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 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;RWVNKSzVyPUCuNFAxOzB|IN88US=> NWO2c3c5W0GQR1XS
IST-MEL1 NGD0[GVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHpU5NKSzVyPUCuNFAxPDB5IN88US=> NEHtZoRUSU6JRWK=
NCI-SNU-1 M{KxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXlTWM2OD1yLkCwNlA4KM7:TR?= MXjTRW5ITVJ?
FADU MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwMECyNFkh|ryP M{XGWnNCVkeHUh?=
C32 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr4bHFKSzVyPUCuNFA{ODRizszN MonBV2FPT0WU
D-566MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXYTWM2OD1yLkCwN|kh|ryP NVX2Umt7W0GQR1XS
LXF-289 NGrFNVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwMEC0NVkh|ryP NWKzT5M3W0GQR1XS
HGC-27 MnS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMEC1NUDPxE1? NHrseohUSU6JRWK=
RPMI-7951 MmDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlriTWM2OD1yLkCwO|E4KM7:TR?= MkjsV2FPT0WU
HSC-3 NXjRTpFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXZTWM2OD1yLkCwPVI6KM7:TR?= MYDTRW5ITVJ?
MIA-PaCa-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnz[2I3UUN3ME2wMlAyODB7IN88US=> NGe0WVNUSU6JRWK=
KS-1 M2DhPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfGV4NJUUN3ME2wMlAyOzV3IN88US=> MoHHV2FPT0WU
CAL-51 MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEG0NFUh|ryP M3f3cHNCVkeHUh?=
MDA-MB-361 NF2yOpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMEG0PVUh|ryP NEW1S5BUSU6JRWK=
TI-73 NFrsXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zQNWlEPTB;MD6wNVc6PiEQvF2= MlPIV2FPT0WU
AGS M1jITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HlNWlEPTB;MD6wNVk{QCEQvF2= MleyV2FPT0WU
NCI-H460 NYTwPWt[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwMEG5O|Qh|ryP MmnTV2FPT0WU
A204 NX;me5dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMEKyOFkh|ryP M{LuN3NCVkeHUh?=
CHL-1 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[xTWM2OD1yLkCyNlUyKM7:TR?= NYrLT29DW0GQR1XS
DU-4475 M2fwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvrNZNKSzVyPUCuNFIzPjFizszN NXfsWYNbW0GQR1XS
CGTH-W-1 Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfDN2ZsUUN3ME2wMlAzOzR7IN88US=> NULYcoE3W0GQR1XS
HCC2218 NUXLcnRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwMEK0PVQh|ryP NUjWTW1xW0GQR1XS
A2780 MonES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnlZ4dvUUN3ME2wMlAzPTNzIN88US=> MmWzV2FPT0WU
NCI-H720 MmHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL1TWM2OD1yLkCyOVQ3KM7:TR?= M{PkWHNCVkeHUh?=
NCI-N87 NXK3Z25xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2iwWmlEPTB;MD6wNlU6OyEQvF2= NEXpOnRUSU6JRWK=
CHP-212 MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\pTmIzUUN3ME2wMlAzPjJ6IN88US=> NInrR4FUSU6JRWK=
NCI-H23 NXq0[W5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS3TWM2OD1yLkCyOlY2KM7:TR?= NHS1cGxUSU6JRWK=
D-263MG MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ToNWlEPTB;MD6wNlc5PiEQvF2= NYToRmdUW0GQR1XS
ME-180 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z5Z2lEPTB;MD6wNlg6OSEQvF2= MkfnV2FPT0WU
SW982 M3;qdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TCTmlEPTB;MD6wNlk6QSEQvF2= M36yTnNCVkeHUh?=
OE19 Mm\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfQSINkUUN3ME2wMlA{ODd5IN88US=> NETyW5dUSU6JRWK=
SK-LU-1 M2i1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjIO4lPUUN3ME2wMlA{ODh{IN88US=> NWLQOIFFW0GQR1XS
H4 M3\JU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u0fGlEPTB;MD6wN|A6KM7:TR?= NVfDXnN5W0GQR1XS
HT-144 NHz5d41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjVXm1YUUN3ME2wMlA{ODl|IN88US=> MkfCV2FPT0WU
SK-UT-1 M4[3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTFTWM2OD1yLkCzNVc5KM7:TR?= NXLYR4dMW0GQR1XS
D-336MG NHG5VlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnJTWM2OD1yLkCzN|A6KM7:TR?= MlrMV2FPT0WU
MDA-MB-175-VII NGHSboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwMEOzOVQh|ryP MoOxV2FPT0WU
GAMG MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHhSnlOUUN3ME2wMlA{PDN3IN88US=> MnrRV2FPT0WU
CP50-MEL-B MmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjkTWM2OD1yLkCzOFUh|ryP MVHTRW5ITVJ?
OVCAR-5 NEDEPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWn3TWo4UUN3ME2wMlA{PDhizszN M3XW[3NCVkeHUh?=
SK-MES-1 M1jJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwMEO2NFYh|ryP M{HzenNCVkeHUh?=
VM-CUB-1 NILUSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PHRmlEPTB;MD6wN|Y2PyEQvF2= M1LWdnNCVkeHUh?=
WM-115 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq0fXpbUUN3ME2wMlA{PzZ{IN88US=> NIXT[WdUSU6JRWK=
DSH1 NXqzcW56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfOOWlxUUN3ME2wMlA{QDB5IN88US=> NEjJRXpUSU6JRWK=
Becker NHPlN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXoTWM2OD1yLkCzPFg2KM7:TR?= MYLTRW5ITVJ?
SW962 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LFT2lEPTB;MD6wN|k1PSEQvF2= NHu1PXBUSU6JRWK=
TYK-nu Mk\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7m[IZKSzVyPUCuNFM6QDVizszN M4XqcnNCVkeHUh?=
HO-1-N-1 Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXqSWhJUUN3ME2wMlA1ODJzIN88US=> MnfQV2FPT0WU
T98G MoPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PpXWlEPTB;MD6wOFExOyEQvF2= MWXTRW5ITVJ?
ACN NGjWflhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnUfnJKSzVyPUCuNFQyPjJizszN MUDTRW5ITVJ?
SW780 NX;sVFAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7j[ZZiUUN3ME2wMlA1OjB|IN88US=> M1v3bHNCVkeHUh?=
Detroit562 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTuTJdnUUN3ME2wMlA1OjN7IN88US=> MoDOV2FPT0WU
BB49-HNC NFSxSXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfyWFhMUUN3ME2wMlA1OjR|IN88US=> NY\IbGg{W0GQR1XS
HN MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXJfFJKSzVyPUCuNFQzPzJizszN M4S3[XNCVkeHUh?=
H9 NV;OfI1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH3TWM2OD1yLkC0N|cyKM7:TR?= NHLzdFRUSU6JRWK=
VA-ES-BJ M4fL[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nDUGlEPTB;MD6wOFQ1PyEQvF2= M4Pm[XNCVkeHUh?=
MEL-JUSO NXjzbJJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjXRXZJUUN3ME2wMlA1PDd3IN88US=> M13rVXNCVkeHUh?=
BT-474 M3POU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzsV3lkUUN3ME2wMlA1PSEQvF2= M1XUPHNCVkeHUh?=
CaR-1 M3\wW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjDSnV5UUN3ME2wMlA1PTR7IN88US=> NX7pSJJSW0GQR1XS
PSN1 M{fTemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwMES2NFMh|ryP NUS4ZYhTW0GQR1XS
KYSE-510 NWm4fWtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;HTWM2OD1yLkC0OlQ6KM7:TR?= MYrTRW5ITVJ?
KP-4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMES3OVMh|ryP NV21NXp3W0GQR1XS
KYSE-410 M4fTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPTS29{UUN3ME2wMlA1Pzd{IN88US=> M2DiTnNCVkeHUh?=
G-402 M3:we2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMES3PFkh|ryP MlrFV2FPT0WU
DOK MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwMES5NFIh|ryP MkHXV2FPT0WU
COR-L88 Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7nTWM2OD1yLkC0PVEzKM7:TR?= Ml3VV2FPT0WU
SKG-IIIa NFOwR|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHK1VJBKSzVyPUCuNFQ6QDZizszN NIXJO5JUSU6JRWK=
AN3-CA M{f3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nDdWlEPTB;MD6wOUDPxE1? MXHTRW5ITVJ?
SW48 NV;4OG5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuxdFBKSzVyPUCuNFUxOzlizszN NIrmcmlUSU6JRWK=
YKG-1 NHy5dGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHyTWM2OD1yLkC1NFcyKM7:TR?= MljDV2FPT0WU
KYSE-150 NUXBVXlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjMeIdKSzVyPUCuNFUzOzVizszN MlfVV2FPT0WU
HuO-3N1 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPiVGFDUUN3ME2wMlA2OjN5IN88US=> MW\TRW5ITVJ?
LB1047-RCC M4jXVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwMEWyPVYh|ryP NIexTZRUSU6JRWK=
NCI-H2030 NIXBU2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwMEW0NVQh|ryP NITYdIRUSU6JRWK=
YH-13 M{HK[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjJNG5KSzVyPUCuNFU4OjJizszN MUDTRW5ITVJ?
5637 NXm3SpE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVexd2VPUUN3ME2wMlA2PzRizszN NEi2TZlUSU6JRWK=
LOXIMVI Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwMEW4O|Ih|ryP Mnv0V2FPT0WU
GT3TKB MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTxbo17UUN3ME2wMlA2QTR{IN88US=> NX[0W4RXW0GQR1XS
TCCSUP NXjUN3BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37hVGlEPTB;MD6wOVk3PCEQvF2= NGnyXFJUSU6JRWK=
EPLC-272H MnPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X1bWlEPTB;MD6wOlIxPSEQvF2= NHnCZ4lUSU6JRWK=
LU-99A NET1O|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPPOYZKSzVyPUCuNFYzOzdizszN M2WxcnNCVkeHUh?=
NCI-H1755 NWi5RphuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrJT|NKSzVyPUCuNFY{PDFizszN NUPne|VnW0GQR1XS
KM12 NGO5[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnPTWM2OD1yLkC2N|Q5KM7:TR?= NEL3c3lUSU6JRWK=
SF295 NWna[llHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwME[0OVIh|ryP Ml7mV2FPT0WU
MZ2-MEL NXXUXmpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq5TWM2OD1yLkC2OVU{KM7:TR?= NFLpdIFUSU6JRWK=
HEC-1 NH7wUINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojITWM2OD1yLkC2OVg5KM7:TR?= MmXpV2FPT0WU
SW684 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LiTGlEPTB;MD6wOlU6OSEQvF2= NXHqWJVVW0GQR1XS
SF539 NVnwbJFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7MN5JKSzVyPUCuNFY3QDFizszN NYjkWoJsW0GQR1XS
GMS-10 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{L3SGlEPTB;MD6wOlY6QSEQvF2= MkPmV2FPT0WU
MV-4-11 NYjyS21YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjyVnVKSzVyPUCuNFY5ODNizszN MYTTRW5ITVJ?
HT-29 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPmTWM2OD1yLkC2PVE6KM7:TR?= NVn0ZotqW0GQR1XS
23132-87 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDqSG5bUUN3ME2wMlA3QTVizszN NGXSXJhUSU6JRWK=
SW620 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGn4cmdKSzVyPUCuNFcxOjZizszN M4jGUXNCVkeHUh?=
HCC1806 Ml7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nGbmlEPTB;MD6wO|E{OSEQvF2= MU\TRW5ITVJ?
Hs-578-T NInN[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInqeZNKSzVyPUCuNFczODhizszN NELYe|BUSU6JRWK=
A2058 NUXUe2RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XJUGlEPTB;MD6wO|IzQCEQvF2= MmTiV2FPT0WU
MEL-HO NV;Ob3Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\sTWM2OD1yLkC3NlU2KM7:TR?= MnfSV2FPT0WU
HCC2998 NXXDdnN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHleINKSzVyPUCuNFc{PDdizszN MVzTRW5ITVJ?
HuO9 MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37nRmlEPTB;MD6wO|U5QSEQvF2= NFjLbGJUSU6JRWK=
CAL-39 M1L3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPGTWM2OD1yLkC3O|Y3KM7:TR?= MWXTRW5ITVJ?
M14 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DOeWlEPTB;MD6wO|kyOyEQvF2= MlrIV2FPT0WU
BFTC-909 NXy1NZp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPicGlHUUN3ME2wMlA4QTZ7IN88US=> M1vRUXNCVkeHUh?=
TE-11 M2roZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMEe5PVYh|ryP MVrTRW5ITVJ?
TGBC1TKB NIjhflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMEiwOFMh|ryP NXjWOIRpW0GQR1XS
L-363 M2D2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPpR4t3UUN3ME2wMlA5OjB4IN88US=> M1js[HNCVkeHUh?=
A431 MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHZZ|lSUUN3ME2wMlA5OjFizszN M4nMSHNCVkeHUh?=
MKN45 NHK2RZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\FTWM2OD1yLkC4NlE6KM7:TR?= MnvJV2FPT0WU
HT-1080 M2LJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\HTJdOUUN3ME2wMlA5PDN7IN88US=> MmnuV2FPT0WU
OVCAR-8 NIPmeZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInic2JKSzVyPUCuNFg3OjJizszN NH3EbphUSU6JRWK=
LCLC-97TM1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y1TmlEPTB;MD6wPFczQCEQvF2= NEHxV5hUSU6JRWK=
M059J NGjuZZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi3TWM2OD1yLkC5NFI4KM7:TR?= MYLTRW5ITVJ?
SK-MEL-2 MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L5N2lEPTB;MD6wPVA3KM7:TR?= MnHFV2FPT0WU
TE-1 NUTDWm5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml21TWM2OD1yLkC5NlA1KM7:TR?= NELXN2ZUSU6JRWK=
KYSE-180 NWHt[2huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi0[Yh1UUN3ME2wMlA6OjZ{IN88US=> MULTRW5ITVJ?
D-247MG NYfvWHk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7tTmJEUUN3ME2wMlA6PDV3IN88US=> M{PndHNCVkeHUh?=
8-MG-BA MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHvXZRKSzVyPUCuNFk1PzJizszN MU\TRW5ITVJ?
NCI-H1792 M4LJVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f2d2lEPTB;MD6wPVYyQCEQvF2= M33XVHNCVkeHUh?=
MCF7 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjmNHlEUUN3ME2wMlA6Pjd5IN88US=> NV\iPI1IW0GQR1XS
NCI-H2122 M2HId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jsTWlEPTB;MD6wPVc1PSEQvF2= NYj1XIw4W0GQR1XS
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LB2241-RCC MoDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfrVGJ7UUN3ME2wMlExODV2IN88US=> NHLB[FlUSU6JRWK=
SN12C M{jDTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LDNWlEPTB;MD6xNFExPyEQvF2= NYHQeJhSW0GQR1XS
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U251 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDv[pZsUUN3ME2wMlExPTJ3IN88US=> M4fNRnNCVkeHUh?=
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BB65-RCC M3vJW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrR[2xrUUN3ME2wMlExPTV2IN88US=> NHzFcYlUSU6JRWK=
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SW1990 M1vYXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTcY9KSzVyPUCuNVIyPTdizszN M1n6enNCVkeHUh?=
NCI-H1437 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPwZmxKSzVyPUCuNVIyPTdizszN Mn\kV2FPT0WU
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RT-112 NHnJXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTQTWM2OD1yLkG0NFM2KM7:TR?= NH\GTIdUSU6JRWK=
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NCI-H2126 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\YXIU6UUN3ME2wMlU3QDF3IN88US=> NWizUmxTW0GQR1XS
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OVCAR-3 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHZRYpbUUN3ME2wMlU6OzRzIN88US=> MV;TRW5ITVJ?
ACHN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jsNmlEPTB;MD62NFU3QSEQvF2= MW\TRW5ITVJ?
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NCI-H661 NF7JOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz6UVZbUUN3ME2wMlYyOTB2IN88US=> MnjMV2FPT0WU
UACC-893 M3y3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XR[WlEPTB;MD62N|Y5OSEQvF2= NX7wS3FOW0GQR1XS
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NCI-H2009 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfJTWM2OD1yLki1N|EyKM7:TR?= NX;xdFZ5W0GQR1XS
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D-392MG Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i5OmlEPTB;MD64PVM2PiEQvF2= MXnTRW5ITVJ?
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P12-ICHIKAWA Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjqOolKSzVyPUeuOFU2OjNizszN MX\TRW5ITVJ?
NCI-H82 Mo\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLtTWM2OD15LkS1O|AyKM7:TR?= MVfTRW5ITVJ?
NCI-H1993 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\qfFdIUUN3ME23Mlg{ODZ|IN88US=> NX2zN5N5W0GQR1XS
RH-1 NEf3ZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjYRok2UUN3ME23Mlg2OjR2IN88US=> MVfTRW5ITVJ?
SW948 NHKxN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7uVWVKSzVyPUeuPVYxPDlizszN NXX2dpBTW0GQR1XS
CAL-33 NYTJeo1mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfUTWM2OD15Lkm5PVM5KM7:TR?= NEjOR3ZUSU6JRWK=
U-266 MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnmS4tKSzVyPUiuNVU4PzdizszN M37JU3NCVkeHUh?=
CAL-72 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3vclBMUUN3ME24MlIxOzJizszN NILXcldUSU6JRWK=
SNU-423 NIi3SlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTFc2dkUUN3ME25MlM3PjZ4IN88US=> MoXDV2FPT0WU
KG-1 M2Ozdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2izZmlEPTB;OT61PFQ2PiEQvF2= Mlj4V2FPT0WU
HCC1395 NFTtNWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTlwOUKzOVIh|ryP NWCwUnduW0GQR1XS
BE-13 NWfzNnVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M131cWlEPTB;MUCuPFg6OiEQvF2= NFH5UIZUSU6JRWK=
MKN7 M1:yfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFyLkm3OlUh|ryP NVq4XG5oW0GQR1XS
697 M2PaR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWewe|VSUUN3ME2xNU4yPDd{IN88US=> MoHPV2FPT0WU
LU-135 M1:w[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFzLkKzNFch|ryP NHrxZZBUSU6JRWK=
ES7 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqzTWM2OD1zMT6zN|E{KM7:TR?= NID1bXpUSU6JRWK=
SK-HEP-1 M2rCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP3[opKSzVyPUGxMlc3PDZizszN Mn;BV2FPT0WU
BEN NFnoWnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MliwTWM2OD1zMT64OVEh|ryP M4O2cXNCVkeHUh?=
NCI-H1770 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknqTWM2OD1zMj6xNlYh|ryP MXrTRW5ITVJ?
SW13 NVLxSGpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHe1VnZKSzVyPUGyMlE2PDFizszN MmqyV2FPT0WU
MZ1-PC NWi5THNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF{LkW0OVIh|ryP NGPJSHBUSU6JRWK=
Mo-T NUj0W3hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF{Lke0NlEh|ryP NHfifnpUSU6JRWK=
HLE NHfYNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF{LkiyNVUh|ryP MnvOV2FPT0WU
RCC10RGB NG\0SHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHOy[G1KSzVyPUGzMlY4OSEQvF2= MUPTRW5ITVJ?
COLO-320-HSR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzUR2xKSzVyPUGzMlc{QDFizszN MYnTRW5ITVJ?
BHT-101 NW\lXWV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPPUYdKSzVyPUGzMlg{PDVizszN NIX1UYtUSU6JRWK=
OCUB-M Ml7uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\rVYVZUUN3ME2xOE4yPjB{IN88US=> M4f2cnNCVkeHUh?=
MEG-01 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mln1TWM2OD1zND6zO|A5KM7:TR?= MVrTRW5ITVJ?
RS4-11 M1PHU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHwe|dKSzVyPUG0Mlc1OiEQvF2= MoGwV2FPT0WU
MN-60 NV;3THZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF2Lke4PVQh|ryP MnO4V2FPT0WU
NCI-H1304 NFTxemdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7xTWM2OD1zNT6wOFI2KM7:TR?= MVfTRW5ITVJ?
Ramos-2G6-4C10 NGX5coVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\lUZp2UUN3ME2xOU4xPThzIN88US=> NWTqVJZIW0GQR1XS
NCI-H2342 NVLEPVJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF3LkKwOFQh|ryP MUnTRW5ITVJ?
LAN-6 NIi4NIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF3LkS0NVQh|ryP M4jOSnNCVkeHUh?=
JVM-2 NH;CSJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXkNW1KSzVyPUG1MlU4PDhizszN MWDTRW5ITVJ?
P30-OHK MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2eyZmlEPTB;MU[uNFYyPCEQvF2= NFfJ[FFUSU6JRWK=
C-33-A MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF4Lk[yNVQh|ryP NUHiXmxOW0GQR1XS
RPMI-8866 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHtb5B7UUN3ME2xOk45PDl4IN88US=> MVnTRW5ITVJ?
NCI-H630 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf4TWM2OD1zNj64OVM4KM7:TR?= M1rESnNCVkeHUh?=
KYSE-140 M1XoRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7idnlKSzVyPUG3MlIxOjhizszN MnS2V2FPT0WU
T84 M1\3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHSTWM2OD1zOD64Olk2KM7:TR?= M2XjbXNCVkeHUh?=
KU-19-19 MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTafWVWUUN3ME2xPE46PjB6IN88US=> MoLyV2FPT0WU
BALL-1 M{K2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF7LkOzPVkh|ryP NIW0SVFUSU6JRWK=
Calu-6 M3LueWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLLTWM2OD1zOT60PVIh|ryP MVvTRW5ITVJ?
EGI-1 NGLV[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPMZoFTUUN3ME2xPU42QThizszN NVjTfYtFW0GQR1XS
MFH-ino NWHFfo5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HqVGlEPTB;MUmuO|Q2PCEQvF2= MmnQV2FPT0WU
GB-1 MkDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LRUWlEPTB;MkCuN|U{PSEQvF2= M{fTV3NCVkeHUh?=
NCI-H1693 M4\KW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrVS|BKSzVyPUKwMlY2ODVizszN M{XPe3NCVkeHUh?=
SW1116 NGLBcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfJeHJKSzVyPUKwMlk{PjJizszN NV;OUYhIW0GQR1XS
H-EMC-SS NUTNOlI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJ{LkC0OUDPxE1? MV;TRW5ITVJ?
D-502MG Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHPTWM2OD1{Mj64NlYyKM7:TR?= M1TZd3NCVkeHUh?=
IA-LM NIG4SJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ja[WlEPTB;MkOuNlQ6OyEQvF2= M1Tuc3NCVkeHUh?=
SW1463 Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK1NVZKSzVyPUKzMlc6KM7:TR?= MkjOV2FPT0WU
JAR MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ2LkOyPVMh|ryP M1f0VHNCVkeHUh?=
HT M{fRdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;yPJBKSzVyPUK0MlQ4PTNizszN MXfTRW5ITVJ?
LCLC-103H MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7ITWM2OD1{ND64OFQ6KM7:TR?= MnHXV2FPT0WU
SNU-449 MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LyeWlEPTB;MkSuPFc1OSEQvF2= NVvx[|dtW0GQR1XS
KE-37 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIiy[lJKSzVyPUK1MlA6OjhizszN M1vsWHNCVkeHUh?=
NCI-H1623 NV\iW282T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;Le5NZUUN3ME2yO{4yOzB|IN88US=> MU\TRW5ITVJ?
MOLT-13 M4HR[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrVbHBnUUN3ME2yO{4{PTF4IN88US=> NV7kWnpiW0GQR1XS
COLO-741 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXnfIhyUUN3ME2zNU4{OzN|IN88US=> MX7TRW5ITVJ?
NB6 NV7NdnNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnewTWM2OD1|Mj6yPFc3KM7:TR?= M4i4[HNCVkeHUh?=
MOLT-16 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDkTWM2OD1|Mz6wNFU2KM7:TR?= Ml60V2FPT0WU
IST-MES1 M1\yWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTN2LkC1OFEh|ryP NV;icY9YW0GQR1XS
A4-Fuk MoHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrTTWM2OD1|NT6wOlYh|ryP NHS0fplUSU6JRWK=
CAL-85-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nRfmlEPTB;M{WuNlgyPyEQvF2= MUTTRW5ITVJ?
CCRF-CEM NYC0dXY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN5LkG1N|Yh|ryP NEjofldUSU6JRWK=
HAL-01 NHnHXG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WxbGlEPTB;M{iuOFg5QSEQvF2= MULTRW5ITVJ?
HEL MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[0XGlEPTB;NEOuN|QxQSEQvF2= MVnTRW5ITVJ?
EW-1 NXHpXYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2D0O2lEPTB;NEOuOFc3QCEQvF2= MmnOV2FPT0WU
MDA-MB-231 NV7jcW41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTR3LkGxPVkh|ryP NFfj[ZhUSU6JRWK=
ABC-1 M3HzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7kZWlKSzVyPUS2Mlg2OzhizszN NX24Z49ZW0GQR1XS
NCI-H446 NE\MOmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi3UZBVUUN3ME20PE42ODV6IN88US=> NYHCWlVWW0GQR1XS
MHH-PREB-1 NULNVGVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfJcGlKSzVyPUS5MlYxODdizszN NGH2S4xUSU6JRWK=
DOHH-2 NXrLcFhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW5cXBLUUN3ME20PU43PjV4IN88US=> M1jDUXNCVkeHUh?=
GCT M33MZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP3TWM2OD12OT62PVc3KM7:TR?= NHj6emFUSU6JRWK=

... 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

文献中の引用 (19)

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

技術サポート&よくある質問(FAQ)

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Related HSP (e.g. HSP90) 阻害剤

  • PU-H71

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

  • KNK437

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

  • VER155008

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

  • FRAX597

    FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.

  • 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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