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 24 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 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnCTWM2OD1yLkCwNFMxOyEQvF2= NEHSfZBUSU6JRWK=
IST-MEL1 NEPPOoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIH4Zm5KSzVyPUCuNFAxPDB5IN88US=> NUjY[WFZW0GQR1XS
NCI-SNU-1 M{LJdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwMECyNFch|ryP MoDtV2FPT0WU
FADU MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2niV2lEPTB;MD6wNFIxQSEQvF2= MYTTRW5ITVJ?
C32 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn5[25KSzVyPUCuNFA{ODRizszN NIm1VGxUSU6JRWK=
D-566MG NWS1O5JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT3OY1uUUN3ME2wMlAxOzlizszN MV7TRW5ITVJ?
LXF-289 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwMEC0NVkh|ryP MWPTRW5ITVJ?
HGC-27 NYnLfGs6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwMEC1NUDPxE1? NV24V45{W0GQR1XS
RPMI-7951 M{nYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vuOmlEPTB;MD6wNFcyPyEQvF2= MmL0V2FPT0WU
HSC-3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTVd40zUUN3ME2wMlAxQTJ7IN88US=> NEm1VINUSU6JRWK=
MIA-PaCa-2 M17TRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTkeGJMUUN3ME2wMlAyODB7IN88US=> NGHmT25USU6JRWK=
KS-1 NFr5XIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nubmlEPTB;MD6wNVM2PSEQvF2= MVrTRW5ITVJ?
CAL-51 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\tT3hKSzVyPUCuNFE1ODVizszN NXXyeFQ4W0GQR1XS
MDA-MB-361 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPOU|dHUUN3ME2wMlAyPDl3IN88US=> NIjUOGJUSU6JRWK=
TI-73 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvPfJU4UUN3ME2wMlAyPzl4IN88US=> M1q0cXNCVkeHUh?=
AGS Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnXTWM2OD1yLkCxPVM5KM7:TR?= MmD3V2FPT0WU
NCI-H460 MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjRUGpKSzVyPUCuNFE6PzRizszN NGTydHNUSU6JRWK=
A204 NFvaOHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj2OGpNUUN3ME2wMlAzOjR7IN88US=> MVnTRW5ITVJ?
CHL-1 NX3NRnRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMEKyOVEh|ryP NInwPFFUSU6JRWK=
DU-4475 Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfTVWtKSzVyPUCuNFIzPjFizszN M3jZcXNCVkeHUh?=
CGTH-W-1 NXT2SFd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LMW2lEPTB;MD6wNlM1QSEQvF2= NXnrV4NkW0GQR1XS
HCC2218 M3vOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXOO4ZKSzVyPUCuNFI1QTRizszN M4rJSXNCVkeHUh?=
A2780 M4W4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLYTWM2OD1yLkCyOVMyKM7:TR?= M2LmfHNCVkeHUh?=
NCI-H720 M4jBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\wN2lEPTB;MD6wNlU1PiEQvF2= M2fMcHNCVkeHUh?=
NCI-N87 M{nnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nYZmlEPTB;MD6wNlU6OyEQvF2= MWHTRW5ITVJ?
CHP-212 M4TiXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTBwMEK2Nlgh|ryP MWTTRW5ITVJ?
NCI-H23 NXXk[2E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzUmlEPTB;MD6wNlY3PSEQvF2= MV7TRW5ITVJ?
D-263MG M{Cwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M332dWlEPTB;MD6wNlc5PiEQvF2= MlnRV2FPT0WU
ME-180 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli5TWM2OD1yLkCyPFkyKM7:TR?= MoLRV2FPT0WU
SW982 MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;VZVZMUUN3ME2wMlAzQTl7IN88US=> NEPhXFVUSU6JRWK=
OE19 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zsbGlEPTB;MD6wN|A4PyEQvF2= MUfTRW5ITVJ?
SK-LU-1 NFjsTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMEOwPFIh|ryP M4rVTnNCVkeHUh?=
H4 NFHHS3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX73W4ZtUUN3ME2wMlA{ODlizszN NWPNVY9sW0GQR1XS
HT-144 M3zte2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vyOWlEPTB;MD6wN|A6OyEQvF2= NIjhUZJUSU6JRWK=
SK-UT-1 MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PwZ2lEPTB;MD6wN|E4QCEQvF2= MUPTRW5ITVJ?
D-336MG NU\pV21VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonJTWM2OD1yLkCzN|A6KM7:TR?= NE\6ZodUSU6JRWK=
MDA-MB-175-VII Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwMEOzOVQh|ryP NXz5RVVNW0GQR1XS
GAMG MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jRemlEPTB;MD6wN|Q{PSEQvF2= MmDTV2FPT0WU
CP50-MEL-B MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV2z[FJHUUN3ME2wMlA{PDVizszN Mm\SV2FPT0WU
OVCAR-5 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvGdG93UUN3ME2wMlA{PDhizszN MVrTRW5ITVJ?
SK-MES-1 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMEO2NFYh|ryP NGPGN5BUSU6JRWK=
VM-CUB-1 M{XrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPsb5BPUUN3ME2wMlA{PjV5IN88US=> NHHTS5pUSU6JRWK=
WM-115 NYfDelBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK3T5JKSzVyPUCuNFM4PjJizszN NEfxXYRUSU6JRWK=
DSH1 NGHFPJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj1TWM2OD1yLkCzPFA4KM7:TR?= NXm0Ro17W0GQR1XS
Becker NWXPZWRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHwSWpKSzVyPUCuNFM5QDVizszN M{O4RXNCVkeHUh?=
SW962 NYHP[lhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMEO5OFUh|ryP MW\TRW5ITVJ?
TYK-nu NInHfWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITpZYZKSzVyPUCuNFM6QDVizszN NH;SWplUSU6JRWK=
HO-1-N-1 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwMESwNlEh|ryP M{DIUnNCVkeHUh?=
T98G NF3HVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHjbWVyUUN3ME2wMlA1OTB|IN88US=> MlH4V2FPT0WU
ACN NFnhUlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DjcmlEPTB;MD6wOFE3OiEQvF2= NH\XeG5USU6JRWK=
SW780 NWewTYpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTDNWtJUUN3ME2wMlA1OjB|IN88US=> NXTE[IJFW0GQR1XS
Detroit562 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\iR2lEPTB;MD6wOFI{QSEQvF2= MXrTRW5ITVJ?
BB49-HNC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GzPGlEPTB;MD6wOFI1OyEQvF2= NELCUXlUSU6JRWK=
HN M3\ENmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4TJZEUUN3ME2wMlA1Ojd{IN88US=> MnTMV2FPT0WU
H9 NHXVXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLRU3dKSzVyPUCuNFQ{PzFizszN MUDTRW5ITVJ?
VA-ES-BJ MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XUT2lEPTB;MD6wOFQ1PyEQvF2= M4DyR3NCVkeHUh?=
MEL-JUSO NGnxTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7Zd2lKSzVyPUCuNFQ1PzVizszN NVK1Z5FyW0GQR1XS
BT-474 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMES1JO69VQ>? MYPTRW5ITVJ?
CaR-1 M1f5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnFTWM2OD1yLkC0OVQ6KM7:TR?= MlvtV2FPT0WU
PSN1 NHS4XGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwMES2NFMh|ryP NFfyWmtUSU6JRWK=
KYSE-510 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rHTWlEPTB;MD6wOFY1QSEQvF2= M4fIS3NCVkeHUh?=
KP-4 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XHbGlEPTB;MD6wOFc2OyEQvF2= MoTxV2FPT0WU
KYSE-410 M2jP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwMES3O|Ih|ryP MmjxV2FPT0WU
G-402 M3;WR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMES3PFkh|ryP NW\lfVRWW0GQR1XS
DOK MlvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17wc2lEPTB;MD6wOFkxOiEQvF2= MoTIV2FPT0WU
COR-L88 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:y[2lEPTB;MD6wOFkyOiEQvF2= MXnTRW5ITVJ?
SKG-IIIa M{f6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMES5PFYh|ryP MlHxV2FPT0WU
AN3-CA M{jyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\XOo1KSzVyPUCuNFUh|ryP NWmzV2h[W0GQR1XS
SW48 NFHQOnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1KwcmlEPTB;MD6wOVA{QSEQvF2= M1THcXNCVkeHUh?=
YKG-1 NXvlXVdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki0TWM2OD1yLkC1NFcyKM7:TR?= MkLSV2FPT0WU
KYSE-150 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3xWFdKSzVyPUCuNFUzOzVizszN NF73PW9USU6JRWK=
HuO-3N1 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMEWyN|ch|ryP MXzTRW5ITVJ?
LB1047-RCC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHOTWM2OD1yLkC1Nlk3KM7:TR?= NIjSdm5USU6JRWK=
NCI-H2030 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\neI9HUUN3ME2wMlA2PDF2IN88US=> MWnTRW5ITVJ?
YH-13 NYLOR3M3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TqT2lEPTB;MD6wOVczOiEQvF2= MnP6V2FPT0WU
5637 NU\ONohET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXvTWM2OD1yLkC1O|Qh|ryP MlHrV2FPT0WU
LOXIMVI NF[wSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i5RWlEPTB;MD6wOVg4OiEQvF2= NV33bndWW0GQR1XS
GT3TKB NEXOUohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD0TWM2OD1yLkC1PVQzKM7:TR?= NV;Sb|ZQW0GQR1XS
TCCSUP NFjSUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nIPGlEPTB;MD6wOVk3PCEQvF2= MVvTRW5ITVJ?
EPLC-272H NGL1PJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zNNmlEPTB;MD6wOlIxPSEQvF2= MnS0V2FPT0WU
LU-99A NWTGXGY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwME[yN|ch|ryP MoqyV2FPT0WU
NCI-H1755 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LVUmlEPTB;MD6wOlM1OSEQvF2= MlPsV2FPT0WU
KM12 M1:xNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrkTWM2OD1yLkC2N|Q5KM7:TR?= MWjTRW5ITVJ?
SF295 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHGyfHVKSzVyPUCuNFY1PTJizszN MW\TRW5ITVJ?
MZ2-MEL NILXSFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\ve2lEPTB;MD6wOlU2OyEQvF2= M3rZU3NCVkeHUh?=
HEC-1 MkPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLJflN7UUN3ME2wMlA3PTh6IN88US=> MnfvV2FPT0WU
SW684 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{frN2lEPTB;MD6wOlU6OSEQvF2= M1rS[nNCVkeHUh?=
SF539 NIn3V|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwME[2PFEh|ryP NHLheo5USU6JRWK=
GMS-10 MlTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwME[2PVkh|ryP M3[zVnNCVkeHUh?=
MV-4-11 M3vyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\QWWlEPTB;MD6wOlgxOyEQvF2= Mk\lV2FPT0WU
HT-29 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwME[5NVkh|ryP MkH2V2FPT0WU
23132-87 NUjucJZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwME[5OUDPxE1? NXLFT5VJW0GQR1XS
SW620 M4rqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTBwMEewNlYh|ryP NXfneIx6W0GQR1XS
HCC1806 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\CUVJKSzVyPUCuNFcyOzFizszN MUDTRW5ITVJ?
Hs-578-T NIK5elFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;kdGlEPTB;MD6wO|IxQCEQvF2= MVrTRW5ITVJ?
A2058 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHnTWM2OD1yLkC3NlI5KM7:TR?= M1rQbXNCVkeHUh?=
MEL-HO M2DBZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K5ZmlEPTB;MD6wO|I2PSEQvF2= NWf6UldZW0GQR1XS
HCC2998 M4q3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwMEezOFch|ryP M{\WOHNCVkeHUh?=
HuO9 MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WzTmlEPTB;MD6wO|U5QSEQvF2= NEDne|VUSU6JRWK=
CAL-39 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPkcXlMUUN3ME2wMlA4PzZ4IN88US=> M{jDVHNCVkeHUh?=
M14 NXPaPW5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPnOGpKSzVyPUCuNFc6OTNizszN NIDEVXdUSU6JRWK=
BFTC-909 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwMEe5Olkh|ryP M1PQZ3NCVkeHUh?=
TE-11 M3m5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\5[Y5KSzVyPUCuNFc6QTZizszN NX;RS5NtW0GQR1XS
TGBC1TKB MkjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q1b2lEPTB;MD6wPFA1OyEQvF2= NUTvPY13W0GQR1XS
L-363 NXLOZoxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tuc2lEPTB;MD6wPFIxPiEQvF2= Mo\DV2FPT0WU
A431 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe2fVMzUUN3ME2wMlA5OjFizszN M4XvcXNCVkeHUh?=
MKN45 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDV[oxKSzVyPUCuNFgzOTlizszN NUjCS4dtW0GQR1XS
HT-1080 MkjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMEi0N|kh|ryP M4C1dHNCVkeHUh?=
OVCAR-8 M4mxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwMEi2NlIh|ryP M3G5VHNCVkeHUh?=
LCLC-97TM1 NWDn[lJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zTWWlEPTB;MD6wPFczQCEQvF2= MUnTRW5ITVJ?
M059J MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETabnRKSzVyPUCuNFkxOjdizszN M{jrOXNCVkeHUh?=
SK-MEL-2 NYToNZA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHQOG52UUN3ME2wMlA6ODZizszN MkDDV2FPT0WU
TE-1 NX62c2k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwMEmyNFQh|ryP MmrLV2FPT0WU
KYSE-180 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3X3SGlEPTB;MD6wPVI3OiEQvF2= M4TURXNCVkeHUh?=
D-247MG NHzxWoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXaTWM2OD1yLkC5OFU2KM7:TR?= M3;aVHNCVkeHUh?=
8-MG-BA NETQU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LLVWlEPTB;MD6wPVQ4OiEQvF2= NYSxUFRSW0GQR1XS
NCI-H1792 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnUUI1OUUN3ME2wMlA6PjF6IN88US=> M3S5T3NCVkeHUh?=
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KG-1 M4PqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\1RmIxUUN3ME25MlU5PDV4IN88US=> M1nkbnNCVkeHUh?=
HCC1395 NX\NOGh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfLXlFKSzVyPUmuPVI{PTJizszN NFvCUWFUSU6JRWK=
BE-13 NWL6cnh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7KRnJKSzVyPUGwMlg5QTJizszN MnPiV2FPT0WU
MKN7 M3rP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfhWphSUUN3ME2xNE46PzZ3IN88US=> M2\3OXNCVkeHUh?=
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LU-135 MmH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DSTmlEPTB;MUGuNlMxPyEQvF2= NGLGbIJUSU6JRWK=
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SK-HEP-1 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TuSWlEPTB;MUGuO|Y1PiEQvF2= M{exeHNCVkeHUh?=
BEN MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;yTWM2OD1zMT64OVEh|ryP MVPTRW5ITVJ?
NCI-H1770 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fDXGlEPTB;MUKuNVI3KM7:TR?= MWTTRW5ITVJ?
SW13 NGLp[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF{LkG1OFEh|ryP MXXTRW5ITVJ?
MZ1-PC MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17VSGlEPTB;MUKuOVQ2OiEQvF2= NXHWRW4{W0GQR1XS
Mo-T MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIiwRlVKSzVyPUGyMlc1OjFizszN M1nDTHNCVkeHUh?=
HLE M4TBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfQ[4pKUUN3ME2xNk45OjF3IN88US=> NInQOYlUSU6JRWK=
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BHT-101 M{TwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfrbmc4UUN3ME2xN{45OzR3IN88US=> M1HSSXNCVkeHUh?=
OCUB-M MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLuN5hEUUN3ME2xOE4yPjB{IN88US=> M1ziVHNCVkeHUh?=
MEG-01 MlvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PLVGlEPTB;MUSuN|cxQCEQvF2= M2Tj[XNCVkeHUh?=
RS4-11 NWDkeotIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr5bVlFUUN3ME2xOE44PDJizszN MlrxV2FPT0WU
MN-60 M{K2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Lz[2lEPTB;MUSuO|g6PCEQvF2= NXqzb|l2W0GQR1XS
NCI-H1304 M1ri[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF3LkC0NlUh|ryP NWiybJFkW0GQR1XS
Ramos-2G6-4C10 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6wN2RKSzVyPUG1MlA2QDFizszN NHLjR4ZUSU6JRWK=
NCI-H2342 NXjoNplMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF3LkKwOFQh|ryP NEO1c3dUSU6JRWK=
LAN-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmP2TWM2OD1zNT60OFE1KM7:TR?= NWL5OFlqW0GQR1XS
JVM-2 M2nZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S2XmlEPTB;MUWuOVc1QCEQvF2= NWPzRmJ5W0GQR1XS
P30-OHK M2rTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF4LkC2NVQh|ryP MoO0V2FPT0WU
C-33-A M3q3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXiZlJVUUN3ME2xOk43OjF2IN88US=> MXzTRW5ITVJ?
RPMI-8866 M1q2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PTVGlEPTB;MU[uPFQ6PiEQvF2= NX3V[mdQW0GQR1XS
NCI-H630 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\sc21xUUN3ME2xOk45PTN5IN88US=> MVXTRW5ITVJ?
KYSE-140 NVf0NHZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF5LkKwNlgh|ryP MX;TRW5ITVJ?
T84 MlTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknhTWM2OD1zOD64Olk2KM7:TR?= M1;UXHNCVkeHUh?=
KU-19-19 M3nyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF32dWpKSzVyPUG4Mlk3ODhizszN NHzPVoVUSU6JRWK=
BALL-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTF7LkOzPVkh|ryP NHnnN4lUSU6JRWK=
Calu-6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vC[2lEPTB;MUmuOFkzKM7:TR?= NXXiVZB2W0GQR1XS
EGI-1 NFjjR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHPTWM2OD1zOT61PVgh|ryP NIjCPG5USU6JRWK=
MFH-ino Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLXbGJwUUN3ME2xPU44PDV2IN88US=> NGrFSWZUSU6JRWK=
GB-1 NILHOZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJyLkO1N|Uh|ryP MnXSV2FPT0WU
NCI-H1693 NEPsOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH1eYhKSzVyPUKwMlY2ODVizszN MYjTRW5ITVJ?
SW1116 NHu5WppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3yzd2lEPTB;MkCuPVM3OiEQvF2= M3PjOXNCVkeHUh?=
H-EMC-SS NWL4TmhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJ{LkC0OUDPxE1? M{PNU3NCVkeHUh?=
D-502MG NFW5fJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnDZnJTUUN3ME2yNk45OjZzIN88US=> Mk\rV2FPT0WU
IA-LM M124OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJ|LkK0PVMh|ryP MUDTRW5ITVJ?
SW1463 M4L1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHNd3BSUUN3ME2yN{44QSEQvF2= M1rEV3NCVkeHUh?=
JAR MmC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSzTWM2OD1{ND6zNlk{KM7:TR?= M{HQWXNCVkeHUh?=
HT NHvsTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGS5d|NKSzVyPUK0MlQ4PTNizszN NWLtb2FHW0GQR1XS
LCLC-103H NGO0OGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrzT3lKSzVyPUK0Mlg1PDlizszN NULuTGVSW0GQR1XS
SNU-449 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJ2Lki3OFEh|ryP MYnTRW5ITVJ?
KE-37 M{\1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK2SJRKSzVyPUK1MlA6OjhizszN NGfEflJUSU6JRWK=
NCI-H1623 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn73TWM2OD1{Nz6xN|A{KM7:TR?= M2jiXnNCVkeHUh?=
MOLT-13 MknLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17H[GlEPTB;MkeuN|UyPiEQvF2= NFTqWoJUSU6JRWK=
COLO-741 NYOyZndMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M162emlEPTB;M{GuN|M{OyEQvF2= NFL6W4ZUSU6JRWK=
NB6 MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvEfVZKSzVyPUOyMlI5PzZizszN NWHhdVJqW0GQR1XS
MOLT-16 NUO3TpMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ThUmlEPTB;M{OuNFA2PSEQvF2= MnrsV2FPT0WU
IST-MES1 M1nPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nGWmlEPTB;M{SuNFU1OSEQvF2= NEXQ[m5USU6JRWK=
A4-Fuk MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDnR|BKSzVyPUO1MlA3PiEQvF2= M120cnNCVkeHUh?=
CAL-85-1 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HKSWlEPTB;M{WuNlgyPyEQvF2= NFP4OGpUSU6JRWK=
CCRF-CEM MontS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTHTWM2OD1|Nz6xOVM3KM7:TR?= M4TtdnNCVkeHUh?=
HAL-01 M{jGNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvDVWVKSzVyPUO4MlQ5QDlizszN NVPzfW5wW0GQR1XS
HEL M1HpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjXb2ZbUUN3ME20N{4{PDB7IN88US=> M2\YSHNCVkeHUh?=
EW-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnwRYFYUUN3ME20N{41PzZ6IN88US=> NIXJTldUSU6JRWK=
MDA-MB-231 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm0SYJ7UUN3ME20OU4yOTl7IN88US=> NWjoOpJsW0GQR1XS
ABC-1 NWL2VmJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu4bHRKSzVyPUS2Mlg2OzhizszN MWHTRW5ITVJ?
NCI-H446 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTR6LkWwOVgh|ryP NVTOUoNiW0GQR1XS
MHH-PREB-1 M2[z[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W4XmlEPTB;NEmuOlAxPyEQvF2= MkTsV2FPT0WU
DOHH-2 NXzL[GdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR7Lk[2OVYh|ryP MX3TRW5ITVJ?
GCT NYnVPWZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTR7Lk[5O|Yh|ryP NF7DXHVUSU6JRWK=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00577889 Completed Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer National Cancer Institute (NCI) March 2008 Phase 2
NCT00577889 Completed Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer National Cancer Institute (NCI) March 2008 Phase 2
NCT00546780 Completed Multiple Myeloma Bristol-Myers Squibb February 2008 Phase 3
NCT00546780 Completed Multiple Myeloma Bristol-Myers Squibb February 2008 Phase 3
NCT00093496 Completed Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer National Cancer Institute (NCI) October 2007 Phase 2
NCT00093496 Completed Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer National Cancer Institute (NCI) October 2007 Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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