Tanespimycin (17-AAG)

製品コードS1141 別名:CP127374,NSC-330507, KOS 953

Tanespimycin (17-AAG)化学構造

分子量(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.

サイズ 価格(税別)  
JPY 32370.00
JPY 24900.00
JPY 61420.00

カスタマーフィードバック(9)

  • (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.

  • 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.

    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.

    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.

  • 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.

    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.

  • 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.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 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.
特性 Displays very low toxicity toward normal cells.
ターゲット
HSP90 [1]
(Cell-free assay)
5 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMECwN|A{KM7:TR?= MkLMV2FPT0WU
IST-MEL1 NIf3eXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnNSWJKSzVyPUCuNFAxPDB5IN88US=> MWLTRW5ITVJ?
NCI-SNU-1 NUHN[Gk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fMPGlEPTB;MD6wNFIxPyEQvF2= NXLXcWc3W0GQR1XS
FADU MnT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrHTWM2OD1yLkCwNlA6KM7:TR?= M{PFfXNCVkeHUh?=
C32 NH\1S3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXO0bnROUUN3ME2wMlAxOzB2IN88US=> MWDTRW5ITVJ?
D-566MG NYfscoROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HLO2lEPTB;MD6wNFM6KM7:TR?= Mkn3V2FPT0WU
LXF-289 M2e0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMEC0NVkh|ryP NX;FXJhbW0GQR1XS
HGC-27 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMEC1NUDPxE1? M2nNe3NCVkeHUh?=
RPMI-7951 NVj2dZJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj6TWM2OD1yLkCwO|E4KM7:TR?= MXrTRW5ITVJ?
HSC-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\IZ4RKSzVyPUCuNFA6OjlizszN NXPFW4VXW0GQR1XS
MIA-PaCa-2 NVHMdmVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;DVYZKSzVyPUCuNFExODlizszN MUnTRW5ITVJ?
KS-1 NIe4XpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3fGNUUUN3ME2wMlAyOzV3IN88US=> M2n2c3NCVkeHUh?=
CAL-51 NIiy[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLwTWM2OD1yLkCxOFA2KM7:TR?= NEW2TpVUSU6JRWK=
MDA-MB-361 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXxXnhKSzVyPUCuNFE1QTVizszN M17ue3NCVkeHUh?=
TI-73 NGL5fVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPiTWM2OD1yLkCxO|k3KM7:TR?= MX;TRW5ITVJ?
AGS NH7SeGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrYUo5tUUN3ME2wMlAyQTN6IN88US=> NH2xS21USU6JRWK=
NCI-H460 NXjvUIRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XPN2lEPTB;MD6wNVk4PCEQvF2= NWf2OZJTW0GQR1XS
A204 NWO1dGRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2S5c2lEPTB;MD6wNlI1QSEQvF2= NVPjblJKW0GQR1XS
CHL-1 NXX1b4hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwMEKyOVEh|ryP M17SR3NCVkeHUh?=
DU-4475 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjxWndKSzVyPUCuNFIzPjFizszN MYDTRW5ITVJ?
CGTH-W-1 M17mNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PHPGlEPTB;MD6wNlM1QSEQvF2= MkTVV2FPT0WU
HCC2218 NVLpSYhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXTWmlTUUN3ME2wMlAzPDl2IN88US=> NYLmVnN[W0GQR1XS
A2780 MlTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMEK1N|Eh|ryP MW\TRW5ITVJ?
NCI-H720 NY\uVnM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTweY9KSzVyPUCuNFI2PDZizszN M37ER3NCVkeHUh?=
NCI-N87 MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHKU5lKSzVyPUCuNFI2QTNizszN NF;BWmFUSU6JRWK=
CHP-212 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LD[mlEPTB;MD6wNlYzQCEQvF2= NEC3cnVUSU6JRWK=
NCI-H23 MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwMEK2OlUh|ryP NI\mOXZUSU6JRWK=
D-263MG MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z2N2lEPTB;MD6wNlc5PiEQvF2= MlHJV2FPT0WU
ME-180 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfKd5VtUUN3ME2wMlAzQDlzIN88US=> MXzTRW5ITVJ?
