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 54 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 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwMECwN|A{KM7:TR?= NULUVHdZW0GQR1XS
IST-MEL1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjGSHBKSzVyPUCuNFAxPDB5IN88US=> MXnTRW5ITVJ?
NCI-SNU-1 M2jyTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4CzV2lEPTB;MD6wNFIxPyEQvF2= MXjTRW5ITVJ?
FADU MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLoTWM2OD1yLkCwNlA6KM7:TR?= NHnRPWVUSU6JRWK=
C32 NHezV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjSTWM2OD1yLkCwN|A1KM7:TR?= MnOzV2FPT0WU
D-566MG MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;OOYhKSzVyPUCuNFA{QSEQvF2= NHXoSoJUSU6JRWK=
LXF-289 NFTtU25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnySIl4UUN3ME2wMlAxPDF7IN88US=> M{LnWXNCVkeHUh?=
HGC-27 NIjPd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fadmlEPTB;MD6wNFUyKM7:TR?= NE\jUVVUSU6JRWK=
RPMI-7951 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j0T2lEPTB;MD6wNFcyPyEQvF2= M{TBS3NCVkeHUh?=
HSC-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwMEC5Nlkh|ryP Ml;LV2FPT0WU
MIA-PaCa-2 NVTJcnFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGracnBKSzVyPUCuNFExODlizszN MWrTRW5ITVJ?
KS-1 NUS0fIhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLzeIZKSzVyPUCuNFE{PTVizszN MX;TRW5ITVJ?
CAL-51 NXPVUYY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf6[4hNUUN3ME2wMlAyPDB3IN88US=> MlPGV2FPT0WU
MDA-MB-361 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T1XGlEPTB;MD6wNVQ6PSEQvF2= NXLLdplFW0GQR1XS
TI-73 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fKeGlEPTB;MD6wNVc6PiEQvF2= NWPVXHNYW0GQR1XS
AGS MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP3W2dKSzVyPUCuNFE6OzhizszN MWDTRW5ITVJ?
NCI-H460 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC2VZJKSzVyPUCuNFE6PzRizszN NV;wTGZQW0GQR1XS
A204 M4jwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O1NGlEPTB;MD6wNlI1QSEQvF2= MUXTRW5ITVJ?
CHL-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XBOmlEPTB;MD6wNlI2OSEQvF2= M2XOe3NCVkeHUh?=
DU-4475 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPOZmpKSzVyPUCuNFIzPjFizszN MUHTRW5ITVJ?
CGTH-W-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwMEKzOFkh|ryP NHnXUmZUSU6JRWK=
HCC2218 MnXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T1SWlEPTB;MD6wNlQ6PCEQvF2= NVfk[ItPW0GQR1XS
A2780 M1S4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr0TWM2OD1yLkCyOVMyKM7:TR?= MU\TRW5ITVJ?
NCI-H720 M1nBNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMEK1OFYh|ryP NWjORYdGW0GQR1XS
NCI-N87 Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMEK1PVMh|ryP MYnTRW5ITVJ?
CHP-212 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j3PWlEPTB;MD6wNlYzQCEQvF2= MknKV2FPT0WU
NCI-H23 M4XXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXoW4JZUUN3ME2wMlAzPjZ3IN88US=> NITyTphUSU6JRWK=
D-263MG NX3Ec4M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jib2lEPTB;MD6wNlc5PiEQvF2= MnLGV2FPT0WU
ME-180 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMEK4PVEh|ryP NHGxNmNUSU6JRWK=
SW982 NVqxOGVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LMeWlEPTB;MD6wNlk6QSEQvF2= NI[xbWRUSU6JRWK=
OE19 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf4TWM2OD1yLkCzNFc4KM7:TR?= Mn:yV2FPT0WU
SK-LU-1 NEjXZZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHQfGVKSzVyPUCuNFMxQDJizszN MVTTRW5ITVJ?
H4 NIHnbWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HibGlEPTB;MD6wN|A6KM7:TR?= NIK5ZmFUSU6JRWK=
