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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9 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.

    (A) Treatment of DIPG cells with an HSP90 inhibitor, 17-AAG, resulted in decreased invasion toward SVZ hNPC CM at high doses. (B) Cell viability of DIPG cells treated with increasing doses of 17-AAG, by the CellTiter-Glo assay.

    Cell, 2017, 170(5):845-859.e19. 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.

  • Co-IP analyses of direct interaction between HSP90 and HIF-1α in 17-AAG (5 μM)-treated HSCs using antibodies against HSP90, HIF-1α or IgG (n = 2).

    Br J Pharmacol, 2017, 174(5):409-423. 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 NUPIcZAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT6TWM2OD1yLkCwNFMxOyEQvF2= NHmxO|RUSU6JRWK=
IST-MEL1 NX\a[GY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fGRmlEPTB;MD6wNFA1ODdizszN NVLtOo1LW0GQR1XS
NCI-SNU-1 Ml:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\LdGlEPTB;MD6wNFIxPyEQvF2= M2TFV3NCVkeHUh?=
FADU M4XLd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7q[IxKSzVyPUCuNFAzODlizszN NFPqSpNUSU6JRWK=
C32 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXoTWM2OD1yLkCwN|A1KM7:TR?= M1zkd3NCVkeHUh?=
D-566MG Mn34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT3fpU3UUN3ME2wMlAxOzlizszN MkXDV2FPT0WU
LXF-289 M4e4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOxTWM2OD1yLkCwOFE6KM7:TR?= MYDTRW5ITVJ?
HGC-27 M1PlVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[xTWM2OD1yLkCwOVEh|ryP NIWyVHBUSU6JRWK=
RPMI-7951 NF;PSlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInXXXBKSzVyPUCuNFA4OTdizszN Ml30V2FPT0WU
HSC-3 M2LDOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITCXm5KSzVyPUCuNFA6OjlizszN NEW5NWdUSU6JRWK=
MIA-PaCa-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfrfo9ZUUN3ME2wMlAyODB7IN88US=> MnLrV2FPT0WU
KS-1 MkT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwMEGzOVUh|ryP MmrGV2FPT0WU
CAL-51 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwMEG0NFUh|ryP NFvUNo9USU6JRWK=
MDA-MB-361 M2HvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ezN2lEPTB;MD6wNVQ6PSEQvF2= NUG5UGFPW0GQR1XS
TI-73 M2PJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMEG3PVYh|ryP NFvCVpBUSU6JRWK=
AGS MkX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;qPGxFUUN3ME2wMlAyQTN6IN88US=> NVHVWodXW0GQR1XS
NCI-H460 NYPEXm15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPFWXNZUUN3ME2wMlAyQTd2IN88US=> MlK4V2FPT0WU
A204 NH3tcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfkfndKSzVyPUCuNFIzPDlizszN M{fZOnNCVkeHUh?=
CHL-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq3VoJKSzVyPUCuNFIzPTFizszN NHS3ZYRUSU6JRWK=
DU-4475 M1LORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwMEKyOlEh|ryP MWXTRW5ITVJ?
CGTH-W-1 NUfRRohpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTmTWM2OD1yLkCyN|Q6KM7:TR?= NFzhNFFUSU6JRWK=
HCC2218 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfY[nlKSzVyPUCuNFI1QTRizszN MY\TRW5ITVJ?
A2780 NWG4OopmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwMEK1N|Eh|ryP MVfTRW5ITVJ?
NCI-H720 M2OyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMEK1OFYh|ryP MlXVV2FPT0WU
NCI-N87 NYrKO5oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS0dW1JUUN3ME2wMlAzPTl|IN88US=> NIjHNFdUSU6JRWK=
CHP-212 M{n5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq2ZXpKSzVyPUCuNFI3OjhizszN MofLV2FPT0WU
NCI-H23 NWPzbW1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jGVmlEPTB;MD6wNlY3PSEQvF2= NH2wXmFUSU6JRWK=
D-263MG NWmxdoJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXaTWM2OD1yLkCyO|g3KM7:TR?= Mn7yV2FPT0WU
ME-180 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjYTWM2OD1yLkCyPFkyKM7:TR?= MmW4V2FPT0WU
SW982 M4m3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrQTWM2OD1yLkCyPVk6KM7:TR?= NYXr[JY6W0GQR1XS
OE19 NVnuUnQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwMEOwO|ch|ryP MVTTRW5ITVJ?
SK-LU-1 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfmZY5XUUN3ME2wMlA{ODh{IN88US=> M{POWnNCVkeHUh?=
H4 NYT4O25uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvhNpNjUUN3ME2wMlA{ODlizszN NVPKOJByW0GQR1XS
HT-144 NH31UZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlraTWM2OD1yLkCzNFk{KM7:TR?= NHT5cFFUSU6JRWK=
SK-UT-1 MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUm3O|hWUUN3ME2wMlA{OTd6IN88US=> NULCR4hjW0GQR1XS
D-336MG NEn1PXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u1VWlEPTB;MD6wN|MxQSEQvF2= M1zCPHNCVkeHUh?=
MDA-MB-175-VII Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2H6T2lEPTB;MD6wN|M2PCEQvF2= M4fmdnNCVkeHUh?=
GAMG NYO3V2NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmD2TWM2OD1yLkCzOFM2KM7:TR?= NUH0XnlxW0GQR1XS
CP50-MEL-B NHnQVXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMEO0OUDPxE1? NGq4[HdUSU6JRWK=
OVCAR-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwMEO0PEDPxE1? M2PwUnNCVkeHUh?=
SK-MES-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTBwMEO2NFYh|ryP MoHnV2FPT0WU
VM-CUB-1 M37aV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMEO2OVch|ryP M{TaOXNCVkeHUh?=
WM-115 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPjNXdpUUN3ME2wMlA{PzZ{IN88US=> M4rHNnNCVkeHUh?=
DSH1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3iwVWlEPTB;MD6wN|gxPyEQvF2= NWrCeoFTW0GQR1XS
Becker NU[4NY5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPzUYFKSzVyPUCuNFM5QDVizszN NEDGO5pUSU6JRWK=
SW962 NIPRPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXaR4htUUN3ME2wMlA{QTR3IN88US=> NF[1bI5USU6JRWK=
TYK-nu NILhfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f0dWlEPTB;MD6wN|k5PSEQvF2= NIGyU|JUSU6JRWK=
HO-1-N-1 MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMESwNlEh|ryP MUPTRW5ITVJ?
T98G MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMESxNFMh|ryP MUXTRW5ITVJ?
ACN NWPTXWY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi1O5RKSzVyPUCuNFQyPjJizszN MYDTRW5ITVJ?
SW780 Mn\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwMESyNFMh|ryP NX:3[404W0GQR1XS
Detroit562 Mn7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TNemlEPTB;MD6wOFI{QSEQvF2= MUHTRW5ITVJ?
BB49-HNC MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMESyOFMh|ryP NILQeWdUSU6JRWK=
HN NG\DWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPvTWM2OD1yLkC0NlczKM7:TR?= NGnVRWdUSU6JRWK=
H9 NH3CbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFm5d21KSzVyPUCuNFQ{PzFizszN MYnTRW5ITVJ?
VA-ES-BJ NXrWV|Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LhW2lEPTB;MD6wOFQ1PyEQvF2= NIDicmVUSU6JRWK=
MEL-JUSO NVnUS4FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGH4fYhKSzVyPUCuNFQ1PzVizszN NXTKbFVpW0GQR1XS
BT-474 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwMES1JO69VQ>? M{P4OXNCVkeHUh?=
CaR-1 NYWzW3NpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\KSFlHUUN3ME2wMlA1PTR7IN88US=> M3zqUnNCVkeHUh?=
PSN1 NXTuXWIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\oU2lEPTB;MD6wOFYxOyEQvF2= NIe2PGZUSU6JRWK=
KYSE-510 NYrMRnoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFGyfoFKSzVyPUCuNFQ3PDlizszN NF\X[Y9USU6JRWK=
KP-4 NF7Bc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMES3OVMh|ryP M2jPRXNCVkeHUh?=
KYSE-410 NHv4PXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknJTWM2OD1yLkC0O|czKM7:TR?= MnzjV2FPT0WU
G-402 M{jsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3WNFRKSzVyPUCuNFQ4QDlizszN Mo\tV2FPT0WU
DOK NHn2XnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLUXItKSzVyPUCuNFQ6ODJizszN NWnBZmVNW0GQR1XS
COR-L88 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fnW2lEPTB;MD6wOFkyOiEQvF2= NGXZSmpUSU6JRWK=
SKG-IIIa MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO3fWt5UUN3ME2wMlA1QTh4IN88US=> NXnmR|FwW0GQR1XS
AN3-CA Mn25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqzTWM2OD1yLkC1JO69VQ>? NYPadnM5W0GQR1XS
SW48 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjVNpJyUUN3ME2wMlA2ODN7IN88US=> Moj3V2FPT0WU
YKG-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLNTWM2OD1yLkC1NFcyKM7:TR?= M1XMfnNCVkeHUh?=
KYSE-150 NEfOcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwMEWyN|Uh|ryP MYnTRW5ITVJ?
HuO-3N1 M2HhbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXQN4NKSzVyPUCuNFUzOzdizszN M{HnfHNCVkeHUh?=
LB1047-RCC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTtTWM2OD1yLkC1Nlk3KM7:TR?= MoTjV2FPT0WU
NCI-H2030 NHfQdppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7rdGJKSzVyPUCuNFU1OTRizszN NVnOb21HW0GQR1XS
YH-13 NInBe4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLKb5ZKSzVyPUCuNFU4OjJizszN MUjTRW5ITVJ?
5637 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuxXWJKSzVyPUCuNFU4PCEQvF2= MmLVV2FPT0WU
LOXIMVI M4jLbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHyN3BKSzVyPUCuNFU5PzJizszN M{DU[HNCVkeHUh?=
GT3TKB MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMEW5OFIh|ryP NEHBXJVUSU6JRWK=
TCCSUP MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;wRVFKSzVyPUCuNFU6PjRizszN NX\Jb2prW0GQR1XS
EPLC-272H MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXCTWM2OD1yLkC2NlA2KM7:TR?= M4jsPHNCVkeHUh?=
LU-99A NIPoZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPBfIFKSzVyPUCuNFYzOzdizszN NVLSTllmW0GQR1XS
NCI-H1755 NYLlTIlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3uV3d{UUN3ME2wMlA3OzRzIN88US=> Mom4V2FPT0WU
KM12 NXfT[|JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInPbHhKSzVyPUCuNFY{PDhizszN Mnn2V2FPT0WU
SF295 NXy1XYtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPFUVNKSzVyPUCuNFY1PTJizszN NIXVTlhUSU6JRWK=
MZ2-MEL M2nKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LiTWlEPTB;MD6wOlU2OyEQvF2= NYP6WlNoW0GQR1XS
HEC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLr[G1KSzVyPUCuNFY2QDhizszN Mk\OV2FPT0WU
SW684 NIPLNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTlTWM2OD1yLkC2OVkyKM7:TR?= MX;TRW5ITVJ?
SF539 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLKOodwUUN3ME2wMlA3PjhzIN88US=> M2G1OXNCVkeHUh?=
GMS-10 NXH0TlEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD3TWM2OD1yLkC2Olk6KM7:TR?= MXnTRW5ITVJ?
MV-4-11 M3\sOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XESGlEPTB;MD6wOlgxOyEQvF2= NV;oTZNXW0GQR1XS
HT-29 MmizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{eyXWlEPTB;MD6wOlkyQSEQvF2= NYXQZ3hZW0GQR1XS
23132-87 Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHZTXRKSzVyPUCuNFY6PSEQvF2= MmnzV2FPT0WU
SW620 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLKNYhpUUN3ME2wMlA4ODJ4IN88US=> NVrudFNbW0GQR1XS
HCC1806 MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPCPYJWUUN3ME2wMlA4OTNzIN88US=> NH[zWZVUSU6JRWK=
Hs-578-T M3roWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDLUZJUUUN3ME2wMlA4OjB6IN88US=> M2XoW3NCVkeHUh?=
A2058 NXLETYg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMEeyNlgh|ryP NWnGc4tYW0GQR1XS
MEL-HO M3rLXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzxfol[UUN3ME2wMlA4OjV3IN88US=> NVz2PYpNW0GQR1XS
HCC2998 NFK1epZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXxXIdKSzVyPUCuNFc{PDdizszN NWTkVW9JW0GQR1XS
HuO9 NHjGe5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rROmlEPTB;MD6wO|U5QSEQvF2= MUjTRW5ITVJ?
