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.

Size Price Stock Quantity  
In DMSO USD 195 In stock
USD 150 In stock
USD 370 In stock

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7 Customer Reviews

  • (A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h.

    PNAS, 2011, 108: 7535-40. Tanespimycin (17-AAG) purchased from Selleck.

    Four types of the colon cancer cells with indicated K-Ras phenotype were incubated with indicated concentration of 17-AAG for 24 h, which were then analyzed for protein expression by WB.

    Oncotarget 2014 5, 4269-82. Tanespimycin (17-AAG) purchased from Selleck.

  • Western blot analysis of immunoprecipitated Hsp90/BIP complexes in MOLT-4 (T-ALL) and RS4;11 (B-ALL) treated for 22 h with CX-4945 (5 μM) and bortezomib (2.5 nM) either alone or in combination. 500 μg of protein lysates were immunoprecipitated with anti-Hsp90 antibody. Relative Induction values (Rel.Ind.) were obtained by normalizing to Hsp90 bands density. 17-AAG: tanespimycin.

    Oncotarget, 2015, 51: S659-S660. Tanespimycin (17-AAG) purchased from Selleck.

    UPR modulators destabilize mSmoM2. NIH 3T3 cells expressing mSmoM2 protein were treated with HSP90 inhibitors 17-AAG (50 uM and 100 uM) and SNX-2112 (25 uM and 50 uM) and the proteasome inhibitor bortezomib (25 uM and 50 uM) for 4 h prior to lysis. DMSO was the vehicle control. Western blotting of whole-cell lysates revealed mSmoM2 protein to be destabilized in response to HSP-90 inhibitors but not in response to bortezomib. Tubulin was the loading control. CHOP results indicate ER stress.

    Mol Cell Biol 2013 33(12), 2375-87. Tanespimycin (17-AAG) purchased from Selleck.

  • Treatment with an Hsp90 inhibitor results in a dose-dependent decrease in complex IV activity. A, because Hsp90 levels were reduced by 80%, in PINK1 null dopaminergic neuronal cells, the effects of specific inhibition of Hsp90 using 17-AAG were analyzed in wild-type neuronal cells. Both complex IV activity and Hsp60 levels were decreased significantly in 17-AAG-treated cells in a dose-dependent manner. B, in contrast, 17-AAG treatment did not affect expression of Hsp90 and LRPPRC.

    J Biol Chem 2012 287, 44109-20. Tanespimycin (17-AAG) purchased from Selleck.

    SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.

    Mol Cancer 2014 13, 150. Tanespimycin (17-AAG) purchased from Selleck.

  • Hsp90 is up-regulated during aging. Whole-cell extracts were prepared from young (PD 20) and old (PD 40) HFSN1 cells. c HFSN1 cells (PD 40) were treated with different concentration of the Hsp90 inhibitor (17-AAG) and then re-incubated for 24 h. Whole-cell extracts were prepared and analyzed by western blot using the indicated antibodies.

    Age 2013 35, 549-62. Tanespimycin (17-AAG) purchased from Selleck.

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 NH3UcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LrNWlEPTB;MD6wNFA{ODNizszN M2LkdHNCVkeHUh?=
IST-MEL1 M4f0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXkTWM2OD1yLkCwNFQxPyEQvF2= MlL2V2FPT0WU
NCI-SNU-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DsfWlEPTB;MD6wNFIxPyEQvF2= M1ruXnNCVkeHUh?=
FADU MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrWcY9CUUN3ME2wMlAxOjB7IN88US=> NHuwSXJUSU6JRWK=
C32 NX;lPHAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwMECzNFQh|ryP NHHKU4hUSU6JRWK=
D-566MG Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILHZpRKSzVyPUCuNFA{QSEQvF2= MoHYV2FPT0WU
LXF-289 NYfjeHMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W5O2lEPTB;MD6wNFQyQSEQvF2= MlTjV2FPT0WU
HGC-27 NILmSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfXWphKSzVyPUCuNFA2OSEQvF2= NIDzbGZUSU6JRWK=
RPMI-7951 NI\PeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHGR4lKSzVyPUCuNFA4OTdizszN MWfTRW5ITVJ?
HSC-3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW0TWM2OD1yLkCwPVI6KM7:TR?= M372cHNCVkeHUh?=
MIA-PaCa-2 MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnhXJZwUUN3ME2wMlAyODB7IN88US=> MYjTRW5ITVJ?
KS-1 M4fTfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwMEGzOVUh|ryP M{LWbnNCVkeHUh?=
CAL-51 M3;hc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwMEG0NFUh|ryP NVn6SItuW0GQR1XS
MDA-MB-361 NVHSXopOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMEG0PVUh|ryP Mnz2V2FPT0WU
TI-73 NXLuNFFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzpdI1KSzVyPUCuNFE4QTZizszN NWnodXpVW0GQR1XS
AGS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwMEG5N|gh|ryP MXrTRW5ITVJ?
NCI-H460 NFvpXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKxSmt3UUN3ME2wMlAyQTd2IN88US=> MVHTRW5ITVJ?
A204 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH63eW1KSzVyPUCuNFIzPDlizszN NEnsepZUSU6JRWK=
CHL-1 M134cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nJSmlEPTB;MD6wNlI2OSEQvF2= M{K2ZnNCVkeHUh?=
DU-4475 NH7KfnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfxUIRZUUN3ME2wMlAzOjZzIN88US=> NHPnfnlUSU6JRWK=
CGTH-W-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETVbnZKSzVyPUCuNFI{PDlizszN NFr4bm1USU6JRWK=
HCC2218 NEjUNolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwMEK0PVQh|ryP NFT3bWFUSU6JRWK=
A2780 NXewV4t[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwMEK1N|Eh|ryP MY\TRW5ITVJ?
NCI-H720 Mnz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEK1OFYh|ryP M3zDVnNCVkeHUh?=
NCI-N87 MnfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULifWhOUUN3ME2wMlAzPTl|IN88US=> NXzofYtyW0GQR1XS
CHP-212 NGXwfY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M171SGlEPTB;MD6wNlYzQCEQvF2= MnLTV2FPT0WU
NCI-H23 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzoSIM1UUN3ME2wMlAzPjZ3IN88US=> MX3TRW5ITVJ?
D-263MG MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMEK3PFYh|ryP NW\Nd|hTW0GQR1XS
ME-180 MoH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33DTGlEPTB;MD6wNlg6OSEQvF2= MXrTRW5ITVJ?
SW982 M2LYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S2dWlEPTB;MD6wNlk6QSEQvF2= NIPUc2dUSU6JRWK=
OE19 MnHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PG[2lEPTB;MD6wN|A4PyEQvF2= MXjTRW5ITVJ?
SK-LU-1 M37pd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTTTFAyUUN3ME2wMlA{ODh{IN88US=> MoLiV2FPT0WU
H4 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\iR2lEPTB;MD6wN|A6KM7:TR?= MUfTRW5ITVJ?
HT-144 NY\jNnJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMEOwPVMh|ryP MnL2V2FPT0WU
SK-UT-1 NEG5e3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMEOxO|gh|ryP MVLTRW5ITVJ?
D-336MG NHT5[5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMEOzNFkh|ryP M{HjNnNCVkeHUh?=
MDA-MB-175-VII NIrIN3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;wPVREUUN3ME2wMlA{OzV2IN88US=> MknjV2FPT0WU
GAMG NIC5[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMEO0N|Uh|ryP NXjWSohGW0GQR1XS
CP50-MEL-B MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHrV5BKSzVyPUCuNFM1PSEQvF2= M3;UWnNCVkeHUh?=
OVCAR-5 NEXDR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz3bFhKSzVyPUCuNFM1QCEQvF2= M1\BW3NCVkeHUh?=
SK-MES-1 NXX6NJFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn6xTWM2OD1yLkCzOlA3KM7:TR?= MlHzV2FPT0WU
VM-CUB-1 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7VTWM2OD1yLkCzOlU4KM7:TR?= M2Lnc3NCVkeHUh?=
WM-115 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr0W29KSzVyPUCuNFM4PjJizszN MlrwV2FPT0WU
DSH1 M1vneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33Od2lEPTB;MD6wN|gxPyEQvF2= NV3QWWZtW0GQR1XS
Becker M{Xzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;1emkxUUN3ME2wMlA{QDh3IN88US=> NHTVd3JUSU6JRWK=
SW962 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW1R2RKSzVyPUCuNFM6PDVizszN M4DBS3NCVkeHUh?=
TYK-nu NIPa[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTvS5NOUUN3ME2wMlA{QTh3IN88US=> Mnu2V2FPT0WU
HO-1-N-1 NHzrNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHewcVVKSzVyPUCuNFQxOjFizszN MnvzV2FPT0WU
T98G M4\tNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3SxSWlEPTB;MD6wOFExOyEQvF2= Mn\YV2FPT0WU
ACN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwMESxOlIh|ryP NHnLNYJUSU6JRWK=
SW780 M{LaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTuSXV{UUN3ME2wMlA1OjB|IN88US=> NGj0c45USU6JRWK=
Detroit562 NVrYWY9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMESyN|kh|ryP MnXiV2FPT0WU
BB49-HNC Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DUWmlEPTB;MD6wOFI1OyEQvF2= NYDSNHhPW0GQR1XS
HN MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED2R5dKSzVyPUCuNFQzPzJizszN NYOyTlhbW0GQR1XS
H9 M3jMSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPOTWM2OD1yLkC0N|cyKM7:TR?= NVrzOlhHW0GQR1XS
VA-ES-BJ NUXDZohDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17qfWlEPTB;MD6wOFQ1PyEQvF2= MVHTRW5ITVJ?
MEL-JUSO NH3OUmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXYZmtbUUN3ME2wMlA1PDd3IN88US=> MnfEV2FPT0WU
BT-474 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XrRmlEPTB;MD6wOFUh|ryP NYr2PFl{W0GQR1XS
CaR-1 NHLGV49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3tcJRKSzVyPUCuNFQ2PDlizszN Moj6V2FPT0WU
PSN1 NW\COItsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XoS2lEPTB;MD6wOFYxOyEQvF2= NVrsR5BuW0GQR1XS
KYSE-510 NGnNfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwMES2OFkh|ryP M4nDbXNCVkeHUh?=
KP-4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwMES3OVMh|ryP MlTxV2FPT0WU
KYSE-410 M1\w[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG1O45KSzVyPUCuNFQ4PzJizszN M3PSU3NCVkeHUh?=
G-402 NVnpN|Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHkb5hKSzVyPUCuNFQ4QDlizszN Mn;zV2FPT0WU
DOK MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTiTWM2OD1yLkC0PVAzKM7:TR?= MUjTRW5ITVJ?
COR-L88 NVHkT|VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwMES5NVIh|ryP NH\peJNUSU6JRWK=
SKG-IIIa MkfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwMES5PFYh|ryP NGHWW2ZUSU6JRWK=
AN3-CA NEjYPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;sTWM2OD1yLkC1JO69VQ>? MWfTRW5ITVJ?
SW48 NYrIRnRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPHcodKSzVyPUCuNFUxOzlizszN NIXkcHRUSU6JRWK=
YKG-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j1Z2lEPTB;MD6wOVA4OSEQvF2= NIDwWmdUSU6JRWK=
KYSE-150 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3Mcm94UUN3ME2wMlA2OjN3IN88US=> NIizVYxUSU6JRWK=
HuO-3N1 NVz4OJJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nJVWlEPTB;MD6wOVI{PyEQvF2= NI\zfoNUSU6JRWK=
LB1047-RCC M2OzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwMEWyPVYh|ryP NHrQb3NUSU6JRWK=
NCI-H2030 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHoTWM2OD1yLkC1OFE1KM7:TR?= NYDieGRCW0GQR1XS
YH-13 NUHMSHlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Lve2lEPTB;MD6wOVczOiEQvF2= MWTTRW5ITVJ?
5637 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\OXpVrUUN3ME2wMlA2PzRizszN NFHtd2ZUSU6JRWK=
LOXIMVI MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfrXW9KSzVyPUCuNFU5PzJizszN NXTIRWhoW0GQR1XS
GT3TKB MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rNfGlEPTB;MD6wOVk1OiEQvF2= M3\oenNCVkeHUh?=
TCCSUP NEDaWWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPISYlFUUN3ME2wMlA2QTZ2IN88US=> MlzpV2FPT0WU
EPLC-272H M1T3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvmfHZKSzVyPUCuNFYzODVizszN MoPhV2FPT0WU
LU-99A NXzhRow1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwME[yN|ch|ryP M3HGd3NCVkeHUh?=
NCI-H1755 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\HbGlEPTB;MD6wOlM1OSEQvF2= NYTsWYJ1W0GQR1XS
KM12 NXnYT4RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwME[zOFgh|ryP NF6w[nJUSU6JRWK=
SF295 M3jBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TBd2lEPTB;MD6wOlQ2OiEQvF2= MX7TRW5ITVJ?
MZ2-MEL M2\4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj2V5FKSzVyPUCuNFY2PTNizszN MmHHV2FPT0WU
HEC-1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTtTWM2OD1yLkC2OVg5KM7:TR?= NH;YdJFUSU6JRWK=
SW684 M1\uPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PpSGlEPTB;MD6wOlU6OSEQvF2= M3[1cHNCVkeHUh?=
SF539 M4jmTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVy4U21FUUN3ME2wMlA3PjhzIN88US=> NYPJdXpGW0GQR1XS
GMS-10 MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LafWlEPTB;MD6wOlY6QSEQvF2= NWfNOph[W0GQR1XS
MV-4-11 NVjvboxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\YeFRKSzVyPUCuNFY5ODNizszN NHXUNnRUSU6JRWK=
HT-29 M4Pu[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XtZ2lEPTB;MD6wOlkyQSEQvF2= NVTFeGQ3W0GQR1XS
23132-87 M37pT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDST|lKSzVyPUCuNFY6PSEQvF2= M{D2bHNCVkeHUh?=
SW620 M3i5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD6c|F{UUN3ME2wMlA4ODJ4IN88US=> NH:1ZWZUSU6JRWK=
HCC1806 M1Xz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C4[mlEPTB;MD6wO|E{OSEQvF2= MUnTRW5ITVJ?
Hs-578-T M1fRbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMEeyNFgh|ryP MknGV2FPT0WU
A2058 M4X3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M364bWlEPTB;MD6wO|IzQCEQvF2= NFrhdVFUSU6JRWK=
MEL-HO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rIS2lEPTB;MD6wO|I2PSEQvF2= NFvLO29USU6JRWK=
HCC2998 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\nTWM2OD1yLkC3N|Q4KM7:TR?= NFvVS5NUSU6JRWK=
HuO9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwMEe1PFkh|ryP MXjTRW5ITVJ?
CAL-39 MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\vPWlEPTB;MD6wO|c3PiEQvF2= NV64S29DW0GQR1XS
M14 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm1WFV{UUN3ME2wMlA4QTF|IN88US=> MUTTRW5ITVJ?
BFTC-909 NWDpPW55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfkTWM2OD1yLkC3PVY6KM7:TR?= MnG4V2FPT0WU
TE-11 MmfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXjTWM2OD1yLkC3PVk3KM7:TR?= NHyyZohUSU6JRWK=
TGBC1TKB M{\SRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwMEiwOFMh|ryP NYDrNWc4W0GQR1XS
L-363 MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMEiyNFYh|ryP M1;uRXNCVkeHUh?=
A431 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HtcmlEPTB;MD6wPFIyKM7:TR?= M4nSZ3NCVkeHUh?=
MKN45 NX3tXHNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzqTWM2OD1yLkC4NlE6KM7:TR?= MmnaV2FPT0WU
HT-1080 NGTwOpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMEi0N|kh|ryP NXzROFJVW0GQR1XS
OVCAR-8 NEjVO5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMEi2NlIh|ryP MlnOV2FPT0WU
LCLC-97TM1 M3O4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVraSWE{UUN3ME2wMlA5PzJ6IN88US=> NYe3VoZGW0GQR1XS
M059J MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DlN2lEPTB;MD6wPVAzPyEQvF2= Mn3QV2FPT0WU
SK-MEL-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLjPJdKSzVyPUCuNFkxPiEQvF2= Moq1V2FPT0WU
TE-1 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfFZ3FKSzVyPUCuNFkzODRizszN MXjTRW5ITVJ?
KYSE-180 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK4eo1sUUN3ME2wMlA6OjZ{IN88US=> MnXqV2FPT0WU
D-247MG Mn7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlGxTWM2OD1yLkC5OFU2KM7:TR?= MlvwV2FPT0WU
8-MG-BA NHq1bG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTyTWM2OD1yLkC5OFczKM7:TR?= MXXTRW5ITVJ?
NCI-H1792 MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMEm2NVgh|ryP MWfTRW5ITVJ?
MCF7 MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMEm2O|ch|ryP M2DjSnNCVkeHUh?=
NCI-H2122 NXTOSGlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3CPXNmUUN3ME2wMlA6PzR3IN88US=> MVXTRW5ITVJ?
EFO-27 NXPUZVlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\oWmlEPTB;MD6wPVk6PyEQvF2= MVjTRW5ITVJ?
LB2241-RCC M{f5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfy[5RSUUN3ME2wMlExODV2IN88US=> MUjTRW5ITVJ?
SN12C M4rXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rRUWlEPTB;MD6xNFExPyEQvF2= MV;TRW5ITVJ?
A498 NETDSmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMUCxPEDPxE1? MoLHV2FPT0WU
PANC-03-27 NXm1S4JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwMUCyPFYh|ryP NYP1N3BoW0GQR1XS
NCI-H1581 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zPfGlEPTB;MD6xNFI6KM7:TR?= NWGySXRLW0GQR1XS
U-87-MG MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPkTWM2OD1yLkGwN|A4KM7:TR?= M3KwZXNCVkeHUh?=
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U251 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7uTWM2OD1yLkGwOVI2KM7:TR?= NU\odWR2W0GQR1XS
MMAC-SF M4XDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMUC1N|Eh|ryP NE\IPWxUSU6JRWK=
BB65-RCC NGXuUlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWW3dINVUUN3ME2wMlExPTV2IN88US=> MVrTRW5ITVJ?
NKM-1 Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjRTWM2OD1yLkGwOlY3KM7:TR?= MlHaV2FPT0WU
HD-MY-Z Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnFTWM2OD1yLkGwPFc{KM7:TR?= MkTXV2FPT0WU
TGBC11TKB NGTtSnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LmS2lEPTB;MD6xNFkxOyEQvF2= NHzH[IpUSU6JRWK=
COLO-679 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PSRWlEPTB;MD6xNVIyOSEQvF2= M37tO3NCVkeHUh?=
TE-8 NIO2NmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwMUGyOlQh|ryP NXW5RplwW0GQR1XS
SK-MEL-28 M2nwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPoS3NKSzVyPUCuNVE{OjFizszN NYXhVJZiW0GQR1XS
SH-4 M2DFSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfmTWM2OD1yLkGxN|U3KM7:TR?= M2XBc3NCVkeHUh?=
KALS-1 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTPTWM2OD1yLkGxN|k{KM7:TR?= MYnTRW5ITVJ?
RKO M4jaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[zeoxKSzVyPUCuNVE4PjRizszN NIP2eJBUSU6JRWK=
OMC-1 MkfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL5T5BKSzVyPUCuNVE4QTdizszN NGT0cI5USU6JRWK=
BT-549 NE\YXppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHVNnFKSzVyPUCuNVE4QTlizszN NV\FV3R6W0GQR1XS
NCI-H28 M2Tkb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\HPHl1UUN3ME2wMlEyQDF5IN88US=> MW\TRW5ITVJ?
RXF393 MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{n1bWlEPTB;MD6xNVk5OiEQvF2= M4TvOnNCVkeHUh?=
COLO-829 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLUTWM2OD1yLkGyNFA2KM7:TR?= Ml;FV2FPT0WU
HMV-II NHvqb3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDzVoI2UUN3ME2wMlEzODJizszN Mmj4V2FPT0WU
SW1990 NY\YRWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTHeoI{UUN3ME2wMlEzOTV5IN88US=> M2K3bXNCVkeHUh?=
NCI-H1437 NYGzRlNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3juSmlEPTB;MD6xNlE2PyEQvF2= NE\nVo5USU6JRWK=
SNB75 NYnMSWc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPyfHBKSzVyPUCuNVIyPjlizszN NXLiVYtrW0GQR1XS
EW-3 NIHESo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMUK2OlEh|ryP NVjYV3dKW0GQR1XS
SAS MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLKTWM2OD1yLkGyOlkh|ryP M1nte3NCVkeHUh?=
NCI-H1666 NUXTWXQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMUK3O|Qh|ryP MUXTRW5ITVJ?
A375 NWP3cFVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzVU|ZKSzVyPUCuNVI4PzhizszN NX3yd3J1W0GQR1XS
CAMA-1 NHTEVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H4S2lEPTB;MD6xNlkzPCEQvF2= MVzTRW5ITVJ?
HuP-T4 M{DWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH6T2kzUUN3ME2wMlEzQTR|IN88US=> MUjTRW5ITVJ?
NCI-H292 M{LzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:3cZNCUUN3ME2wMlE{OTFizszN MWLTRW5ITVJ?
PC-14 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPkTWM2OD1yLkGzNlEyKM7:TR?= NGfFWmVUSU6JRWK=
BPH-1 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSwPJVKSzVyPUCuNVM1OSEQvF2= NUHWbIw5W0GQR1XS
GAK NXvkS|Q3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrRXIRKUUN3ME2wMlE{PTZ5IN88US=> NGL3ZXFUSU6JRWK=
VMRC-RCZ NGDBN3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHQTWM2OD1yLkGzO|YzKM7:TR?= NEfHcIVUSU6JRWK=
SK-MEL-24 M4PVO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\6[mlEPTB;MD6xN|g4KM7:TR?= MX;TRW5ITVJ?
LB831-BLC NGXK[mVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXSTWM2OD1yLkGzPFg{KM7:TR?= MnnFV2FPT0WU
NCI-H2452 Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMUO5OVYh|ryP MWLTRW5ITVJ?
RT-112 M2TX[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TuTmlEPTB;MD6xOFA{PSEQvF2= NEPHd|lUSU6JRWK=
GP5d Mk\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX74Z|VSUUN3ME2wMlE1OTB2IN88US=> MoDFV2FPT0WU
LC-2-ad NGP0[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LU[2lEPTB;MD6xOFEzOSEQvF2= M3fX[XNCVkeHUh?=
MPP-89 NU\LNlJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;4cVFqUUN3ME2wMlE1OTJ3IN88US=> NILjSIRUSU6JRWK=
NUGC-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwMUS0O|gh|ryP MVLTRW5ITVJ?
GI-1 M3PMdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfqU|M1UUN3ME2wMlE1PTV6IN88US=> MV;TRW5ITVJ?
HCC1419 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K3VmlEPTB;MD6xOFU4PiEQvF2= NV7idFlDW0GQR1XS
SW1573 MoHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TQOWlEPTB;MD6xOFc2QCEQvF2= MUDTRW5ITVJ?
NCI-H2347 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HuOmlEPTB;MD6xOFg{QSEQvF2= NWCzfm5DW0GQR1XS
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639-V Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TsemlEPTB;MD6xOVAyOyEQvF2= MWLTRW5ITVJ?
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NCI-H1648 NILyU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjCe2FuUUN3ME2wMlE2OjN{IN88US=> NEXTOGlUSU6JRWK=
786-0 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ntNGlEPTB;MD6xOVM5OSEQvF2= MknhV2FPT0WU
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BxPC-3 NWDu[5M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW1TWM2OD1yLkG1PVY3KM7:TR?= M13hN3NCVkeHUh?=
CAL-62 MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMU[xOlkh|ryP NXPx[5lbW0GQR1XS
HCC1937 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwMU[yO|Uh|ryP MkW4V2FPT0WU
NCI-H1299 NHXycFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGweJFQUUN3ME2wMlE3Ojh3IN88US=> MV\TRW5ITVJ?
SW1088 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP5TY1KSzVyPUCuNVY1OTNizszN MXLTRW5ITVJ?
FTC-133 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMU[1OEDPxE1? NEPPdpVUSU6JRWK=
OC-314 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj5SGEzUUN3ME2wMlE3PjlizszN NH\GR5pUSU6JRWK=
SCC-9 NFW0VlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG4TWM2OD1yLkG2O|E3KM7:TR?= MoHYV2FPT0WU
HT-1376 NF;5eZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfGe5VKSzVyPUCuNVY6OzZizszN M{S2dHNCVkeHUh?=
U-2-OS M17I[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjNZ3VTUUN3ME2wMlE4OTd|IN88US=> MVnTRW5ITVJ?
COLO-824 NXLVW41UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknVTWM2OD1yLkG3Nlk1KM7:TR?= MnmxV2FPT0WU
BB30-HNC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y4NmlEPTB;MD6xO|M{KM7:TR?= NXzXSJBYW0GQR1XS
NCI-H2087 Mor0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z2dWlEPTB;MD6xO|M3QCEQvF2= NXXzbZExW0GQR1XS
NCI-H2170 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m5ZmlEPTB;MD6xO|U{PiEQvF2= MUjTRW5ITVJ?
SK-OV-3 NITpN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTBwMUe1O|Eh|ryP MkLuV2FPT0WU
MZ7-mel Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwMUe2OFkh|ryP MkLVV2FPT0WU
NCI-H650 NG\R[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVGxZXFvUUN3ME2wMlE4Pjh{IN88US=> NGPxeIxUSU6JRWK=
KOSC-2 NVrweXpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwMUe3N|Qh|ryP NVnTU3lwW0GQR1XS
SCC-4 MnLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnOUnNRUUN3ME2wMlE4Pzd5IN88US=> M3n5dnNCVkeHUh?=
MDA-MB-157 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwMUiwPFIh|ryP M3fwNnNCVkeHUh?=
KYSE-520 NEPxO45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXkNI5KSzVyPUCuNVgzKM7:TR?= NXzHVHlxW0GQR1XS
LK-2 M{jLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULQRVRPUUN3ME2wMlE5OzB|IN88US=> MXjTRW5ITVJ?
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IGROV-1 NGXBeXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;zfmlEPTB;MD6xPFQ1OyEQvF2= M4\aWXNCVkeHUh?=
DEL NEfIPJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LYW2lEPTB;MD6xPFQ2KM7:TR?= M2\NfHNCVkeHUh?=
NCI-H1395 MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjySIZIUUN3ME2wMlE5Pjh{IN88US=> NYe0OlU1W0GQR1XS
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CAL-27 M{LH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDTOpFKSzVyPUCuNVkxOjJizszN NG\WRZNUSU6JRWK=
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NCI-H1650 M3nQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMkCwOVch|ryP NY\GU|FGW0GQR1XS
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AM-38 Ml7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfzfYlSUUN3ME2wMlIxQDR6IN88US=> MonSV2FPT0WU
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HPAF-II MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMkGyOlQh|ryP NEjjOWFUSU6JRWK=
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MFE-280 NGPBN|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXxcYlKSzVyPUCuNlEzQThizszN NHTpcmVUSU6JRWK=
TE-9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MliyTWM2OD1yLkKxO|g3KM7:TR?= M4HEN3NCVkeHUh?=
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EoL-1-cell Mm\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3mWZA2UUN3ME2wMlIzOjB|IN88US=> NXOzdYR4W0GQR1XS
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... 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 <1 mg/mL
In vivo 5%DMSO+corn oil 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 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
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
NCT00514371 Completed Multiple Myeloma Bristol-Myers Squibb August 2007 Phase 2|Phase 3
NCT00779428 Completed Advanced Malignancies Bristol-Myers Squibb July 2006 Phase 2
NCT00354185 Terminated Adult Nasal Type Extranodal NK/T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Post-transplant Lymphoproliferative Disorder|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic 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|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Stage III Adult Burkitt Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Mixed Cell Lymphoma|Stage III Adult Diffuse Small Cleaved Cell Lymphoma|Stage III Adult Hodgkin Lymphoma|Stage III Adult Immunoblastic Large Cell Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Adult T-cell Leukemia/Lymphoma|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage III Mantle Cell Lymphoma|Stage III Marginal Zone Lymphoma|Stage III Mycosis Fungoides/Sezary Syndrome|Stage III Small Lymphocytic Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-cell Leukemia/Lymphoma|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Mycosis Fungoides/Sezary Syndrome|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenström Macroglobulinemia National Cancer Institute (NCI) May 2006 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID