17-AAG (Tanespimycin) 化学構造
分子量: 585.69

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Quality Control & MSDS

製品説明

  • Compare HSP (e.g. HSP90) Inhibitors
    HSP (e.g. HSP90)製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 17-AAG (Tanespimycin)は、5nMのIC50による強力な熱ショックタンパク質90(Hsp90)阻害剤です。
ターゲット HSP90
IC50 5 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A549 NGLQZmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMECwN|A{KM7:TR?= NX76V4ZyW0GQR1XS
IST-MEL1 Moj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL5TZlHUUN3ME2wMlAxODRyNzFOwG0> M{HTbXNCVkeHUh?=
NCI-SNU-1 M2DHemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMECyNFch|ryP NVHJU4tZW0GQR1XS
FADU NUnhVlI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwMECyNFkh|ryP MoPrV2FPT0WU
C32 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwMECzNFQh|ryP NEXjbZdUSU6JRWK=
D-566MG NVXYNXFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrGN3hKSzVyPUCuNFA{QSEQvF2= NGf1epdUSU6JRWK=
LXF-289 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[2WmlEPTB;MD6wNFQyQSEQvF2= NH;KcGFUSU6JRWK=
HGC-27 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjKUmFKSzVyPUCuNFA2OSEQvF2= NH7GOIFUSU6JRWK=
RPMI-7951 M4DqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwMEC3NVch|ryP NIP6WodUSU6JRWK=
HSC-3 NXPG[JhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwMEC5Nlkh|ryP NIHHOW5USU6JRWK=
MIA-PaCa-2 MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TIemlEPTB;MD6wNVAxQSEQvF2= NIfTVIRUSU6JRWK=
KS-1 NXPBPY8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwMEGzOVUh|ryP NUCzTmQ2W0GQR1XS
CAL-51 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ntVmlEPTB;MD6wNVQxPSEQvF2= MUDTRW5ITVJ?
MDA-MB-361 NGHzVlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnXcGV{UUN3ME2wMlAyPDl3IN88US=> NFLs[nVUSU6JRWK=
TI-73 NYjSdWgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\DXFhKSzVyPUCuNFE4QTZizszN NHflfYtUSU6JRWK=
AGS MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMEG5N|gh|ryP NEjmUWNUSU6JRWK=
NCI-H460 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMEG5O|Qh|ryP MWHTRW5ITVJ?
A204 NUPBc5hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwMEKyOFkh|ryP MonmV2FPT0WU
CHL-1 NUG3cYtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;teodMUUN3ME2wMlAzOjVzIN88US=> M1\Fe3NCVkeHUh?=
DU-4475 M4PFNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fNdmlEPTB;MD6wNlI3OSEQvF2= Ml3oV2FPT0WU
CGTH-W-1 MmnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXteWxKSzVyPUCuNFI{PDlizszN MVzTRW5ITVJ?
HCC2218 NULGOZV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjMT4dKSzVyPUCuNFI1QTRizszN M4XKcHNCVkeHUh?=
A2780 M2XwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMEK1N|Eh|ryP NVPNc4RTW0GQR1XS
NCI-H720 NUToeoF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnvTWM2OD1yLkCyOVQ3KM7:TR?= M1PXOnNCVkeHUh?=
NCI-N87 M1nXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwMEK1PVMh|ryP MX;TRW5ITVJ?
CHP-212 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMEK2Nlgh|ryP M2rpWXNCVkeHUh?=
NCI-H23 M1GzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r0SWlEPTB;MD6wNlY3PSEQvF2= M17TdHNCVkeHUh?=
D-263MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3sW3pKSzVyPUCuNFI4QDZizszN M1ToRXNCVkeHUh?=
ME-180 NYrWZXlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfFboY1UUN3ME2wMlAzQDlzIN88US=> MVXTRW5ITVJ?
SW982 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7OVFhKSzVyPUCuNFI6QTlizszN MnPYV2FPT0WU
OE19 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe2[4FRUUN3ME2wMlA{ODd5IN88US=> MmTNV2FPT0WU
SK-LU-1 Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ftb2lEPTB;MD6wN|A5OiEQvF2= MmPOV2FPT0WU
H4 MmDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHQPIlKSzVyPUCuNFMxQSEQvF2= M2XPc3NCVkeHUh?=
HT-144 Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfiV2VKSzVyPUCuNFMxQTNizszN NXG2UWxEW0GQR1XS
SK-UT-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPWVG1KSzVyPUCuNFMyPzhizszN MXzTRW5ITVJ?
D-336MG NWTBboFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TDW2lEPTB;MD6wN|MxQSEQvF2= M1nhUnNCVkeHUh?=
MDA-MB-175-VII NI\tT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1flNWlEPTB;MD6wN|M2PCEQvF2= MoX0V2FPT0WU
GAMG NEDtW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIWzPVNKSzVyPUCuNFM1OzVizszN MlXQV2FPT0WU
CP50-MEL-B NHToUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojLTWM2OD1yLkCzOFUh|ryP MXPTRW5ITVJ?
OVCAR-5 NXPNN3pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnlPJczUUN3ME2wMlA{PDhizszN NVHQWYR3W0GQR1XS
SK-MES-1 NX7yUmRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DUPWlEPTB;MD6wN|YxPiEQvF2= NH7uZ3BUSU6JRWK=
VM-CUB-1 NYrQOVJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XrS2lEPTB;MD6wN|Y2PyEQvF2= M13j[3NCVkeHUh?=
WM-115 NHX4T4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H1bWlEPTB;MD6wN|c3OiEQvF2= MWLTRW5ITVJ?
DSH1 Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XNWmlEPTB;MD6wN|gxPyEQvF2= NEPQWZVUSU6JRWK=
Becker MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jtOmlEPTB;MD6wN|g5PSEQvF2= NU\I[YF5W0GQR1XS
SW962 NVHVVGJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3z[WVpUUN3ME2wMlA{QTR3IN88US=> M3n3T3NCVkeHUh?=
TYK-nu M1rVVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnFTWM2OD1yLkCzPVg2KM7:TR?= NEXMc2tUSU6JRWK=
HO-1-N-1 NIHWfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr3eXNKSzVyPUCuNFQxOjFizszN NVr3dXluW0GQR1XS
T98G NHP5WHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwMESxNFMh|ryP NXruR41mW0GQR1XS
ACN M4PqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnvbVV6UUN3ME2wMlA1OTZ{IN88US=> MoLoV2FPT0WU
SW780 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fzc2lEPTB;MD6wOFIxOyEQvF2= MmHFV2FPT0WU
Detroit562 NYjPWXJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzTTWM2OD1yLkC0NlM6KM7:TR?= M3mxeXNCVkeHUh?=
BB49-HNC M{G0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\sUIV{UUN3ME2wMlA1OjR|IN88US=> NVnQdXIyW0GQR1XS
HN MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TWb2lEPTB;MD6wOFI4OiEQvF2= MljIV2FPT0WU
H9 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnL1TWM2OD1yLkC0N|cyKM7:TR?= M1nTNXNCVkeHUh?=
VA-ES-BJ M3TkbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mny0TWM2OD1yLkC0OFQ4KM7:TR?= M3XxVXNCVkeHUh?=
MEL-JUSO MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjadJZQUUN3ME2wMlA1PDd3IN88US=> M3vvU3NCVkeHUh?=
BT-474 NWr1VVdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwMES1JO69VQ>? MWDTRW5ITVJ?
CaR-1 NX;QPIZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnRPFRKSzVyPUCuNFQ2PDlizszN MUDTRW5ITVJ?
PSN1 M{LocGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LNdWlEPTB;MD6wOFYxOyEQvF2= NYT0OXV{W0GQR1XS
KYSE-510 MkG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMES2OFkh|ryP NXey[|VQW0GQR1XS
KP-4 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;LTWM2OD1yLkC0O|U{KM7:TR?= MXnTRW5ITVJ?
KYSE-410 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK5TWM2OD1yLkC0O|czKM7:TR?= NETUNYlUSU6JRWK=
G-402 NUTFbG1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwMES3PFkh|ryP M4rzc3NCVkeHUh?=
DOK NXLJPYJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwMES5NFIh|ryP M1HuOXNCVkeHUh?=
COR-L88 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPPc2VKSzVyPUCuNFQ6OTJizszN MXzTRW5ITVJ?
SKG-IIIa NUn2WWw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz1TJdKSzVyPUCuNFQ6QDZizszN MY\TRW5ITVJ?
AN3-CA MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rncGlEPTB;MD6wOUDPxE1? NF\0NXBUSU6JRWK=
SW48 M2f2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnBZ4FKSzVyPUCuNFUxOzlizszN NGPIe5pUSU6JRWK=
YKG-1 NFuzUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuyTWM2OD1yLkC1NFcyKM7:TR?= Ml7HV2FPT0WU
KYSE-150 M4f4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHvfHNKSzVyPUCuNFUzOzVizszN M1TQe3NCVkeHUh?=
HuO-3N1 M4\RSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfpbGZKSzVyPUCuNFUzOzdizszN MYHTRW5ITVJ?
LB1047-RCC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\4WpBKSzVyPUCuNFUzQTZizszN MV;TRW5ITVJ?
NCI-H2030 NGGxZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMEW0NVQh|ryP M1PDcnNCVkeHUh?=
YH-13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnGeHlKSzVyPUCuNFU4OjJizszN M4fRfHNCVkeHUh?=
5637 Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;NNWlEPTB;MD6wOVc1KM7:TR?= NEC1VldUSU6JRWK=
LOXIMVI NEXFeW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfUXIJKSzVyPUCuNFU5PzJizszN M4m5eXNCVkeHUh?=
GT3TKB NHzTNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwMEW5OFIh|ryP NY\P[Zc2W0GQR1XS
TCCSUP MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvwcHJKSzVyPUCuNFU6PjRizszN NHrGO3VUSU6JRWK=
EPLC-272H MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq0dYhKSzVyPUCuNFYzODVizszN NW\rNpVzW0GQR1XS
LU-99A MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwME[yN|ch|ryP M1;Cc3NCVkeHUh?=
NCI-H1755 NWH2fnFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGyTWM2OD1yLkC2N|QyKM7:TR?= MXHTRW5ITVJ?
KM12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwME[zOFgh|ryP NHHOTm1USU6JRWK=
SF295 MlnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TLZ2lEPTB;MD6wOlQ2OiEQvF2= MXjTRW5ITVJ?
MZ2-MEL M2\vT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzBTWM2OD1yLkC2OVU{KM7:TR?= NET2[VhUSU6JRWK=
HEC-1 NWDaN4pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwME[1PFgh|ryP Mmi0V2FPT0WU
SW684 M4XhNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml76TWM2OD1yLkC2OVkyKM7:TR?= NIDJSIxUSU6JRWK=
SF539 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TzVWlEPTB;MD6wOlY5OSEQvF2= NETtWHZUSU6JRWK=
GMS-10 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;EfWlEPTB;MD6wOlY6QSEQvF2= NGjzRXpUSU6JRWK=
MV-4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwME[4NFMh|ryP NGHs[FRUSU6JRWK=
HT-29 NEDKUY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwME[5NVkh|ryP M4HVRXNCVkeHUh?=
23132-87 NIXT[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnkbm9KSzVyPUCuNFY6PSEQvF2= M2rVS3NCVkeHUh?=
SW620 NIrKfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMEewNlYh|ryP M4nWSHNCVkeHUh?=
HCC1806 NUfhRVRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTV[GJzUUN3ME2wMlA4OTNzIN88US=> NXf0SZpxW0GQR1XS
Hs-578-T MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrm[2pbUUN3ME2wMlA4OjB6IN88US=> NEjuXmFUSU6JRWK=
A2058 NVPvOHFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMEeyNlgh|ryP M4X0XXNCVkeHUh?=
MEL-HO MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfNfG5iUUN3ME2wMlA4OjV3IN88US=> NGrKXZVUSU6JRWK=
HCC2998 M3nocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLwTWM2OD1yLkC3N|Q4KM7:TR?= MmLXV2FPT0WU
HuO9 M4TwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHT[ndKSzVyPUCuNFc2QDlizszN Mo\YV2FPT0WU
CAL-39 M3rPSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMEe3OlYh|ryP M3jV[HNCVkeHUh?=
M14 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwMEe5NVMh|ryP MojGV2FPT0WU
BFTC-909 M3rhb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vMXWlEPTB;MD6wO|k3QSEQvF2= NV\MWVlJW0GQR1XS
TE-11 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XCVmlEPTB;MD6wO|k6PiEQvF2= NX35XIN3W0GQR1XS
TGBC1TKB MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;yTWM2OD1yLkC4NFQ{KM7:TR?= NFfWbItUSU6JRWK=
L-363 MlvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwMEiyNFYh|ryP MlHFV2FPT0WU
A431 M2K1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjGSpFrUUN3ME2wMlA5OjFizszN Mnj1V2FPT0WU
MKN45 NGXhO4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwMEiyNVkh|ryP NXHxbGJQW0GQR1XS
HT-1080 M{jUVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwMEi0N|kh|ryP NYixVGZpW0GQR1XS
OVCAR-8 M1mz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\wZWFJUUN3ME2wMlA5PjJ{IN88US=> MnTZV2FPT0WU
LCLC-97TM1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPwVWFKSzVyPUCuNFg4OjhizszN MlXRV2FPT0WU
M059J MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C5WmlEPTB;MD6wPVAzPyEQvF2= M1y0eXNCVkeHUh?=
SK-MEL-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37xfmlEPTB;MD6wPVA3KM7:TR?= M3;DOXNCVkeHUh?=
TE-1 NYm4WIZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwMEmyNFQh|ryP M2nZcHNCVkeHUh?=
KYSE-180 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7D[Jd6UUN3ME2wMlA6OjZ{IN88US=> NWLE[ndHW0GQR1XS
D-247MG M2\5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwMEm0OVUh|ryP MYfTRW5ITVJ?
8-MG-BA NWrnb5hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMEm0O|Ih|ryP NV\KVZpHW0GQR1XS
NCI-H1792 NEnGcGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPERY91UUN3ME2wMlA6PjF6IN88US=> NXrJSJB1W0GQR1XS
MCF7 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFqwUY1KSzVyPUCuNFk3PzdizszN MYfTRW5ITVJ?
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P12-ICHIKAWA MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO4UXhKSzVyPUeuOFU2OjNizszN NEK3e3BUSU6JRWK=
NCI-H82 NGTudpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTdwNEW3NFEh|ryP NX6wN2xVW0GQR1XS
NCI-H1993 M{LW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTdwOEOwOlMh|ryP M3z4NXNCVkeHUh?=
RH-1 M4rGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jzSGlEPTB;Nz64OVI1PCEQvF2= MXXTRW5ITVJ?
SW948 M3yzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoWzTWM2OD15Lkm2NFQ6KM7:TR?= NFW2eFVUSU6JRWK=
CAL-33 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTdwOUm5N|gh|ryP MYrTRW5ITVJ?
U-266 NYnZUXNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1z0U2lEPTB;OD6xOVc4PyEQvF2= M4TPZXNCVkeHUh?=
CAL-72 MnfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInPbndKSzVyPUiuNlA{OiEQvF2= M1vjRXNCVkeHUh?=
SNU-423 NF3oSIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\tTWlEPTB;OT6zOlY3PiEQvF2= MXPTRW5ITVJ?
KG-1 M3HEOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK5ZWQ6UUN3ME25MlU5PDV4IN88US=> MUnTRW5ITVJ?
HCC1395 M2OxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTlwOUKzOVIh|ryP NYm2bHVOW0GQR1XS
BE-13 M4i3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT0TWM2OD1zMD64PFkzKM7:TR?= MmnPV2FPT0WU
MKN7 NYnuRWZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFyLkm3OlUh|ryP MVXTRW5ITVJ?
697 NYH0SoEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTtc2pyUUN3ME2xNU4yPDd{IN88US=> M4\McXNCVkeHUh?=
LU-135 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HHR2lEPTB;MUGuNlMxPyEQvF2= MWXTRW5ITVJ?
ES7 M1GxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfHWFFKSzVyPUGxMlM{OTNizszN MkDmV2FPT0WU
SK-HEP-1 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILGNWRKSzVyPUGxMlc3PDZizszN M2P4c3NCVkeHUh?=
BEN M1vnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m5bWlEPTB;MUGuPFUyKM7:TR?= MVvTRW5ITVJ?
NCI-H1770 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTHVllmUUN3ME2xNk4yOjZizszN M3;iTHNCVkeHUh?=
SW13 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7P[3lCUUN3ME2xNk4yPTRzIN88US=> NX;0S|BLW0GQR1XS
MZ1-PC NUeyepFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXX[FJKSzVyPUGyMlU1PTJizszN MmPVV2FPT0WU
Mo-T MlnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofJTWM2OD1zMj63OFIyKM7:TR?= MVrTRW5ITVJ?
HLE NULkcG84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnSRpRKSzVyPUGyMlgzOTVizszN NILGW5lUSU6JRWK=
RCC10RGB NFHOcXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVKxU2c4UUN3ME2xN{43PzFizszN MWjTRW5ITVJ?
COLO-320-HSR NV\rUpdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\DRoxpUUN3ME2xN{44OzhzIN88US=> M13V[nNCVkeHUh?=
BHT-101 M4DFVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj6VFhWUUN3ME2xN{45OzR3IN88US=> MX3TRW5ITVJ?
OCUB-M MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHSU|dKSzVyPUG0MlE3ODJizszN MXTTRW5ITVJ?
MEG-01 NFHyUoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;sPGlEPTB;MUSuN|cxQCEQvF2= MmL5V2FPT0WU
RS4-11 NGm4RZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF2Lke0NkDPxE1? NGGwR5VUSU6JRWK=
MN-60 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrPTWM2OD1zND63PFk1KM7:TR?= M2\obHNCVkeHUh?=
NCI-H1304 NYPvbIF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnoTWM2OD1zNT6wOFI2KM7:TR?= NU\JVnF6W0GQR1XS
Ramos-2G6-4C10 M33xVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF3LkC1PFEh|ryP M3vTeXNCVkeHUh?=
NCI-H2342 Mn\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PyRWlEPTB;MUWuNlA1PCEQvF2= MYjTRW5ITVJ?
LAN-6 NITPbodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF3LkS0NVQh|ryP NHH3TIdUSU6JRWK=
JVM-2 NXeycoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEOxWo5KSzVyPUG1MlU4PDhizszN NFvjc2xUSU6JRWK=
P30-OHK NVHUbFNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3mz[2lEPTB;MU[uNFYyPCEQvF2= MX7TRW5ITVJ?
C-33-A Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXmOHpKSzVyPUG2MlYzOTRizszN NGS4bWlUSU6JRWK=
RPMI-8866 NIjSZZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zpZ2lEPTB;MU[uPFQ6PiEQvF2= MmLPV2FPT0WU
NCI-H630 NXr2XHhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\4dodKSzVyPUG2Mlg2OzdizszN NIHZ[WxUSU6JRWK=
KYSE-140 NWrMWFBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzKNJNKSzVyPUG3MlIxOjhizszN M4PVR3NCVkeHUh?=
T84 NEmxTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXWbGlYUUN3ME2xPE45Pjl3IN88US=> MYHTRW5ITVJ?
KU-19-19 M1PDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO5TWM2OD1zOD65OlA5KM7:TR?= M1vYUHNCVkeHUh?=
BALL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3ETWM2OD1zOT6zN|k6KM7:TR?= MW\TRW5ITVJ?
Calu-6 NGXTcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfpTWM2OD1zOT60PVIh|ryP NFLZOW1USU6JRWK=
EGI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF7LkW5PEDPxE1? NEPhbJhUSU6JRWK=
MFH-ino Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF7Lke0OVQh|ryP NYHmS2FMW0GQR1XS
GB-1 NGXP[JRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfMTW03UUN3ME2yNE4{PTN3IN88US=> NUfNd|dSW0GQR1XS
NCI-H1693 MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTFTWM2OD1{MD62OVA2KM7:TR?= M1naVnNCVkeHUh?=
SW1116 NFfxbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\UUJpkUUN3ME2yNE46OzZ{IN88US=> MmrYV2FPT0WU
H-EMC-SS MkjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS3R4hKSzVyPUKyMlA1PSEQvF2= Mm\uV2FPT0WU
D-502MG M{fVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTRbllDUUN3ME2yNk45OjZzIN88US=> NF;PdmpUSU6JRWK=
IA-LM MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGzbJJKSzVyPUKzMlI1QTNizszN Mn3EV2FPT0WU
SW1463 M3;TT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfKepY1UUN3ME2yN{44QSEQvF2= NH;4VoRUSU6JRWK=
JAR MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJ2LkOyPVMh|ryP MnGxV2FPT0WU
HT NV3VSVlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv2TGNkUUN3ME2yOE41PzV|IN88US=> NFm4TFdUSU6JRWK=
LCLC-103H NXPRPJdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ2Lki0OFkh|ryP MULTRW5ITVJ?
SNU-449 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF25VZpKSzVyPUK0Mlg4PDFizszN M{LYTHNCVkeHUh?=
KE-37 NX\nXVJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXqTWM2OD1{NT6wPVI5KM7:TR?= NFezbGNUSU6JRWK=
NCI-H1623 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;yTWM2OD1{Nz6xN|A{KM7:TR?= MnTCV2FPT0WU
MOLT-13 NWXpWmNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJ5LkO1NVYh|ryP MVjTRW5ITVJ?
COLO-741 NEXwWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvuRnFjUUN3ME2zNU4{OzN|IN88US=> NHXKVlNUSU6JRWK=
NB6 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLtXZpKSzVyPUOyMlI5PzZizszN MnzvV2FPT0WU
MOLT-16 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LGXWlEPTB;M{OuNFA2PSEQvF2= MVHTRW5ITVJ?
IST-MES1 NYnPOHdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjXTWM2OD1|ND6wOVQyKM7:TR?= NUC3ZpNKW0GQR1XS
A4-Fuk MnLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\0[VVSUUN3ME2zOU4xPjZizszN NXG1[oxqW0GQR1XS
CAL-85-1 NYW1V|RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN3LkK4NVch|ryP MYHTRW5ITVJ?
CCRF-CEM NX;YbodUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ezfGlEPTB;M{euNVU{PiEQvF2= NXy3enYyW0GQR1XS
HAL-01 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrZRoVKSzVyPUO4MlQ5QDlizszN MVnTRW5ITVJ?
HEL NIPndYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrWXVFKSzVyPUSzMlM1ODlizszN NXH4Tm97W0GQR1XS
EW-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TVRmlEPTB;NEOuOFc3QCEQvF2= MV3TRW5ITVJ?
MDA-MB-231 NETnWFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvxSItCUUN3ME20OU4yOTl7IN88US=> NXzNTFlSW0GQR1XS
ABC-1 MmHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmftTWM2OD12Nj64OVM5KM7:TR?= M330VHNCVkeHUh?=
NCI-H446 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDqVIRKSzVyPUS4MlUxPThizszN NHvUV41USU6JRWK=
MHH-PREB-1 M1S4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;CcZBKSzVyPUS5MlYxODdizszN MnXiV2FPT0WU
DOHH-2 NGjxU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e4[WlEPTB;NEmuOlY2PiEQvF2= MmjNV2FPT0WU
GCT NELucI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\pTWM2OD12OT62PVc3KM7:TR?= M2fOOXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase II study of 17-AAG in patients with relapsed/refractory CD30 plus anaplastic large cell lymphoma (ALCL) relapsed/refractory mantle cell lymphoma (MCL) and relapsed/refractory classical Hodgkin's lymphoma (HL) has been completed.
特集 Displays very low toxicity toward normal cells.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞株 BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 5 days
実験の流れ 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.

動物実験: [2]

動物モデル 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
製剤 Dissolved in DMSO, and diluted in egg phospholipids (EPL) vehicle
投薬量 ~50 mg/kg
投与方法 Injection i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download 17-AAG (Tanespimycin) SDF
分子量 585.69
化学式

C31H43N3O8

CAS No. 75747-14-7
保管 2年-20℃
6月-80℃in solvent
別名 CP127374,NSC-330507, KOS 953
溶解度 (25°C) * In vitro DMSO 100 mg/mL (170.73 mM)
エタノール 5 mg/mL (8.53 mM)
<1 mg/mL (<1 mM)
In vivo
* <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.
化学名 17-demethoxy-17-(2-propenylamino)- [(3R,5R,6S,7R,8E,10R,11R,12Z,14E)-6-Hydroxy-5,11,21-trimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate

カスタマーフィードバック (7)


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Rating
Source , , PNAS, 2011, 108: 7535-40. 17-AAG (Tanespimycin) purchased from Selleck
Method Western Blot
Cell Lines H3122 & H3122 CR cells
Concentrations 10 nM
Incubation Time 72 h
Results As shown in Fig. A, 17-AAG potently suppressed cell growth in both parental H3122 and H3122 CR cells. However, in contrast to NVP-TAE684 and AP26113, 17-AAG also inhibited the viability of SKBR3 and BT474 cell lines. 17-AAG treatment decreased both p-ALK 眏Ỵ眐㠞眎膉癠 皐﷘ř᐀ŔřĀ 㺣癞帉癞Ѐ瑖兽ﱔᆊࣿřĀࣾ彿兾奋兾巫兾婶ࣿ橢ࣿ彿兾

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Rating
Source Oncotarget, 2014, 5, 4269-82. 17-AAG (Tanespimycin) purchased from Selleck
Method Western blot
Cell Lines Ls-174T, HCT116, Caco2, Hke3 cells
Concentrations 0.5, 2 uM
Incubation Time 24 h
Results Colon cancer cells harboring WT or MT K-Ras were treated with 17-AAG and effects on the Ras expression were analyzed by WB. Results in Figure showed that incubation with 17-AAG only down-regulates K-Ras in K-Ras MT cells but decreases Raf-1 {an established Hsp90 client} in all cell lines. The result, for the first time, demonstrated that both transfected and endogenous MT K-Ras is an Hsp90 client protein.

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Rating
Source Oncotarget, 2015, 51: S659-S660. 17-AAG (Tanespimycin) purchased from Selleck
Method Western Blot
Cell Lines MOLT-4 & RS4;11 cells
Concentrations
Incubation Time 22 h
Results In both MOLT-4 and RS4;11 cells, the combined treatment inhibited the interactions between Hsp90 and BIP/Grp78 more effectively than CX-4945 single treatment and to the same extent as tanespimycin (17-AAG).

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Rating
Source Mol Cell Biol, 2013, 33(12), 2375-87. 17-AAG (Tanespimycin) purchased from Selleck
Method Western blot
Cell Lines NIH 3T3 cells
Concentrations 25, 50 uM
Incubation Time 4 h
Results 17-AAG and SNX-2112, both of which induce the UPR by targeting the chaperone HSP90, decreased mSmoM2 protein levels (lanes 2 to 5 compared to lane 1), further supporting the sensitivity of active Smo mutants to UPR induction.

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Rating
Source J Biol Chem, 2012, 287, 44109-20. 17-AAG (Tanespimycin) purchased from Selleck
Method Western Blot
Cell Lines Dopaminergic Neuronal Cell lines
Concentrations 10-20uM
Incubation Time
Results As expected, both complex IV activity and Hsp60 levels exhibited a dose-dependent decrease in response to treatment with 17-AAG (Fig. 4A). However, 17-AAG treatment did not alter levels of Hsp90 and LRPPRC levels

Click to enlarge
Rating
Source Mol Cancer, 2014, 13, 150. 17-AAG (Tanespimycin) purchased from Selleck
Method Western blot
Cell Lines SKBR3 cells
Concentrations 1, 2 uM
Incubation Time 24 h
Results Hsp90 and Cdc37 protein levels showed no distinct change according to a drug concentration gradient, whereas Hsp70, a marker of Hsp90 inhibition, the protein level was greatly induced by treatment with 17AAG or FW-04-806.

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Rating
Source Age, 2013, 35, 549-62. 17-AAG (Tanespimycin) purchased from Selleck
Method Western Blot
Cell Lines HFSN1 cells
Concentrations 0.1/0.5uM
Incubation Time 24 h
Results Figure 2c shows that the decrease in the level of Hsp90 after treatment with 0.5 μM of 17-AAG was accompanied by a decrease in the level of both the survivin and phospho-survivin proteins.

文献中の引用 (19)

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  • Luminespib (AUY-922, NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922)は高度的に HSP90 を抑制、 HSP90α と HSP90β を作用すると、 IC50 がそれぞれ 13 nM 、 21 nM となる。

  • Ganetespib (STA-9090)

    Ganetespib (STA-9090)は独特な triazolone-containing Hsp90阻害剤、 IC50 が4 nM となる.

  • 17-DMAG (Alvespimycin) HCl

    17-DMAG (Alvespimycin) HClは、62nMのIC50による強力なHsp90阻害剤です。

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

  • Geldanamycin

    ノーカット二量体Hsp90またはN末端領域Hsp90と結合している間、Geldanamycinは1.2のμMまたは0.78のμMによるKdによる天然既存のHsp90阻害剤です。

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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