HT-144 M{G2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPZR2JYUUN3ME2wMlA{ODl|IN88US=> NVfkZXFuW0GQR1XS
SK-UT-1 Moj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMEOxO|gh|ryP NX7aXJpQW0GQR1XS
D-336MG NYO4O5FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP6dXFKSzVyPUCuNFM{ODlizszN NWLwcVZvW0GQR1XS
MDA-MB-175-VII NILWdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnmzTWM2OD1yLkCzN|U1KM7:TR?= Mlz0V2FPT0WU
GAMG NHTI[5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTBwMEO0N|Uh|ryP M1TJUXNCVkeHUh?=
CP50-MEL-B M{TpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzYTWM2OD1yLkCzOFUh|ryP NF34b5VUSU6JRWK=
OVCAR-5 M3TJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjNNnptUUN3ME2wMlA{PDhizszN MWPTRW5ITVJ?
SK-MES-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMEO2NFYh|ryP M4XRWXNCVkeHUh?=
VM-CUB-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Pzd2lEPTB;MD6wN|Y2PyEQvF2= MX3TRW5ITVJ?
WM-115 NV76UHdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT4TG9KSzVyPUCuNFM4PjJizszN NE\meGpUSU6JRWK=
DSH1 NUXRT|BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWCze2VEUUN3ME2wMlA{QDB5IN88US=> MU\TRW5ITVJ?
Becker M3z0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPRRWpsUUN3ME2wMlA{QDh3IN88US=> MXTTRW5ITVJ?
SW962 M{KxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG5TWM2OD1yLkCzPVQ2KM7:TR?= MnrvV2FPT0WU
TYK-nu MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XER2lEPTB;MD6wN|k5PSEQvF2= M3H1XnNCVkeHUh?=
HO-1-N-1 NGrncpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[4N4tKSzVyPUCuNFQxOjFizszN NUTiSWczW0GQR1XS
T98G M1PmZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[yTWM2OD1yLkC0NVA{KM7:TR?= M1vsenNCVkeHUh?=
ACN NFfOepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TmSmlEPTB;MD6wOFE3OiEQvF2= MkGwV2FPT0WU
SW780 M3flO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMESyNFMh|ryP NHXseYdUSU6JRWK=
Detroit562 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Sw[mlEPTB;MD6wOFI{QSEQvF2= NIf0OHJUSU6JRWK=
BB49-HNC MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP5VIFKSzVyPUCuNFQzPDNizszN M{fVN3NCVkeHUh?=
HN MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzsR4NKSzVyPUCuNFQzPzJizszN NVrLbHBwW0GQR1XS
H9 NHfYRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXlTWM2OD1yLkC0N|cyKM7:TR?= NETkXVJUSU6JRWK=
VA-ES-BJ M3zaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnJO|F[UUN3ME2wMlA1PDR5IN88US=> NX3wT2Q3W0GQR1XS
MEL-JUSO M1vsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP4TWM2OD1yLkC0OFc2KM7:TR?= MVTTRW5ITVJ?
BT-474 MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMES1JO69VQ>? NHiwNVdUSU6JRWK=
CaR-1 M4POOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPXcnlKSzVyPUCuNFQ2PDlizszN MnjyV2FPT0WU
PSN1 NFfxOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHLR|BKSzVyPUCuNFQ3ODNizszN NH;rUWJUSU6JRWK=
KYSE-510 MkfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzSTWM2OD1yLkC0OlQ6KM7:TR?= NGToeWhUSU6JRWK=
KP-4 NF76RlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jHZmlEPTB;MD6wOFc2OyEQvF2= M3jRNnNCVkeHUh?=
KYSE-410 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q4fmlEPTB;MD6wOFc4OiEQvF2= MXHTRW5ITVJ?
G-402 NUXsOmxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXGW|VLUUN3ME2wMlA1Pzh7IN88US=> NFTONFBUSU6JRWK=
DOK MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHGzbJFKSzVyPUCuNFQ6ODJizszN NELVOY9USU6JRWK=
COR-L88 M4nFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXhZohKSzVyPUCuNFQ6OTJizszN NH;pW4tUSU6JRWK=
