvVWlUSU6JRWK=
SW1116 NVzxW2ltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT2bXRQUUN3ME2yNE46OzZ{IN88US=> MXzTRW5ITVJ?
H-EMC-SS NX\aV5FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HzRmlEPTB;MkKuNFQ2KM7:TR?= MV\TRW5ITVJ?
D-502MG NVfwWWFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXUTWM2OD1{Mj64NlYyKM7:TR?= MVLTRW5ITVJ?
IA-LM MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJ|LkK0PVMh|ryP NI\iZmJUSU6JRWK=
SW1463 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjabIZ1UUN3ME2yN{44QSEQvF2= MUHTRW5ITVJ?
JAR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:zcohKSzVyPUK0MlMzQTNizszN NIXp[HBUSU6JRWK=
HT MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJ2LkS3OVMh|ryP MVzTRW5ITVJ?
LCLC-103H MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7YephKSzVyPUK0Mlg1PDlizszN M{ntcnNCVkeHUh?=
SNU-449 NUfLTmNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJ2Lki3OFEh|ryP M1XpPHNCVkeHUh?=
KE-37 NIrpb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJ3LkC5Nlgh|ryP MoLTV2FPT0WU
NCI-H1623 NXLCN4ZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz2TWM2OD1{Nz6xN|A{KM7:TR?= MWDTRW5ITVJ?
MOLT-13 NF\wcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHPTWM2OD1{Nz6zOVE3KM7:TR?= NIrVVZpUSU6JRWK=
COLO-741 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XXVGlEPTB;M{GuN|M{OyEQvF2= M1uzPHNCVkeHUh?=
NB6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;DZ|lKSzVyPUOyMlI5PzZizszN NVXMUIVMW0GQR1XS
MOLT-16 M3\5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLW[4Y6UUN3ME2zN{4xODV3IN88US=> MXfTRW5ITVJ?
IST-MES1 M2jFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn21TWM2OD1|ND6wOVQyKM7:TR?= M2LUN3NCVkeHUh?=
A4-Fuk MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PEdWlEPTB;M{WuNFY3KM7:TR?= MlGyV2FPT0WU
CAL-85-1 M3y0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XyN2lEPTB;M{WuNlgyPyEQvF2= NGrIfJdUSU6JRWK=
CCRF-CEM NF3HXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTN5LkG1N|Yh|ryP NYHUVXpbW0GQR1XS
HAL-01 NXzSXIZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN6LkS4PFkh|ryP MnLrV2FPT0WU
HEL MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR|LkO0NFkh|ryP MXPTRW5ITVJ?
EW-1 M2[2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TJSWlEPTB;NEOuOFc3QCEQvF2= MXnTRW5ITVJ?
MDA-MB-231 M1;6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof4TWM2OD12NT6xNVk6KM7:TR?= MVPTRW5ITVJ?
ABC-1 NGLHdGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv3O4ZKSzVyPUS2Mlg2OzhizszN NFrv[HhUSU6JRWK=
NCI-H446 NV35[oNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR6LkWwOVgh|ryP NH\qU4ZUSU6JRWK=
MHH-PREB-1 Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR7Lk[wNFch|ryP MVvTRW5ITVJ?
DOHH-2 NUDaR|NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDyTWM2OD12OT62OlU3KM7:TR?= MoH6V2FPT0WU
GCT NE\sRlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmqyTWM2OD12OT62PVc3KM7:TR?= MVrTRW5ITVJ?

... 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]
- Collapse

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
Smiles COC1CC(C)CC2=C(NCC=C)C(=O)C=C(NC(=O)C(=C\C=C/C(OC)C(OC(N)=O)/C(=C/C(C)C1O)C)\C)C2=O

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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