SW982 NU\4emJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLoTlBKSzVyPUCuNFI6QTlizszN NYLIZWRxW0GQR1XS
OE19 NXG3dpFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDiTWM2OD1yLkCzNFc4KM7:TR?= NFOzOmtUSU6JRWK=
SK-LU-1 NULLOGFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMEOwPFIh|ryP M1ruTHNCVkeHUh?=
H4 M3v1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETTTJJKSzVyPUCuNFMxQSEQvF2= M3nqOHNCVkeHUh?=
HT-144 NIrlOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq5SmtKSzVyPUCuNFMxQTNizszN NXnP[oNXW0GQR1XS
SK-UT-1 NEHJ[XNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\UNGtKSzVyPUCuNFMyPzhizszN M4\Fd3NCVkeHUh?=
D-336MG MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f2c2lEPTB;MD6wN|MxQSEQvF2= Mo\IV2FPT0WU
MDA-MB-175-VII M4rOWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzoZlRKSzVyPUCuNFM{PTRizszN NFSyZWJUSU6JRWK=
GAMG M{XJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjFTWM2OD1yLkCzOFM2KM7:TR?= MlPWV2FPT0WU
CP50-MEL-B M1TqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzPWZFKSzVyPUCuNFM1PSEQvF2= M1PSVXNCVkeHUh?=
OVCAR-5 M{HRWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL6TWM2OD1yLkCzOFgh|ryP NITqb2FUSU6JRWK=
SK-MES-1 MmnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwMEO2NFYh|ryP NWjvfYw4W0GQR1XS
VM-CUB-1 M4S4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7OSHF1UUN3ME2wMlA{PjV5IN88US=> MUTTRW5ITVJ?
WM-115 NIW2flhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMEO3OlIh|ryP MY\TRW5ITVJ?
DSH1 M4PNOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwMEO4NFch|ryP M{e1NnNCVkeHUh?=
Becker M3m2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjVenZPUUN3ME2wMlA{QDh3IN88US=> MljrV2FPT0WU
SW962 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDBTWM2OD1yLkCzPVQ2KM7:TR?= NEK4cVlUSU6JRWK=
TYK-nu NFHlSXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMEO5PFUh|ryP NFvNTXhUSU6JRWK=
HO-1-N-1 M4XyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ztdGlEPTB;MD6wOFAzOSEQvF2= M2njOXNCVkeHUh?=
T98G NGmwTVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELnV5FKSzVyPUCuNFQyODNizszN NX:zWnlkW0GQR1XS
ACN NHu1T41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\oRVhKSzVyPUCuNFQyPjJizszN NVe3RpRVW0GQR1XS
SW780 M2ruNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMESyNFMh|ryP M3TiT3NCVkeHUh?=
Detroit562 M2DzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X3fmlEPTB;MD6wOFI{QSEQvF2= MV;TRW5ITVJ?
BB49-HNC NEjqeW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TyN2lEPTB;MD6wOFI1OyEQvF2= NHHsPItUSU6JRWK=
HN MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni1TWM2OD1yLkC0NlczKM7:TR?= NW[xZnViW0GQR1XS
H9 NUK4R2p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITMUWtKSzVyPUCuNFQ{PzFizszN NF7tNlFUSU6JRWK=
VA-ES-BJ NGW0boxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMES0OFch|ryP M2rEfXNCVkeHUh?=
MEL-JUSO NGXTSmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT4VWJKUUN3ME2wMlA1PDd3IN88US=> M3LZOnNCVkeHUh?=
BT-474 M3LNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LlUGlEPTB;MD6wOFUh|ryP M3frXnNCVkeHUh?=
CaR-1 NWfjd|c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPRbJFKSzVyPUCuNFQ2PDlizszN MUDTRW5ITVJ?
PSN1 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH33OXRKSzVyPUCuNFQ3ODNizszN NHjiPXVUSU6JRWK=
KYSE-510 NWDUVpVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwMES2OFkh|ryP MUjTRW5ITVJ?
KP-4 NHfkU|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW1O5NpUUN3ME2wMlA1PzV|IN88US=> M{TrPHNCVkeHUh?=
KYSE-410 MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID2dFdKSzVyPUCuNFQ4PzJizszN NETGTVJUSU6JRWK=
G-402 NGjFN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMES3PFkh|ryP NF;pW5hUSU6JRWK=
DOK MlT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPsOXpSUUN3ME2wMlA1QTB{IN88US=> NUPSTWxvW0GQR1XS
COR-L88 M{X0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXhTWM2OD1yLkC0PVEzKM7:TR?= MYHTRW5ITVJ?