SKG-IIIa M1rxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlWwTWM2OD1yLkC0PVg3KM7:TR?= NF;qOYpUSU6JRWK=
AN3-CA MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMEWg{txO M2XPT3NCVkeHUh?=
SW48 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGezdWFKSzVyPUCuNFUxOzlizszN NIrPeZVUSU6JRWK=
YKG-1 M17IOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33HNmlEPTB;MD6wOVA4OSEQvF2= MnzZV2FPT0WU
KYSE-150 NXf1dFcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwMEWyN|Uh|ryP NWnVTY9NW0GQR1XS
HuO-3N1 NGLhVYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojMTWM2OD1yLkC1NlM4KM7:TR?= NXrN[|NDW0GQR1XS
LB1047-RCC NUKyT2YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2CwdWlEPTB;MD6wOVI6PiEQvF2= MYTTRW5ITVJ?
NCI-H2030 NYLSS|FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfjTWM2OD1yLkC1OFE1KM7:TR?= MX3TRW5ITVJ?
YH-13 M{f6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHz5eVdKSzVyPUCuNFU4OjJizszN NFn1OpZUSU6JRWK=
5637 MknnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojzTWM2OD1yLkC1O|Qh|ryP NH;abZlUSU6JRWK=
LOXIMVI M4Pyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Po[WlEPTB;MD6wOVg4OiEQvF2= M2rHTHNCVkeHUh?=
GT3TKB NX3zNJJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nTTmlEPTB;MD6wOVk1OiEQvF2= Mlz5V2FPT0WU
TCCSUP NIO0eoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnqPZpkUUN3ME2wMlA2QTZ2IN88US=> M4i4c3NCVkeHUh?=
EPLC-272H MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDiS2JKSzVyPUCuNFYzODVizszN M4i1bnNCVkeHUh?=
LU-99A NHzMbYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwME[yN|ch|ryP NF\Se2tUSU6JRWK=
NCI-H1755 M4jKemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwME[zOFEh|ryP MoTRV2FPT0WU
KM12 NUjkVXN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fFd2lEPTB;MD6wOlM1QCEQvF2= NGPRWoVUSU6JRWK=
SF295 NWLGeJM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7zTWM2OD1yLkC2OFUzKM7:TR?= NHLqe5hUSU6JRWK=
MZ2-MEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jhNGlEPTB;MD6wOlU2OyEQvF2= NHux[GVUSU6JRWK=
HEC-1 NXHCUHlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHDTmhKSzVyPUCuNFY2QDhizszN M4jsb3NCVkeHUh?=
SW684 M3PsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX36SHJ6UUN3ME2wMlA3PTlzIN88US=> NXTiR21CW0GQR1XS
SF539 NVTocZlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HjVmlEPTB;MD6wOlY5OSEQvF2= M{[xUnNCVkeHUh?=
GMS-10 M2qzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLnTWM2OD1yLkC2Olk6KM7:TR?= M1LvTXNCVkeHUh?=
MV-4-11 MnvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPPTWZKSzVyPUCuNFY5ODNizszN NWXuZm1uW0GQR1XS
HT-29 NWftVIRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrvUnpTUUN3ME2wMlA3QTF7IN88US=> M3vMWHNCVkeHUh?=
23132-87 M2PCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHVe4ZnUUN3ME2wMlA3QTVizszN NVu4[2lpW0GQR1XS
SW620 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX2NIRKSzVyPUCuNFcxOjZizszN NHXmXoFUSU6JRWK=
HCC1806 M2D4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\uTWM2OD1yLkC3NVMyKM7:TR?= NWHGbXBUW0GQR1XS
Hs-578-T NWK1b|FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwMEeyNFgh|ryP MorsV2FPT0WU
A2058 NH7SdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK3UnBPUUN3ME2wMlA4OjJ6IN88US=> MmnGV2FPT0WU
MEL-HO NUHobZFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonPTWM2OD1yLkC3NlU2KM7:TR?= NHf5[3NUSU6JRWK=
HCC2998 NGTiNJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXiPXRKSzVyPUCuNFc{PDdizszN M2rkbHNCVkeHUh?=
HuO9 NGjqVXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfqdHBKSzVyPUCuNFc2QDlizszN Mn\hV2FPT0WU
CAL-39 M4Ts[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzUW29xUUN3ME2wMlA4PzZ4IN88US=> MX;TRW5ITVJ?
M14 NIPRNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwMEe5NVMh|ryP M37DdHNCVkeHUh?=
BFTC-909 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXre|V5UUN3ME2wMlA4QTZ7IN88US=> NU\RS5VRW0GQR1XS
TE-11 M2nGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;veldKSzVyPUCuNFc6QTZizszN MWLTRW5ITVJ?
TGBC1TKB M1fuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMEiwOFMh|ryP M1TZdHNCVkeHUh?=
L-363 NEjHZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq4TWM2OD1yLkC4NlA3KM7:TR?= MlvIV2FPT0WU
A431 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33k[WlEPTB;MD6wPFIyKM7:TR?= NXfkdWJ[W0GQR1XS
MKN45 MmHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXwNZVNUUN3ME2wMlA5OjF7IN88US=> NEXFVWNUSU6JRWK=
HT-1080 NU\iN|ZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjqOpJQUUN3ME2wMlA5PDN7IN88US=> MoHvV2FPT0WU
OVCAR-8 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PHVWlEPTB;MD6wPFYzOiEQvF2= NVXUdpRIW0GQR1XS
LCLC-97TM1 NVvWT|hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULJVo1iUUN3ME2wMlA5PzJ6IN88US=> NHrVTJdUSU6JRWK=
M059J MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHxeFhKSzVyPUCuNFkxOjdizszN NH;JOndUSU6JRWK=
SK-MEL-2 M2HoXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjtTWM2OD1yLkC5NFYh|ryP NFvRNm5USU6JRWK=
TE-1 M2S4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXIeVlKSzVyPUCuNFkzODRizszN MnK3V2FPT0WU
KYSE-180 NFr5TFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWS4TmRvUUN3ME2wMlA6OjZ{IN88US=> MkLWV2FPT0WU
D-247MG NUDQVVJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjWbXJYUUN3ME2wMlA6PDV3IN88US=> NH3SPIlUSU6JRWK=
8-MG-BA MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu3cIdKSzVyPUCuNFk1PzJizszN NHzzbpVUSU6JRWK=
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NCI-H1793 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwM{i1NUDPxE1? MWrTRW5ITVJ?
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NCI-H1703 NFnO[|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLTTWM2OD1yLkSxOFQ3KM7:TR?= MoPEV2FPT0WU
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CTV-1 NInR[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD4S4JFUUN3ME2wMlUzPjZ7IN88US=> M{[wSHNCVkeHUh?=
PANC-08-13 NFz4b3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPLTWM2OD1yLkWzNVc4KM7:TR?= M2\ScnNCVkeHUh?=
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NCI-H2126 NV3qTldxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz0TWM2OD1yLkW2PFE2KM7:TR?= NWfqR4wzW0GQR1XS
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NCI-H661 NV[2eHRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPaV49KSzVyPUCuOlEyODRizszN NUnUO3BsW0GQR1XS
UACC-893 M3:2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwNkO2PFEh|ryP MmflV2FPT0WU
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SF268 Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH75[INKSzVyPUCuOlQ{PDlizszN MVXTRW5ITVJ?
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RPMI-8226 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTHRlhKSzVyPUCuOlY{OjNizszN Mn7tV2FPT0WU
MKN28 NV;qfmZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XDR2lEPTB;MD62OlYzPCEQvF2= NX;BbpFMW0GQR1XS
MDA-MB-453 M1H4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjWN3RrUUN3ME2wMlY4OThizszN NHSxdnFUSU6JRWK=
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NCI-H358 MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXyTWM2OD1yLk[4O|I3KM7:TR?= MmTKV2FPT0WU