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BFTC-909 MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLZb3doUUN3ME2wMlA4QTZ7IN88US=> NEmwclVUSU6JRWK=
TE-11 NIS3U5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwMEe5PVYh|ryP M3fXc3NCVkeHUh?=
TGBC1TKB NILRSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:2c2lEPTB;MD6wPFA1OyEQvF2= M125VHNCVkeHUh?=
L-363 M3\BVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojxTWM2OD1yLkC4NlA3KM7:TR?= MnnRV2FPT0WU
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MKN45 M1TzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMEiyNVkh|ryP M2fBNHNCVkeHUh?=
HT-1080 NWXENno2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\IbmlEPTB;MD6wPFQ{QSEQvF2= M1T2UnNCVkeHUh?=
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LCLC-97TM1 NFH2RYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfkOpNkUUN3ME2wMlA5PzJ6IN88US=> MX3TRW5ITVJ?
M059J MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPaRVJmUUN3ME2wMlA6ODJ5IN88US=> MYXTRW5ITVJ?
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TE-1 M{fsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jKV2lEPTB;MD6wPVIxPCEQvF2= M1HuWnNCVkeHUh?=
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LB2241-RCC NGjDd3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C3XGlEPTB;MD6xNFA2PCEQvF2= NH;6OopUSU6JRWK=
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NCI-H1581 NX\WRYo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvabZdzUUN3ME2wMlExOjlizszN NV\jcmptW0GQR1XS
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BB65-RCC NHTyXWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSxWm8yUUN3ME2wMlExPTV2IN88US=> M33FenNCVkeHUh?=
NKM-1 NHrOS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLSTWM2OD1yLkGwOlY3KM7:TR?= NVO1OIk{W0GQR1XS
HD-MY-Z MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nCNWlEPTB;MD6xNFg4OyEQvF2= NFXPfWdUSU6JRWK=
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COLO-679 NEjwfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHRe5JKSzVyPUCuNVEzOTFizszN MVLTRW5ITVJ?
TE-8 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnRPWlKSzVyPUCuNVEzPjRizszN NH;0WpRUSU6JRWK=
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NCI-H28 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPYTWM2OD1yLkGxPFE4KM7:TR?= NW\y[5h4W0GQR1XS
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COLO-829 NGSycJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi4WpRtUUN3ME2wMlEzODB3IN88US=> MUfTRW5ITVJ?
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SW1990 M2fQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O5eWlEPTB;MD6xNlE2PyEQvF2= NX\KcZRwW0GQR1XS
NCI-H1437 NVrDfWFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MortTWM2OD1yLkGyNVU4KM7:TR?= Mn7RV2FPT0WU
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NCI-H1666 M2PMO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL4N5EzUUN3ME2wMlEzPzd2IN88US=> MWrTRW5ITVJ?
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CAMA-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7YcFRnUUN3ME2wMlEzQTJ2IN88US=> MV;TRW5ITVJ?
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NCI-H292 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwMUOxNUDPxE1? NGjIWGJUSU6JRWK=
PC-14 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\YTWM2OD1yLkGzNlEyKM7:TR?= NHi4O|RUSU6JRWK=
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HT-1376 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\HbnhGUUN3ME2wMlE3QTN4IN88US=> MVjTRW5ITVJ?
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MFM-223 NGrmO2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[2emlEPTB;MD6yOlM3OyEQvF2= M2PJc3NCVkeHUh?=
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NCI-H1355 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7ZTWM2OD1yLkK4NFc1KM7:TR?= NHTLfVJUSU6JRWK=
NCI-H1048 NX:2fGg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfpTWM2OD1yLkK4PVU3KM7:TR?= NF24[3ZUSU6JRWK=
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SW1710 NYLwbVRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHqbmR[UUN3ME2wMlI6PDl2IN88US=> NVTU[45sW0GQR1XS
KY821 M3LPT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwMkm4O|Ih|ryP NH3TcGZUSU6JRWK=
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ES8 MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTFR5ZKSzVyPUCuN|A4QDRizszN NVHheXlPW0GQR1XS
COLO-792 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjNZmRuUUN3ME2wMlMyOjVzIN88US=> NY\4co46W0GQR1XS
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ChaGo-K-1 MmDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj1V5dKSzVyPUCuN|E4OTVizszN MWrTRW5ITVJ?
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SJSA-1 M2qx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\vbWlEPTB;MD6zNVg1PyEQvF2= MVPTRW5ITVJ?
KNS-62 Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TodWlEPTB;MD6zNlA5QCEQvF2= M3q4ZnNCVkeHUh?=
CAKI-1 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrLcoZQUUN3ME2wMlMzOTFzIN88US=> NHzm[m5USU6JRWK=
UACC-62 NXjzeWR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGxTWM2OD1yLkOyNlI4KM7:TR?= NVLmbYw{W0GQR1XS
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CTB-1 M4nqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O5[WlEPTB;MD6zNlc2OyEQvF2= M2HKVnNCVkeHUh?=
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T-24 MofGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHMXmVKSzVyPUCuN|MyPTlizszN MXHTRW5ITVJ?
KYSE-70 Mkj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzL[YJxUUN3ME2wMlM{Ojh|IN88US=> MoPjV2FPT0WU
SW626 NInwVJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwM{O1N|Ih|ryP NGjPbYlUSU6JRWK=
LB996-RCC M{GyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTBwM{O2NVkh|ryP MkTGV2FPT0WU
DMS-273 M1K2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nKUGlEPTB;MD6zN|kyPiEQvF2= MoPpV2FPT0WU
SW1783 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLGTWM2OD1yLkOzPVk4KM7:TR?= MoDVV2FPT0WU
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HSC-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPZNJhKSzVyPUCuN|QxPTNizszN M{nLbXNCVkeHUh?=
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COLO-684 NFq0[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jzdWlEPTB;MD6zOFUxOSEQvF2= NYDzZ|dZW0GQR1XS
NCI-H2405 NITsd3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwM{S2N|Eh|ryP NGrX[odUSU6JRWK=
NCI-H2228 M3zOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP4TpdKSzVyPUCuN|U{PTdizszN M2fpUXNCVkeHUh?=
NB13 M1Puemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwM{[4Nlkh|ryP NEX6R|NUSU6JRWK=
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DK-MG MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwM{exPFgh|ryP NVTIRlFCW0GQR1XS
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CFPAC-1 MoTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGqwWYNKSzVyPUCuN|c2OThizszN MVLTRW5ITVJ?
KARPAS-45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli2TWM2OD1yLkO3PFYzKM7:TR?= MlrCV2FPT0WU
NCI-H1793 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVi4NZVWUUN3ME2wMlM5PTFizszN NH;xWXFUSU6JRWK=
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EW-18 NGfhOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwM{i5OFEh|ryP M{DTWnNCVkeHUh?=
RO82-W-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnKTWM2OD1yLkO5Olk6KM7:TR?= M3TtRnNCVkeHUh?=
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PANC-10-05 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwNEGxO{DPxE1? NUP3OmljW0GQR1XS
NCI-H1703 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwNEG0OFYh|ryP MlXLV2FPT0WU
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LN-405 M2Hjbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjIbVNKSzVyPUCuOFE3QDdizszN MY\TRW5ITVJ?
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CAL-12T MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTte3F4UUN3ME2wMlQzPzhizszN MnjxV2FPT0WU
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GOTO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwNEWxOkDPxE1? NX25dpZ2W0GQR1XS
C3A MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW2WIxiUUN3ME2wMlQ2PDN5IN88US=> MYjTRW5ITVJ?
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NCI-H1573 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjn[|NZUUN3ME2wMlQ2PTZ7IN88US=> NFTGc|FUSU6JRWK=
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A101D MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LRU2lEPTB;MD60PFA2OyEQvF2= MoCxV2FPT0WU
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MSTO-211H MnzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3hPGxqUUN3ME2wMlU2PzZ{IN88US=> NIi3[IVUSU6JRWK=
NCI-H2126 M3WzSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK4XXNKSzVyPUCuOVY5OTVizszN M4D3WHNCVkeHUh?=
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NCI-H661 NHPhXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULYfFR5UUN3ME2wMlYyOTB2IN88US=> Mon6V2FPT0WU
UACC-893 NI[wfmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\BblhKSzVyPUCuOlM3QDFizszN Moi4V2FPT0WU
JVM-3 NY\4TYQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnwS2ppUUN3ME2wMlY{QDB2IN88US=> NYXDOZltW0GQR1XS
SF268 NXvXdXVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPab2N4UUN3ME2wMlY1OzR7IN88US=> MUHTRW5ITVJ?