SKG-IIIa M37B[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Hk[GlEPTB;MD6wOFk5PiEQvF2= NH\jNWpUSU6JRWK=
AN3-CA NXjDW4ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTiXIJKSzVyPUCuNFUh|ryP MV\TRW5ITVJ?
SW48 NWm2fJhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\VWWlEPTB;MD6wOVA{QSEQvF2= Ml7HV2FPT0WU
YKG-1 M{jw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXqflNzUUN3ME2wMlA2ODdzIN88US=> MWrTRW5ITVJ?
KYSE-150 M4\IZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHhTWM2OD1yLkC1NlM2KM7:TR?= M3\HXHNCVkeHUh?=
HuO-3N1 NEjTdodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:yfnpKUUN3ME2wMlA2OjN5IN88US=> NWH3c2NxW0GQR1XS
LB1047-RCC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMEWyPVYh|ryP M4jPbHNCVkeHUh?=
NCI-H2030 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwMEW0NVQh|ryP M3O3V3NCVkeHUh?=
YH-13 NE\YSlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fGVGlEPTB;MD6wOVczOiEQvF2= MYHTRW5ITVJ?
5637 M2H0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwMEW3OEDPxE1? M{W0UXNCVkeHUh?=
LOXIMVI Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nyeWlEPTB;MD6wOVg4OiEQvF2= NYfyd4tNW0GQR1XS
GT3TKB NWjGR|FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorKTWM2OD1yLkC1PVQzKM7:TR?= NGq3dmFUSU6JRWK=
TCCSUP MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\LbGlEPTB;MD6wOVk3PCEQvF2= NYHHZ4ZRW0GQR1XS
EPLC-272H NI\QNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwME[yNFUh|ryP Mlq4V2FPT0WU
LU-99A M1PvVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfxRYJpUUN3ME2wMlA3OjN5IN88US=> MYHTRW5ITVJ?
NCI-H1755 NF7rU5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXG4flh5UUN3ME2wMlA3OzRzIN88US=> M1TZXXNCVkeHUh?=
KM12 NYj5SmhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTkeXdvUUN3ME2wMlA3OzR6IN88US=> NYO3ZnQ2W0GQR1XS
SF295 M1HVcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH1UlUyUUN3ME2wMlA3PDV{IN88US=> NX7OUG9OW0GQR1XS
MZ2-MEL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zoVWlEPTB;MD6wOlU2OyEQvF2= MmnzV2FPT0WU
HEC-1 NFvyTJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwME[1PFgh|ryP MkDzV2FPT0WU
SW684 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPCbWZ3UUN3ME2wMlA3PTlzIN88US=> NIG3[2NUSU6JRWK=
SF539 NUniT24{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwME[2PFEh|ryP MmXjV2FPT0WU
GMS-10 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDpNXRZUUN3ME2wMlA3Pjl7IN88US=> M{DqdnNCVkeHUh?=
MV-4-11 NFfmPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fkVWlEPTB;MD6wOlgxOyEQvF2= M3S1TnNCVkeHUh?=
HT-29 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWqzSoNIUUN3ME2wMlA3QTF7IN88US=> MkD4V2FPT0WU
23132-87 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof0TWM2OD1yLkC2PVUh|ryP MWDTRW5ITVJ?
SW620 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojKTWM2OD1yLkC3NFI3KM7:TR?= NV7Cc|RyW0GQR1XS
HCC1806 NUnkZpN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTBwMEexN|Eh|ryP MVjTRW5ITVJ?
Hs-578-T NVTuWGxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISzUlNKSzVyPUCuNFczODhizszN MkHoV2FPT0WU
A2058 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvMXlFKSzVyPUCuNFczOjhizszN NWXXTGVPW0GQR1XS
MEL-HO NUHJZppqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHT5fIFKSzVyPUCuNFczPTVizszN MU\TRW5ITVJ?
HCC2998 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C2fmlEPTB;MD6wO|M1PyEQvF2= MmrQV2FPT0WU
HuO9 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHQRVdHUUN3ME2wMlA4PTh7IN88US=> NIrnR5FUSU6JRWK=
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UACC-893 NY\xZYVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;lb3ZOUUN3ME2wMlY{PjhzIN88US=> Mn[0V2FPT0WU
JVM-3 NEfBPYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHaSndKSzVyPUCuOlM5ODRizszN NHLsd4JUSU6JRWK=
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OCI-AML2 NYjjTI94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;oTWM2OD1yLk[1N|k4KM7:TR?= M1\HTHNCVkeHUh?=
RPMI-8226 NXnFb3dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwNk[zNlMh|ryP NWf0TmpmW0GQR1XS
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MDA-MB-453 MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPETWM2OD1yLk[3NVgh|ryP MYDTRW5ITVJ?
BV-173 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYruVYpxUUN3ME2wMlY5Pjd7IN88US=> M1nsNHNCVkeHUh?=
NCI-H358 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwNki3NlYh|ryP NUjJbGNuW0GQR1XS
NCI-H1651 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TB[WlEPTB;MD63JO69VQ>? NWXLfpZ7W0GQR1XS
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NCI-H522 NUnROnVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjFXlFQUUN3ME2wMlg4Pzh|IN88US=> Mkm2V2FPT0WU
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LU-65 M2DhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwOUK1PVEh|ryP MnSyV2FPT0WU
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MHH-NB-11 NIPC[2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTRwN{W0OlEh|ryP M3W0enNCVkeHUh?=
Calu-3 NVHvTppqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr4TWM2OD12Lke4OVQ5KM7:TR?= M1jwSHNCVkeHUh?=
HT55 Ml3nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jWcGlEPTB;ND64OFU1PSEQvF2= M4f4fnNCVkeHUh?=
SK-N-FI M{HRO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7I[HVKSzVyPUSuPFUxODlizszN M1GzN3NCVkeHUh?=
ES1 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DT[2lEPTB;ND64OlA2PyEQvF2= M4myRXNCVkeHUh?=
SF126 MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPzSpViUUN3ME20Mlk{OTh2IN88US=> MmexV2FPT0WU
ES5 NGnaS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjuSoRKSzVyPUWuNVI1OjdizszN MU\TRW5ITVJ?
LoVo NEm0ToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nGNGlEPTB;NT6xOVg4OSEQvF2= MmnQV2FPT0WU
SNU-387 NGKzXJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrTOZNKSzVyPUWuN|I{OzlizszN NWHUdYt{W0GQR1XS
C8166 NE\hUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G1WmlEPTB;NT6zOlM{QSEQvF2= NFLoUmVUSU6JRWK=
LS-1034 NULRVFZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrkXYJbUUN3ME21MlQzOzB5IN88US=> MX\TRW5ITVJ?
GR-ST MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzEWopKSzVyPUWuOVIzODFizszN M{XObnNCVkeHUh?=
NCI-H1092 M1qzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\4Z2JWUUN3ME21MlczQDR|IN88US=> Mn3SV2FPT0WU
647-V Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnrT4ZKSzVyPUWuO|Q4ODZizszN MoizV2FPT0WU
EW-13 NYPhdIJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3BVHZtUUN3ME21Mlc3PjJ5IN88US=> NIPSNVBUSU6JRWK=
KGN MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jQN2lEPTB;Nj6wPVkzOSEQvF2= M{jmXXNCVkeHUh?=
D-423MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnsZXdKSzVyPU[uOFAzQDRizszN NWraUZFMW0GQR1XS
ECC10 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTdwMUCxNFEh|ryP MmHtV2FPT0WU
TE-5 MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTdwNEGyPVgh|ryP MX\TRW5ITVJ?
P12-ICHIKAWA M{W3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\hTWM2OD15LkS1OVI{KM7:TR?= NVT5SHQ4W0GQR1XS
NCI-H82 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTdwNEW3NFEh|ryP MYLTRW5ITVJ?
NCI-H1993 NF;NZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTdwOEOwOlMh|ryP M3zVW3NCVkeHUh?=
RH-1 MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT4UIFKSzVyPUeuPFUzPDRizszN MXHTRW5ITVJ?
SW948 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTdwOU[wOFkh|ryP Mn\vV2FPT0WU
CAL-33 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTdwOUm5N|gh|ryP NHHyZotUSU6JRWK=
U-266 M1:5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRThwMUW3O|ch|ryP MmnhV2FPT0WU
CAL-72 NWq5[GFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDCTWM2OD16LkKwN|Ih|ryP NHG1TXhUSU6JRWK=
SNU-423 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn5OoVLUUN3ME25MlM3PjZ4IN88US=> NHqyNoZUSU6JRWK=
KG-1 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi0d5VKSzVyPUmuOVg1PTZizszN MUXTRW5ITVJ?
HCC1395 NFvTWohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTMTWM2OD17LkmyN|UzKM7:TR?= NH;OeI9USU6JRWK=
BE-13 NITVbJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHqTWM2OD1zMD64PFkzKM7:TR?= MlnhV2FPT0WU
MKN7 M1jLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPwTWM2OD1zMD65O|Y2KM7:TR?= MYHTRW5ITVJ?
697 M4rLVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHNNWlHUUN3ME2xNU4yPDd{IN88US=> MYnTRW5ITVJ?
LU-135 MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\sRWlEPTB;MUGuNlMxPyEQvF2= NV;NeWlnW0GQR1XS
ES7 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXzfYVKSzVyPUGxMlM{OTNizszN M2T1PHNCVkeHUh?=
SK-HEP-1 NH;zdndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTFzLke2OFYh|ryP MVnTRW5ITVJ?
BEN NXvGbGhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\UTWM2OD1zMT64OVEh|ryP NUTabFF6W0GQR1XS
NCI-H1770 NVvaZXR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjBTWM2OD1zMj6xNlYh|ryP MXrTRW5ITVJ?
SW13 MkjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnUTWM2OD1zMj6xOVQyKM7:TR?= MYfTRW5ITVJ?
MZ1-PC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4myVGlEPTB;MUKuOVQ2OiEQvF2= MnroV2FPT0WU
Mo-T Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyxd5RKSzVyPUGyMlc1OjFizszN NYfaSZZnW0GQR1XS
HLE MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjSTot{UUN3ME2xNk45OjF3IN88US=> MnzHV2FPT0WU
RCC10RGB M1fmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF|Lk[3NUDPxE1? NWHJdng3W0GQR1XS
COLO-320-HSR NUfUUlR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHaTWM2OD1zMz63N|gyKM7:TR?= Ml;qV2FPT0WU
BHT-101 NYPuW4RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF|LkizOFUh|ryP NF3JWolUSU6JRWK=
OCUB-M M{LkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT6TWM2OD1zND6xOlAzKM7:TR?= M4TyUHNCVkeHUh?=
MEG-01 MlPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnETWM2OD1zND6zO|A5KM7:TR?= NFS0WI9USU6JRWK=
RS4-11 NFvY[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmqzTWM2OD1zND63OFIh|ryP NXH0VG5xW0GQR1XS
MN-60 M17icGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTF2Lke4PVQh|ryP Ml7jV2FPT0WU
NCI-H1304 NU[4TG5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:5T2dvUUN3ME2xOU4xPDJ3IN88US=> NIfYNGZUSU6JRWK=
Ramos-2G6-4C10 Mn3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF3LkC1PFEh|ryP MkT6V2FPT0WU
NCI-H2342 M3LzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF3LkKwOFQh|ryP MorNV2FPT0WU
LAN-6 MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjyeXFrUUN3ME2xOU41PDF2IN88US=> MVzTRW5ITVJ?
JVM-2 M4SwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XNXGlEPTB;MUWuOVc1QCEQvF2= NInzRmxUSU6JRWK=
P30-OHK MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\BVXFKSzVyPUG2MlA3OTRizszN MmDyV2FPT0WU
C-33-A NVfi[pFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF4Lk[yNVQh|ryP MmPnV2FPT0WU
RPMI-8866 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTF4Lki0PVYh|ryP M4LqVXNCVkeHUh?=
NCI-H630 MkK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Ky[mlEPTB;MU[uPFU{PyEQvF2= MnzBV2FPT0WU
KYSE-140 NX3rUpJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF5LkKwNlgh|ryP M1XiWHNCVkeHUh?=
T84 MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvJTWM2OD1zOD64Olk2KM7:TR?= NH60NVNUSU6JRWK=
KU-19-19 MmjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUi5UGlHUUN3ME2xPE46PjB6IN88US=> MlLKV2FPT0WU
BALL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF7LkOzPVkh|ryP NFfaR3dUSU6JRWK=
Calu-6 NV[zW2dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTtWY1KSzVyPUG5MlQ6OiEQvF2= NWLWbYFpW0GQR1XS
EGI-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF7LkW5PEDPxE1? MnvIV2FPT0WU
MFH-ino NGftcHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF7Lke0OVQh|ryP Mn71V2FPT0WU
GB-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHnO2dnUUN3ME2yNE4{PTN3IN88US=> NFPHPVFUSU6JRWK=
NCI-H1693 NY\INHNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDaTWM2OD1{MD62OVA2KM7:TR?= NU\RdY0{W0GQR1XS
SW1116 NITibZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrlN49KSzVyPUKwMlk{PjJizszN M4jERnNCVkeHUh?=
H-EMC-SS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPLSVRKSzVyPUKyMlA1PSEQvF2= MmrjV2FPT0WU
D-502MG M2DmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTUUlZKSzVyPUKyMlgzPjFizszN NI\1[JZUSU6JRWK=
IA-LM MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rnXmlEPTB;MkOuNlQ6OyEQvF2= M4XBNXNCVkeHUh?=
SW1463 MkT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7RTWM2OD1{Mz63PUDPxE1? M4XOW3NCVkeHUh?=
JAR MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf5eI5KSzVyPUK0MlMzQTNizszN MVrTRW5ITVJ?
HT MmPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ2LkS3OVMh|ryP M2jBfXNCVkeHUh?=
LCLC-103H M{Oxfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJ2Lki0OFkh|ryP Mo\lV2FPT0WU
SNU-449 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\mT3lKSzVyPUK0Mlg4PDFizszN M3PWOHNCVkeHUh?=
KE-37 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnXWHYyUUN3ME2yOU4xQTJ6IN88US=> M1\kUnNCVkeHUh?=
NCI-H1623 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJ5LkGzNFMh|ryP M{XYRnNCVkeHUh?=
MOLT-13 MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHESYhpUUN3ME2yO{4{PTF4IN88US=> NGnSbGRUSU6JRWK=
COLO-741 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTNzLkOzN|Mh|ryP MXzTRW5ITVJ?
NB6 M4LEUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN{LkK4O|Yh|ryP NGDTcm1USU6JRWK=
MOLT-16 MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7QTpNKSzVyPUOzMlAxPTVizszN MXrTRW5ITVJ?
IST-MES1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTN2LkC1OFEh|ryP M3\FVXNCVkeHUh?=
A4-Fuk NH6x[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN3LkC2OkDPxE1? MmTuV2FPT0WU
CAL-85-1 M4fEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3rNm5KSzVyPUO1MlI5OTdizszN NIPQfIlUSU6JRWK=
CCRF-CEM NEXxOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TMXmlEPTB;M{euNVU{PiEQvF2= MXLTRW5ITVJ?
HAL-01 MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN6LkS4PFkh|ryP MlixV2FPT0WU
HEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\6eWlKSzVyPUSzMlM1ODlizszN NUHycW94W0GQR1XS
EW-1 NHX4NIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJflBXUUN3ME20N{41PzZ6IN88US=> MXLTRW5ITVJ?
MDA-MB-231 NFnvfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCyTWM2OD12NT6xNVk6KM7:TR?= M{TYN3NCVkeHUh?=
ABC-1 M1vvd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn2W4pKSzVyPUS2Mlg2OzhizszN NEXDc5RUSU6JRWK=
NCI-H446 Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;UcGlKSzVyPUS4MlUxPThizszN NGHtPVNUSU6JRWK=
MHH-PREB-1 NFPVUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L4b2lEPTB;NEmuOlAxPyEQvF2= NH;hdXdUSU6JRWK=
DOHH-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPt[IxKSzVyPUS5MlY3PTZizszN NELYOm1USU6JRWK=
GCT NUjFT4dIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rSfmlEPTB;NEmuOlk4PiEQvF2= MoHHV2FPT0WU

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[2]
+ 展開
  • 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.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (170.73 mM)
Ethanol 5 mg/mL (8.53 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5%DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 585.69
化学式

C31H43N3O8

CAS No. 75747-14-7
保管
in solvent
別名 CP127374,NSC-330507, KOS 953

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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
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
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
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

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よくある質問(FAQ)

  • 質問1:

    What kind of subtypes does this compound inhibit? HSP90α or HSP90β ?

  • 回答:

    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)シグナル伝達経路

HSP (e.g. HSP90) Inhibitors with Unique Features

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