NCI-H1651 NYjtRpM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\qTWM2OD1yLkeg{txO NHPZU3NUSU6JRWK=
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EFM-19 MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrhTIJUUUN3ME2wMlc{PjdzIN88US=> M3e5RnNCVkeHUh?=
RERF-LC-MS M{f0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moe1TWM2OD1yLke0OlE{KM7:TR?= MoXsV2FPT0WU
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UACC-257 NXLGbY9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTufJhmUUN3ME2wMlgzOjNzIN88US=> NGDKT|NUSU6JRWK=
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NCI-H2009 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP2bpBKSzVyPUCuPFU{OTFizszN NWLvU2NXW0GQR1XS
NCI-H522 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvpZnlKSzVyPUCuPFc4QDNizszN Mly3V2FPT0WU
Saos-2 NFPqcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTBwOEe4O|Eh|ryP MoSzV2FPT0WU
NB17 M4K5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3NTWM2OD1yLki4NFI2KM7:TR?= NHj3VY9USU6JRWK=
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P12-ICHIKAWA M{X5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXpbGFKSzVyPUeuOFU2OjNizszN MXPTRW5ITVJ?
NCI-H82 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzDSGU5UUN3ME23MlQ2PzBzIN88US=> Mkj2V2FPT0WU
NCI-H1993 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTdwOEOwOlMh|ryP NVTy[XhTW0GQR1XS
RH-1 M{LIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTdwOEWyOFQh|ryP NHjwcFJUSU6JRWK=
SW948 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLtTWM2OD15Lkm2NFQ6KM7:TR?= MXHTRW5ITVJ?
CAL-33 MoXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LQZmlEPTB;Nz65PVk{QCEQvF2= MorIV2FPT0WU
U-266 NYfYfHFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRThwMUW3O|ch|ryP Mk\MV2FPT0WU
CAL-72 M2nHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTKd|JKSzVyPUiuNlA{OiEQvF2= NHfBZnlUSU6JRWK=
SNU-423 NF7nO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTlwM{[2OlYh|ryP NWD2eVN7W0GQR1XS
KG-1 NWK4fohzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLFbJBlUUN3ME25MlU5PDV4IN88US=> M3XQbHNCVkeHUh?=
HCC1395 NX75dYhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jmN2lEPTB;OT65NlM2OiEQvF2= NYjhUXllW0GQR1XS
BE-13 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zLXmlEPTB;MUCuPFg6OiEQvF2= M{nRU3NCVkeHUh?=
MKN7 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DK[WlEPTB;MUCuPVc3PSEQvF2= MWDTRW5ITVJ?
697 M{GxR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3PTWM2OD1zMT6xOFczKM7:TR?= MnyzV2FPT0WU
LU-135 M3fVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XGdWlEPTB;MUGuNlMxPyEQvF2= MXLTRW5ITVJ?
ES7 M{L6dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLCTWM2OD1zMT6zN|E{KM7:TR?= MYnTRW5ITVJ?
SK-HEP-1 NWHwbY1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki3TWM2OD1zMT63OlQ3KM7:TR?= NEH1fHFUSU6JRWK=
BEN Mk[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFzLki1NUDPxE1? NF3zbXFUSU6JRWK=
NCI-H1770 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDGNYpKSzVyPUGyMlEzPiEQvF2= NHr0TopUSU6JRWK=
SW13 NIjYS5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTF{LkG1OFEh|ryP MX\TRW5ITVJ?
MZ1-PC M4nqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXDd3BKSzVyPUGyMlU1PTJizszN NIfHUppUSU6JRWK=
Mo-T M2TOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nDNGlEPTB;MUKuO|QzOSEQvF2= MkC2V2FPT0WU
HLE M2nxUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPR[YtIUUN3ME2xNk45OjF3IN88US=> NEPBVplUSU6JRWK=
RCC10RGB NXvC[pA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTF|Lk[3NUDPxE1? NGjjdo9USU6JRWK=
COLO-320-HSR NV[3[ooyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF|LkezPFEh|ryP NGD4cWZUSU6JRWK=
BHT-101 NHfsOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jofmlEPTB;MUOuPFM1PSEQvF2= M4K4SHNCVkeHUh?=
OCUB-M MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTITWM2OD1zND6xOlAzKM7:TR?= NVW0eZJ4W0GQR1XS
MEG-01 Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHKTWM2OD1zND6zO|A5KM7:TR?= MVnTRW5ITVJ?
RS4-11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHvW2FVUUN3ME2xOE44PDJizszN NHT6ZYZUSU6JRWK=
MN-60 Mn62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2yWIhKSzVyPUG0Mlc5QTRizszN NWfvPZl7W0GQR1XS
NCI-H1304 NEXzWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfDbmxLUUN3ME2xOU4xPDJ3IN88US=> NFHlPGNUSU6JRWK=
Ramos-2G6-4C10 M3iyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrlTWM2OD1zNT6wOVgyKM7:TR?= MULTRW5ITVJ?
NCI-H2342 NHrCeZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnteJRKSzVyPUG1MlIxPDRizszN M4i0ZnNCVkeHUh?=
LAN-6 NVThcpI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF3LkS0NVQh|ryP M1HoSXNCVkeHUh?=
JVM-2 NIH4bWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILqe2tKSzVyPUG1MlU4PDhizszN NUjyVJdYW0GQR1XS
P30-OHK MmS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2OxXWlEPTB;MU[uNFYyPCEQvF2= MmHLV2FPT0WU
C-33-A NXPJSnRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrRWmlKSzVyPUG2MlYzOTRizszN M3m2RXNCVkeHUh?=
RPMI-8866 NXz3XXZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfrO4k1UUN3ME2xOk45PDl4IN88US=> NIrpXVhUSU6JRWK=
NCI-H630 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmriTWM2OD1zNj64OVM4KM7:TR?= NEC3cVRUSU6JRWK=
KYSE-140 NHPVeVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2e0N2lEPTB;MUeuNlAzQCEQvF2= NFXGV|ZUSU6JRWK=
T84 MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml32TWM2OD1zOD64Olk2KM7:TR?= NUHSeJIzW0GQR1XS
KU-19-19 M2TD[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF6Lkm2NFgh|ryP NYHTeFZQW0GQR1XS
BALL-1 NEjsZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTub|dKSzVyPUG5MlM{QTlizszN MXjTRW5ITVJ?
Calu-6 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;3dGlEPTB;MUmuOFkzKM7:TR?= Mk[5V2FPT0WU
EGI-1 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u1R2lEPTB;MUmuOVk5KM7:TR?= MWXTRW5ITVJ?
MFH-ino NV;nS2pDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjOTWM2OD1zOT63OFU1KM7:TR?= M4\sbHNCVkeHUh?=
GB-1 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLLZpZVUUN3ME2yNE4{PTN3IN88US=> MVvTRW5ITVJ?
NCI-H1693 MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJyLk[1NFUh|ryP M13FdHNCVkeHUh?=
SW1116 NVvlTWxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nMR2lEPTB;MkCuPVM3OiEQvF2= Mnu5V2FPT0WU
H-EMC-SS MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnewTWM2OD1{Mj6wOFUh|ryP MnXEV2FPT0WU
D-502MG NFzU[WRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT6SIE{UUN3ME2yNk45OjZzIN88US=> NIjNUGFUSU6JRWK=
IA-LM M4nJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrwfo16UUN3ME2yN{4zPDl|IN88US=> NWOze5pJW0GQR1XS
SW1463 NFnEWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnWTWM2OD1{Mz63PUDPxE1? NHjsZXNUSU6JRWK=
JAR MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLpTWM2OD1{ND6zNlk{KM7:TR?= NETGTYFUSU6JRWK=
HT NF:4NoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfxfGF3UUN3ME2yOE41PzV|IN88US=> MYHTRW5ITVJ?
LCLC-103H NXmzbHlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLTTWM2OD1{ND64OFQ6KM7:TR?= NHGz[ItUSU6JRWK=
SNU-449 M{HSXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ2Lki3OFEh|ryP NFr0TlZUSU6JRWK=
KE-37 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrnb3dKSzVyPUK1MlA6OjhizszN NHTreZFUSU6JRWK=
NCI-H1623 M1\ZdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LhO2lEPTB;MkeuNVMxOyEQvF2= MmHEV2FPT0WU
MOLT-13 NXXLUIhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ5LkO1NVYh|ryP M4fS[nNCVkeHUh?=
COLO-741 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTNzLkOzN|Mh|ryP MUPTRW5ITVJ?
NB6 NYLtN5FbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3FfZZlUUN3ME2zNk4zQDd4IN88US=> M3\4TXNCVkeHUh?=
MOLT-16 NX;xVo1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSTWM2OD1|Mz6wNFU2KM7:TR?= NWHuOXpLW0GQR1XS
IST-MES1 MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTN2LkC1OFEh|ryP MmDFV2FPT0WU
A4-Fuk NYHGVoUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\hbYtyUUN3ME2zOU4xPjZizszN MmewV2FPT0WU
CAL-85-1 NUXGSnVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmixTWM2OD1|NT6yPFE4KM7:TR?= MVrTRW5ITVJ?
CCRF-CEM M2\Ecmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:4N3JiUUN3ME2zO{4yPTN4IN88US=> Mn;lV2FPT0WU
HAL-01 M{iwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXtOpFKSzVyPUO4MlQ5QDlizszN M3TNbHNCVkeHUh?=
HEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTR|LkO0NFkh|ryP M3ntWHNCVkeHUh?=
EW-1 M1m5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvQRo4yUUN3ME20N{41PzZ6IN88US=> M2\lUnNCVkeHUh?=
MDA-MB-231 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfCUW1KSzVyPUS1MlEyQTlizszN M1W1WXNCVkeHUh?=
ABC-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\3UIFMUUN3ME20Ok45PTN6IN88US=> M3\5VXNCVkeHUh?=
NCI-H446 M3v4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXVbIlKSzVyPUS4MlUxPThizszN NHLKTnFUSU6JRWK=
MHH-PREB-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi0RXZKSzVyPUS5MlYxODdizszN NFjaUZVUSU6JRWK=
DOHH-2 NIjpeXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;xTWM2OD12OT62OlU3KM7:TR?= MWTTRW5ITVJ?
GCT NWnud3NxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi5eVlKSzVyPUS5MlY6PzZizszN NW\teVdWW0GQR1XS

... 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

selleck catalog

HSP (e.g. HSP90) Signaling Pathway Map

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

  • Selective HSP90 Inhibitor

    NVP-BEP800 : HSP90β-selective, IC50=58 nM.

  • Most Potent HSP90 Inhibitor

    KW-2478 : HSP90, IC50=3.8 nM.

  • HSP90 Inhibitor in Clinical Trial

    17-DMAG (Alvespimycin) HCl : Phase II for Kidney Cancer.

  • Newest HSP90 Inhibitor

    XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

Related HSP (e.g. HSP90) Products

  • PU-H71 New

    PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

  • KNK437 New

    KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

  • VER155008 New

    VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

  • Luminespib (AUY-922, NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.

  • Ganetespib (STA-9090)

    Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.

  • Alvespimycin (17-DMAG) HCl

    Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

    Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.

  • Geldanamycin

    Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

  • HSP990 (NVP-HSP990)

    NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM.

    Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.

  • Elesclomol (STA-4783)

    Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.

  • Onalespib (AT13387)

    Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID