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>? MVXJR|UxRTBwMECwN|A{KM7:TR?= MXjTRW5ITVJ?
IST-MEL1 NEL0UFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTBwMECwOFA4KM7:TR?= MYPTRW5ITVJ?
NCI-SNU-1 M1XH[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwMECyNFch|ryP NWG1VXhCW0GQR1XS
FADU NGLQ[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rDPGlEPTB;MD6wNFIxQSEQvF2= MlyyV2FPT0WU
C32 MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnETWM2OD1yLkCwN|A1KM7:TR?= NXfqfGZUW0GQR1XS
D-566MG M13WOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvvOphmUUN3ME2wMlAxOzlizszN NUn5XZd4W0GQR1XS
LXF-289 NGK4[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHTXI44UUN3ME2wMlAxPDF7IN88US=> M2K0UXNCVkeHUh?=
HGC-27 NGSzboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DqNmlEPTB;MD6wNFUyKM7:TR?= NIPlc5lUSU6JRWK=
RPMI-7951 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEC3NVch|ryP NHmzOFBUSU6JRWK=
HSC-3 M1;mWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nEU2lEPTB;MD6wNFkzQSEQvF2= MYnTRW5ITVJ?
MIA-PaCa-2 NGjQSGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe5bWlKSzVyPUCuNFExODlizszN MmjhV2FPT0WU
KS-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GzU2lEPTB;MD6wNVM2PSEQvF2= MXjTRW5ITVJ?
CAL-51 NHToTZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i1OGlEPTB;MD6wNVQxPSEQvF2= NFfZbJVUSU6JRWK=
MDA-MB-361 NXLPWZdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwMEG0PVUh|ryP MXjTRW5ITVJ?
TI-73 M4jMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrqTWM2OD1yLkCxO|k3KM7:TR?= NFjtXoRUSU6JRWK=
AGS MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr3ZZZIUUN3ME2wMlAyQTN6IN88US=> M1PQbHNCVkeHUh?=
NCI-H460 NU\OO|lmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjIc5E4UUN3ME2wMlAyQTd2IN88US=> NUHTTmZIW0GQR1XS
A204 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHlWXB4UUN3ME2wMlAzOjR7IN88US=> MoO3V2FPT0WU
CHL-1 Ml\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHofo5KSzVyPUCuNFIzPTFizszN Mn61V2FPT0WU
DU-4475 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwMEKyOlEh|ryP MnXBV2FPT0WU
CGTH-W-1 MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\ocVRKSzVyPUCuNFI{PDlizszN NGPRdWJUSU6JRWK=
HCC2218 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHtSlNKSzVyPUCuNFI1QTRizszN M4fodHNCVkeHUh?=
A2780 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTxWlFlUUN3ME2wMlAzPTNzIN88US=> NILtSolUSU6JRWK=
NCI-H720 M3HMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\rT2lEPTB;MD6wNlU1PiEQvF2= NYfQbZZNW0GQR1XS
NCI-N87 M3nIfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvjTnRrUUN3ME2wMlAzPTl|IN88US=> MWnTRW5ITVJ?
CHP-212 NFXxOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTQPWNKSzVyPUCuNFI3OjhizszN MmDBV2FPT0WU
NCI-H23 NFTyV3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMEK2OlUh|ryP NWPSNZlRW0GQR1XS
D-263MG MkLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMEK3PFYh|ryP MmLtV2FPT0WU
ME-180 NH7hXW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMEK4PVEh|ryP M1zOPXNCVkeHUh?=
SW982 M1q0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TGemlEPTB;MD6wNlk6QSEQvF2= M4\zRnNCVkeHUh?=
OE19 M{PjeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\jfldKSzVyPUCuNFMxPzdizszN MXTTRW5ITVJ?
SK-LU-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwMEOwPFIh|ryP NEGx[mJUSU6JRWK=
H4 NYTWVGxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUntTpl7UUN3ME2wMlA{ODlizszN NF\EOpZUSU6JRWK=
HT-144 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjqVoZnUUN3ME2wMlA{ODl|IN88US=> NFe0TIFUSU6JRWK=
SK-UT-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwMEOxO|gh|ryP NHfZN4RUSU6JRWK=
D-336MG NVntOWJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TXSmlEPTB;MD6wN|MxQSEQvF2= MmTFV2FPT0WU
MDA-MB-175-VII M4fMPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTETWM2OD1yLkCzN|U1KM7:TR?= MWHTRW5ITVJ?
GAMG MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwMEO0N|Uh|ryP NUmzcFFbW0GQR1XS
CP50-MEL-B MnLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwMEO0OUDPxE1? NYX2UHY4W0GQR1XS
OVCAR-5 NGryeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMEO0PEDPxE1? NXvDT2ZTW0GQR1XS
SK-MES-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMEO2NFYh|ryP Mlv1V2FPT0WU
VM-CUB-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMEO2OVch|ryP M4Pib3NCVkeHUh?=
WM-115 M1LheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPFZpRKSzVyPUCuNFM4PjJizszN M3nWN3NCVkeHUh?=
DSH1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMEO4NFch|ryP M4i0dnNCVkeHUh?=
Becker MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7nR2tKSzVyPUCuNFM5QDVizszN M1;3cXNCVkeHUh?=
SW962 M1\4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMEO5OFUh|ryP M3i0fXNCVkeHUh?=
TYK-nu NFvZdnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljUTWM2OD1yLkCzPVg2KM7:TR?= NE\RdYNUSU6JRWK=
HO-1-N-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWruV5ByUUN3ME2wMlA1ODJzIN88US=> MXHTRW5ITVJ?
T98G NFzaZZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmW1TWM2OD1yLkC0NVA{KM7:TR?= MXfTRW5ITVJ?
ACN NUWyRVZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHDfYxSUUN3ME2wMlA1OTZ{IN88US=> NW\TPJRKW0GQR1XS
SW780 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwMESyNFMh|ryP NHP4OY5USU6JRWK=
Detroit562 NHrwXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnMZWRvUUN3ME2wMlA1OjN7IN88US=> MoHsV2FPT0WU
BB49-HNC MoPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe4OFJKSzVyPUCuNFQzPDNizszN NIX1NWFUSU6JRWK=
HN NXr1R2M3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwMESyO|Ih|ryP MoGxV2FPT0WU
H9 M3XBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{njc2lEPTB;MD6wOFM4OSEQvF2= MoTmV2FPT0WU
VA-ES-BJ NXHRR2NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnUR40xUUN3ME2wMlA1PDR5IN88US=> M1n2SXNCVkeHUh?=
MEL-JUSO MonqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fhPGlEPTB;MD6wOFQ4PSEQvF2= MkTjV2FPT0WU
BT-474 NUWxWXRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDo[FdKSzVyPUCuNFQ2KM7:TR?= MY\TRW5ITVJ?
CaR-1 NFvzfZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwMES1OFkh|ryP Ml;FV2FPT0WU
PSN1 M3HPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwMES2NFMh|ryP MVXTRW5ITVJ?
KYSE-510 NV74S3hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfkSIhwUUN3ME2wMlA1PjR7IN88US=> M2nSNnNCVkeHUh?=
KP-4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PFUWlEPTB;MD6wOFc2OyEQvF2= MX7TRW5ITVJ?
KYSE-410 MnP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr2VGtKSzVyPUCuNFQ4PzJizszN NXH4VVc2W0GQR1XS
G-402 M1\QfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnMTWM2OD1yLkC0O|g6KM7:TR?= NUXFbGh3W0GQR1XS
DOK MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmC2TWM2OD1yLkC0PVAzKM7:TR?= NF34UVFUSU6JRWK=
COR-L88 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnnWYhKSzVyPUCuNFQ6OTJizszN NVrWe2t4W0GQR1XS
SKG-IIIa M3;Nemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS0WXI1UUN3ME2wMlA1QTh4IN88US=> MoXnV2FPT0WU
AN3-CA NV;4UZZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XESmlEPTB;MD6wOUDPxE1? MUTTRW5ITVJ?
SW48 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTOTYo5UUN3ME2wMlA2ODN7IN88US=> NIjrZndUSU6JRWK=
YKG-1 MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwMEWwO|Eh|ryP NUnsS|N5W0GQR1XS
KYSE-150 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwMEWyN|Uh|ryP MkS1V2FPT0WU
HuO-3N1 NHnr[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTm[3huUUN3ME2wMlA2OjN5IN88US=> NXXz[4h2W0GQR1XS
LB1047-RCC MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojGTWM2OD1yLkC1Nlk3KM7:TR?= M1LLZ3NCVkeHUh?=
NCI-H2030 NUHodXAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEn5RWlKSzVyPUCuNFU1OTRizszN M2HXfnNCVkeHUh?=
YH-13 NYr1c5g5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwMEW3NlIh|ryP MoC3V2FPT0WU
5637 MkDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLUTWM2OD1yLkC1O|Qh|ryP NYj0ZnhZW0GQR1XS
LOXIMVI NWfRS5ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HO[2lEPTB;MD6wOVg4OiEQvF2= NGnsfGhUSU6JRWK=
GT3TKB MnewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPIPY5ZUUN3ME2wMlA2QTR{IN88US=> NXGwdW5nW0GQR1XS
TCCSUP MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwMEW5OlQh|ryP NXTyNpczW0GQR1XS
EPLC-272H M1f5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXnU5NKSzVyPUCuNFYzODVizszN MmfQV2FPT0WU
LU-99A NXHwdndOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwME[yN|ch|ryP NHey[|NUSU6JRWK=
NCI-H1755 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHWTWM2OD1yLkC2N|QyKM7:TR?= MWTTRW5ITVJ?
KM12 M1zHU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KyOGlEPTB;MD6wOlM1QCEQvF2= M1TuVXNCVkeHUh?=
SF295 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwME[0OVIh|ryP NIr5NnpUSU6JRWK=
MZ2-MEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHRc5luUUN3ME2wMlA3PTV|IN88US=> NImwbnhUSU6JRWK=
HEC-1 M4P2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfHTWM2OD1yLkC2OVg5KM7:TR?= NX\DeZNvW0GQR1XS
SW684 MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwME[1PVEh|ryP Mn;0V2FPT0WU
SF539 NHy5S3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rmSmlEPTB;MD6wOlY5OSEQvF2= MlmwV2FPT0WU
GMS-10 M{fVNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzYTWM2OD1yLkC2Olk6KM7:TR?= MWDTRW5ITVJ?
MV-4-11 NYnz[4VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHpO4xKSzVyPUCuNFY5ODNizszN NYT1UIs{W0GQR1XS
HT-29 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHjNGo4UUN3ME2wMlA3QTF7IN88US=> MoH4V2FPT0WU
23132-87 NITn[XVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwME[5OUDPxE1? MmD0V2FPT0WU
SW620 NXHSeGRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\pV2lEPTB;MD6wO|AzPiEQvF2= NUSydGM{W0GQR1XS
HCC1806 NYHZPW9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO5NJB7UUN3ME2wMlA4OTNzIN88US=> NV[yfpRQW0GQR1XS
Hs-578-T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMEeyNFgh|ryP NYXMVHFVW0GQR1XS
A2058 M1KwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmqwTWM2OD1yLkC3NlI5KM7:TR?= MonrV2FPT0WU
MEL-HO MkLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMEeyOVUh|ryP NWLndGg1W0GQR1XS
HCC2998 NETDSG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjMOGl{UUN3ME2wMlA4OzR5IN88US=> NWHYV5N[W0GQR1XS
HuO9 M2ftVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn5N|RiUUN3ME2wMlA4PTh7IN88US=> NETJV3RUSU6JRWK=
CAL-39 NWP0fJVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz0UHNKSzVyPUCuNFc4PjZizszN M3rxenNCVkeHUh?=
M14 NGTmd2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LkXWlEPTB;MD6wO|kyOyEQvF2= NV\4cJlHW0GQR1XS
BFTC-909 NETyOG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W3WmlEPTB;MD6wO|k3QSEQvF2= MU\TRW5ITVJ?
TE-11 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMEe5PVYh|ryP M1vGcXNCVkeHUh?=
TGBC1TKB M{DubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnXeJdtUUN3ME2wMlA5ODR|IN88US=> NGOyNpBUSU6JRWK=
L-363 NWLoSHA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rNPWlEPTB;MD6wPFIxPiEQvF2= NEfISnJUSU6JRWK=
A431 NH3I[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f6SGlEPTB;MD6wPFIyKM7:TR?= MnfEV2FPT0WU
MKN45 NVTCPIFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL6e2VKSzVyPUCuNFgzOTlizszN M3vOOXNCVkeHUh?=
HT-1080 NXXieoE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLZTWM2OD1yLkC4OFM6KM7:TR?= NV7M[Xl3W0GQR1XS
OVCAR-8 NGXDTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTydIRTUUN3ME2wMlA5PjJ{IN88US=> MYjTRW5ITVJ?
LCLC-97TM1 NVX2[m9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\GTWM2OD1yLkC4O|I5KM7:TR?= MUDTRW5ITVJ?
M059J NFOxe|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zXeGlEPTB;MD6wPVAzPyEQvF2= MVrTRW5ITVJ?
SK-MEL-2 M2[2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X4NmlEPTB;MD6wPVA3KM7:TR?= NYf6boN6W0GQR1XS
TE-1 M4LaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn60TWM2OD1yLkC5NlA1KM7:TR?= MUDTRW5ITVJ?
KYSE-180 NV;Cb4VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHFcZRoUUN3ME2wMlA6OjZ{IN88US=> NU\jXYo{W0GQR1XS
D-247MG M3PxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvxTWM2OD1yLkC5OFU2KM7:TR?= NUSxPGh5W0GQR1XS
8-MG-BA NYjobWRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rjRmlEPTB;MD6wPVQ4OiEQvF2= Mlm3V2FPT0WU
NCI-H1792 M164S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M370TmlEPTB;MD6wPVYyQCEQvF2= M1zuT3NCVkeHUh?=
MCF7 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;MTWM2OD1yLkC5Olc4KM7:TR?= MV\TRW5ITVJ?
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TE-5 NFji[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHLXm84UUN3ME23MlQyOjl6IN88US=> MnjJV2FPT0WU
P12-ICHIKAWA NHO5NY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTkelBFUUN3ME23MlQ2PTJ|IN88US=> MnLJV2FPT0WU
NCI-H82 M3HadGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3YNmxKSzVyPUeuOFU4ODFizszN MoHMV2FPT0WU
NCI-H1993 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULNOm0{UUN3ME23Mlg{ODZ|IN88US=> M4DuWHNCVkeHUh?=
RH-1 NY\tUGs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj2UXliUUN3ME23Mlg2OjR2IN88US=> M2DhdXNCVkeHUh?=
SW948 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG1OINKSzVyPUeuPVYxPDlizszN M1\icHNCVkeHUh?=
CAL-33 M4rBb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3jOpJKSzVyPUeuPVk6OzhizszN MUnTRW5ITVJ?
U-266 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j3OGlEPTB;OD6xOVc4PyEQvF2= M3n0[HNCVkeHUh?=
CAL-72 NFu2XJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NICycFdKSzVyPUiuNlA{OiEQvF2= NY\mOZBmW0GQR1XS
SNU-423 NWjMcox5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\PdGxKSzVyPUmuN|Y3PjZizszN NGHxNFdUSU6JRWK=
KG-1 NVjMZpdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS0THFkUUN3ME25MlU5PDV4IN88US=> NH;PUWVUSU6JRWK=
HCC1395 NHq5cWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTlwOUKzOVIh|ryP M{jDbnNCVkeHUh?=
BE-13 M33FfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTFyLki4PVIh|ryP MlH6V2FPT0WU
MKN7 NWLqc4h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f5ZWlEPTB;MUCuPVc3PSEQvF2= M4nBbHNCVkeHUh?=
697 M2\ZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLGe21XUUN3ME2xNU4yPDd{IN88US=> MkO4V2FPT0WU
LU-135 MorES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XrTWlEPTB;MUGuNlMxPyEQvF2= MkHkV2FPT0WU
ES7 M4PVcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXKWmpNUUN3ME2xNU4{OzF|IN88US=> Mn\6V2FPT0WU
SK-HEP-1 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XXdGlEPTB;MUGuO|Y1PiEQvF2= NVzLVGx2W0GQR1XS
BEN M3\rV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TO[2lEPTB;MUGuPFUyKM7:TR?= NF7KR3NUSU6JRWK=
NCI-H1770 NHTU[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrb|I4UUN3ME2xNk4yOjZizszN MknXV2FPT0WU
SW13 M3W1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;TZ|k3UUN3ME2xNk4yPTRzIN88US=> NY[3Z|JpW0GQR1XS
MZ1-PC M{mwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fLUWlEPTB;MUKuOVQ2OiEQvF2= NWDLW4ttW0GQR1XS
Mo-T Ml7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF{Lke0NlEh|ryP MXfTRW5ITVJ?
HLE M2jPcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjsUJFKSzVyPUGyMlgzOTVizszN NFnTUGFUSU6JRWK=
RCC10RGB M1u4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[2dJJKSzVyPUGzMlY4OSEQvF2= NGLFRo9USU6JRWK=
COLO-320-HSR M1\KeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LNSGlEPTB;MUOuO|M5OSEQvF2= NFnoWIlUSU6JRWK=
BHT-101 Mor6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF|LkizOFUh|ryP NGLMOVhUSU6JRWK=
OCUB-M M1\lT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\wb2lEPTB;MUSuNVYxOiEQvF2= NYLuVVVSW0GQR1XS
MEG-01 NX7CZXoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknnTWM2OD1zND6zO|A5KM7:TR?= NEf6WVFUSU6JRWK=
RS4-11 NVTVNWRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7ERVNKSzVyPUG0Mlc1OiEQvF2= MnrXV2FPT0WU
MN-60 NF7Me2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nRRmlEPTB;MUSuO|g6PCEQvF2= NUDSepN4W0GQR1XS
NCI-H1304 NIP2OYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\SSGU1UUN3ME2xOU4xPDJ3IN88US=> MnjRV2FPT0WU
Ramos-2G6-4C10 NWmyNJhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF3LkC1PFEh|ryP NIfCNllUSU6JRWK=
NCI-H2342 M{jWRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTF3LkKwOFQh|ryP NHfv[WhUSU6JRWK=
LAN-6 NWPFe285T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP1dYs3UUN3ME2xOU41PDF2IN88US=> MnPHV2FPT0WU
JVM-2 NIjUeWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzrTWM2OD1zNT61O|Q5KM7:TR?= NFG4WFhUSU6JRWK=
P30-OHK NYeyZWNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV70PXhnUUN3ME2xOk4xPjF2IN88US=> MoW5V2FPT0WU
C-33-A M{TGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TqeGlEPTB;MU[uOlIyPCEQvF2= MYPTRW5ITVJ?
RPMI-8866 NVHudYlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrHPHNVUUN3ME2xOk45PDl4IN88US=> MlfuV2FPT0WU
NCI-H630 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF4Lki1N|ch|ryP MVHTRW5ITVJ?
KYSE-140 M{Dr[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nGSWlEPTB;MUeuNlAzQCEQvF2= NHrFeYtUSU6JRWK=
T84 M4PWTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnYNG5KSzVyPUG4Mlg3QTVizszN MnTRV2FPT0WU
KU-19-19 M{HsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmn1TWM2OD1zOD65OlA5KM7:TR?= NGnDfnhUSU6JRWK=
BALL-1 MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTF7LkOzPVkh|ryP NWHyXVdxW0GQR1XS
Calu-6 MoS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF7LkS5NkDPxE1? Mmj4V2FPT0WU
EGI-1 NWX2WZhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLlTWM2OD1zOT61PVgh|ryP M3nyZXNCVkeHUh?=
MFH-ino MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF7Lke0OVQh|ryP M3zrPHNCVkeHUh?=
GB-1 NVn5OXF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTJyLkO1N|Uh|ryP NFfmW4pUSU6JRWK=
NCI-H1693 M2TCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLyTWM2OD1{MD62OVA2KM7:TR?= M1Pw[HNCVkeHUh?=
SW1116 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\DXWlEPTB;MkCuPVM3OiEQvF2= NE\LNHFUSU6JRWK=
H-EMC-SS M4nxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTYTWM2OD1{Mj6wOFUh|ryP MU\TRW5ITVJ?
D-502MG M3nJO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrVYRKSzVyPUKyMlgzPjFizszN M17zRXNCVkeHUh?=
IA-LM NE\wNIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnyUJpKSzVyPUKzMlI1QTNizszN MnTxV2FPT0WU
SW1463 M3qzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3XNYUzUUN3ME2yN{44QSEQvF2= NF\HOnRUSU6JRWK=
JAR MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;1clZjUUN3ME2yOE4{Ojl|IN88US=> MVzTRW5ITVJ?
HT M3y0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfDbnR2UUN3ME2yOE41PzV|IN88US=> NGL6dZpUSU6JRWK=
LCLC-103H MkjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ2Lki0OFkh|ryP MYjTRW5ITVJ?
SNU-449 NI\mV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\xUVhPUUN3ME2yOE45PzRzIN88US=> NITGbYdUSU6JRWK=
KE-37 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLkd|NDUUN3ME2yOU4xQTJ6IN88US=> M4\oe3NCVkeHUh?=
NCI-H1623 NF\qfolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXGW2w3UUN3ME2yO{4yOzB|IN88US=> NGLHXHlUSU6JRWK=
MOLT-13 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\WeHltUUN3ME2yO{4{PTF4IN88US=> Mn3jV2FPT0WU
COLO-741 NH3PZYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy5NJpKSzVyPUOxMlM{OzNizszN NWjJOGI4W0GQR1XS
NB6 NXrZcGo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zOVWlEPTB;M{KuNlg4PiEQvF2= NXW3d5VkW0GQR1XS
MOLT-16 MkfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T3c2lEPTB;M{OuNFA2PSEQvF2= MmnlV2FPT0WU
IST-MES1 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G4fmlEPTB;M{SuNFU1OSEQvF2= NH3aSHBUSU6JRWK=
A4-Fuk M4LnUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHYTWM2OD1|NT6wOlYh|ryP MWTTRW5ITVJ?
CAL-85-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTN3LkK4NVch|ryP MXXTRW5ITVJ?
CCRF-CEM MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHjfJU6UUN3ME2zO{4yPTN4IN88US=> MmPCV2FPT0WU
HAL-01 MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXxV2Q6UUN3ME2zPE41QDh7IN88US=> M{XDb3NCVkeHUh?=
HEL MkHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTR|LkO0NFkh|ryP NFWy[4NUSU6JRWK=
EW-1 NUG0eGk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrWTWM2OD12Mz60O|Y5KM7:TR?= NX7ETYhjW0GQR1XS
MDA-MB-231 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP4blZKSzVyPUS1MlEyQTlizszN MXTTRW5ITVJ?
ABC-1 MlTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPTpZvUUN3ME20Ok45PTN6IN88US=> NXfy[W1ZW0GQR1XS
NCI-H446 MlLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7DcJc3UUN3ME20PE42ODV6IN88US=> Mn7jV2FPT0WU
MHH-PREB-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfKO4ZwUUN3ME20PU43ODB5IN88US=> M{L1V3NCVkeHUh?=
DOHH-2 NXjxNY5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTR7Lk[2OVYh|ryP NILvT2xUSU6JRWK=
GCT NW\NSHdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jYRmlEPTB;NEmuOlk4PiEQvF2= MUnTRW5ITVJ?

... 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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