OCI-AML2 MkjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fDTGlEPTB;MD62OVM6PyEQvF2= NILDUnlUSU6JRWK=
RPMI-8226 NFTu[|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHaTWM2OD1yLk[2N|I{KM7:TR?= M3XvOXNCVkeHUh?=
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MDA-MB-453 NVXLUIVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HzRmlEPTB;MD62O|E5KM7:TR?= MnW4V2FPT0WU
BV-173 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNki2O|kh|ryP NXi4Um51W0GQR1XS
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MEG-01 NXK3cYdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTxTWM2OD1zND6zO|A5KM7:TR?= MnfPV2FPT0WU
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RPMI-8866 M4fBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XXPGlEPTB;MU[uPFQ6PiEQvF2= MVLTRW5ITVJ?
NCI-H630 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nZOWlEPTB;MU[uPFU{PyEQvF2= M2Kw[XNCVkeHUh?=
KYSE-140 NV73coxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTwTWM2OD1zNz6yNFI5KM7:TR?= M3TIcXNCVkeHUh?=
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Calu-6 MkjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF7LkS5NkDPxE1? MW\TRW5ITVJ?
EGI-1 NXS3XG46T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF7LkW5PEDPxE1? MYHTRW5ITVJ?
MFH-ino M4PIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF7Lke0OVQh|ryP MUTTRW5ITVJ?
GB-1 NH7nU5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvNTWM2OD1{MD6zOVM2KM7:TR?= NH7T[5FUSU6JRWK=
NCI-H1693 M4jkWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3uTIJKSzVyPUKwMlY2ODVizszN NHHTfmxUSU6JRWK=
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H-EMC-SS Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\WTWM2OD1{Mj6wOFUh|ryP MYPTRW5ITVJ?
D-502MG NG\hcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XKOGlEPTB;MkKuPFI3OSEQvF2= M3TjVHNCVkeHUh?=
IA-LM NUPORYZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7tTWM2OD1{Mz6yOFk{KM7:TR?= NHXvOmZUSU6JRWK=
SW1463 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjSfmxKSzVyPUKzMlc6KM7:TR?= M3ruWnNCVkeHUh?=
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LCLC-103H M3\pVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HIOGlEPTB;MkSuPFQ1QSEQvF2= NHTmSFFUSU6JRWK=
SNU-449 NETrbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ2Lki3OFEh|ryP NVjUWYdUW0GQR1XS
KE-37 NE\OZ4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ3LkC5Nlgh|ryP NHTSdY1USU6JRWK=
NCI-H1623 NVXmd2x1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3HTWM2OD1{Nz6xN|A{KM7:TR?= M17nV3NCVkeHUh?=
MOLT-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i1O2lEPTB;MkeuN|UyPiEQvF2= MW\TRW5ITVJ?
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NB6 NIjjdoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2noN2lEPTB;M{KuNlg4PiEQvF2= NUHHTYR3W0GQR1XS
MOLT-16 MmDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;2ToFKSzVyPUOzMlAxPTVizszN NFj1V4dUSU6JRWK=
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A4-Fuk MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnudphjUUN3ME2zOU4xPjZizszN MVPTRW5ITVJ?
CAL-85-1 NIX6WWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXp[IRKSzVyPUO1MlI5OTdizszN M1\OcXNCVkeHUh?=
CCRF-CEM MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTzTWM2OD1|Nz6xOVM3KM7:TR?= MUTTRW5ITVJ?
HAL-01 NHv0fmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTMSHFKSzVyPUO4MlQ5QDlizszN NX\V[4dWW0GQR1XS
HEL NHX5WoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTYcJRWUUN3ME20N{4{PDB7IN88US=> MoDPV2FPT0WU
EW-1 NU\EWJd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DMUWlEPTB;NEOuOFc3QCEQvF2= M4POTHNCVkeHUh?=
MDA-MB-231 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn0Vo45UUN3ME20OU4yOTl7IN88US=> M3PB[nNCVkeHUh?=
ABC-1 MlHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTR4Lki1N|gh|ryP M3naNXNCVkeHUh?=
NCI-H446 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PJXGlEPTB;NEiuOVA2QCEQvF2= NXjXcncyW0GQR1XS
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DOHH-2 NX3iO3U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPoO3BJUUN3ME20PU43PjV4IN88US=> M4P2UXNCVkeHUh?=
GCT NUjhdGlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDBUIx6UUN3ME20PU43QTd4IN88US=> M1\jN3NCVkeHUh?=

... 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:
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
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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID