Ganetespib (STA-9090) 化学構造
分子量: 364.4

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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 Ganetespib (STA-9090)は独特な triazolone-containing Hsp90阻害剤、 IC50 が4 nM となる.
ターゲット HSP90
IC50 4 nM [1]
In vitro試験 The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. [1] Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. [1] Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. [2] Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. [3] Ganetespib treatment rapidly caused the degradation of known Hsp90 client proteins, exhibits superior potency to the ansamycin inhibitor 17-AAG, and shows sustained activity even with short exposure times.[3] In anohter study, Ganetespib induces apoptosis of malignant canine mast cell lines. Ganetespib is active at significantly lower concentrations for C2 and BR canine malignant mast cells with IC50 of 19 and 4 nM, respectively, while 17-AAG inhibits C2 and BR canine malignant mast cells with IC50 of 958 and 44 nM, respectively. [4] Both the expression of WT and mutant Kit are downregulated by 100 nM Ganetespib after 24 hours in all lines treated including C2 and BMCMCs cells. However, no effects on PI3K or HSP90 expression are observed following treatment with Ganetespib.[4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HL60 NVTlUXJWSXCxcITvd4l{KEG|c3H5 NETHPIM{OC96MD:xOVAwOjVyIH7N MmPnNlQwPDhxN{KgbC=> MmPubY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NUXXNGxOOjV6OEK1OVA>
MV411 M17vfmFxd3C2b4Ppd{BCe3OjeR?= MV6zNE85OC9zNUCvNlUxKG6P MmT6NlQwPDhxN{KgbC=> NWfUXIdDcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MV2yOVg5OjV3MB?=
MGC-803 M4GyOmNmdGxiVnnhZoltcXS7IFHzd4F6 MnXCNE4yNTFyMECgcm0> MoWyO|IhcA>? MWnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3rzeFI2PTlyOEC1
SGC-7901 M17wZWNmdGxiVnnhZoltcXS7IFHzd4F6 NVTFdZY5OC5zLUGwNFAhdk1? M4DwO|czKGh? M4nW[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M2THb|I2PTlyOEC1
MKN-28 NFX2UppE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHnER3gxNjFvMUCwNEBvVQ>? M4XNTlczKGh? M{C2fYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWLkWlNmOjV3OUC4NFU>
MGC-803 NWfFUm9xTnWwY4Tpc44hSXO|YYm= MVewMlEuOTByMDDuUS=> M3;XNVI1KGh? M1:4NIlv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? NVP6doVVOjV3OUC4NFU>
HCT-116 NXqxe2FwTnWwY4Tpc44hSXO|YYm= NXq0N|RIPTCwTR?= NFq4NYQzPCCq NISxbY5FVVOR NVW0c3lwcW6mdXPl[EBIOC:JMTDhdpJme3R? MYeyOVIyODd7NB?=
HT-29 NFuzbohHfW6ldHnvckBCe3OjeR?= M3;OTlUxdk1? MV[yOEBp MoDCSG1UVw>? MnSzbY5lfWOnZDDHNE9IOSCjcoLld5Q> Mkj5NlUzOTB5OUS=
SCC25 M3rFO2N6fG:6aXPpeJkhSXO|YYm= NX3oUGNCOTBxNUCgcm0> NX\MbIFjOjRiaB?= MVXk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MWCyOVIxPTR|MB?=
FUDA Mmf2R5l1d3irY3n0fUBCe3OjeR?= NHu5foEyOC93MDDuUS=> MXSyOEBp MU\k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= Mn;xNlUzODV2M{C=
Detroit562 MmWwR5l1d3irY3n0fUBCe3OjeR?= MV[xNE82OCCwTR?= MlvGNlQhcA>? NIXlNldl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MXSyOVIxPTR|MB?=
CAL27 Ml\vR5l1d3irY3n0fUBCe3OjeR?= NUXl[mVmOTBxNUCgcm0> NYTpTYlyOjRiaB?= NHG5Z4Nl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MXGyOVIxPTR|MB?=
DSH1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHZTWM2OD14IH7N M4nLSlI1Pzh2OEO5
SW-1710 NW\xNJhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXpTWM2OD14IH7N MXWyOFc5PDh|OR?=
T24 M2\iTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorxTWM2OD15IH7N NGfZRXAzPDd6NEizPS=>
RT112 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTlibl2= NYXCOpNyOjR5OES4N|k>
639-V MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPlfIJKSzVyPUGwJI5O M3LFc|I1Pzh2OEO5
SCaBER M2i5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTOWXBsUUN3ME2xNEBvVQ>? NYfoOmJ7OjR5OES4N|k>
BFTC MorwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTIVIVKSzVyPUG3JI5O NVTneJM3OjR5OES4N|k>
J82 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF6IH7N NG\jTnUzPDd6NEizPS=>
HT-1376 NYDhXoZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofDTWM2OD1{MTDuUS=> NH;2[5MzPDd6NEizPS=>
647-V NH\BTpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLVd2hKSzVyPUK3JI5O MljyNlQ4QDR6M{m=
UM-UC3 M2\neWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;admFKSzVyPUOzJI5O M3TF[|I1Pzh2OEO5
LB831-BLC MnGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDRO5hGUUN3ME2zOEBvVQ>? M4rTVVI1Pzh2OEO5
KU-19-19 NIm2[Y5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jSe2lEPTB;M{[gcm0> MUiyOFc5PDh|OR?=
35612 NIDy[YVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN6IH7N MlvxNlQ4QDR6M{m=
5637 NHX5bHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\YXlBZUUN3ME20OEBvVQ>? MkjGNlQ4QDR6M{m=
HT-1197 NXS2bZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPjTlRKSzVyPUWzJI5O NV3ze2xiOjR5OES4N|k>
MGH-U3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXKxO3VSUUN3ME21N{BvVQ>? NGC3RlMzPDd6NEizPS=>
TCCSUP NUPadIkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvZc4tKSzVyPUG0NkBvVQ>? M2DEOVI1Pzh2OEO5
RT4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu4Uo16UUN3ME2xO|M{KG6P MXWyOFc5PDh|OR?=
SW780 NFXBO3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37uWWlEPTB;M{S1NUBvVQ>? NIDXbI4zPDd6NEizPS=>
RKO NFv2S|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1qyOWlEPTB;NDDuUS=> M1O1VFI1Pjh{N{S3
LS-411 N NV3WSlhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPPSYhKSzVyPUWgcm0> M1i4cFI1Pjh{N{S3
SW620 NEfEPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRThibl2= Mk\5NlQ3QDJ5NEe=
HCT-15 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRThibl2= M37sblI1Pjh{N{S3
HuTu-80 M{PRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjwWJlKSzVyPUGzJI5O M2r2dVI1Pjh{N{S3
HCT 116 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTFTWM2OD1zNDDuUS=> MV[yOFY5Ojd2Nx?=
COLO-205 M1XrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLvTWM2OD1zNDDuUS=> MXKyOFY5Ojd2Nx?=
NCI-H747 NYe4fFhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jteWlEPTB;MUegcm0> NXvFdWhtOjR4OEK3OFc>
COLO-678 NUH0XWpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;4V2lEPTB;MkGgcm0> NUjTXVNkOjR4OEK3OFc>
LoVo M{[zWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDQ[ohwUUN3ME2yNkBvVQ>? NIHERpEzPDZ6Mke0Oy=>
LS-1034 NY\DeoRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITGSGlKSzVyPUOxJI5O M2r5[|I1Pjh{N{S3
SNU-C2B NWf4NnNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUSzNZVCUUN3ME20OUBvVQ>? M4XkZVI1Pjh{N{S3
LS-123 NGn2bWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nJZ2lEPTB;N{Ogcm0> NF;5enMzPDZ6Mke0Oy=>
SK-CO-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRThzIH7N NITNTlUzPDZ6Mke0Oy=>
HCC2998 NVHnZVlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF6wVVNKSzVyPUGyPEBvVQ>? M3PIN|I1Pjh{N{S3
MDA-MB-231 MV;GeY5kfGmxbjDBd5NigQ>? M2XOSlExOCCwTR?= NGnCbHA{OCCvaX6= MXzpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MlK5NlQzPDh{NkW=
MDA-MB-435 NY\sOVdYTnWwY4Tpc44hSXO|YYm= M1XWPVExOCCwTR?= MVqzNEBucW5? MWfpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? M3;2SVI1OjR6Mk[1
BT-20  MkO3SpVv[3Srb36gRZN{[Xl? NXX6bXl6OTByL{K1NEBvVQ>? NYD3[ndYOjRiaB?= NXfxbWVkemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI Mlq1NlQyPzN3NEG=
MDA-MB-231 MVfGeY5kfGmxbjDBd5NigQ>? Mk\ONVAxKG6P MVeyOEBp MoTybY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> M2LxbFI1OTd|NUSx
H82 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HkTWlEPTB;M{CuNlchdk1? M1ezelI1OTZ4NUC1
GLC4 M3;OXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;EbmVKSzVyPUKwMlQ4KG6P MlXUNlQyPjZ3MEW=
H69 NEfIVnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\ze21SUUN3ME24N{4{PiCwTR?= MmnWNlQyPjZ3MEW=
H128 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\1TWM2OD14OT61OUBvVQ>? NF6yO|EzPDF4NkWwOS=>
H146 M1freGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XnNGlEPTB;MkiuOVEhdk1? NWDLOWRFOjRzNk[1NFU>
H187 M4m2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Xsd2lEPTB;MkSuPVkhdk1? NETXSWIzPDF4NkWwOS=>
H526 NXHhNYc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGe3VJBKSzVyPUKxMlY1KG6P NVT0NmRsOjRzNk[1NFU>
N592 NXruR4trT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF2LkGyJI5O MXuyOFE3PjVyNR?=
H620 NYH6Rml4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTN{Lk[3JI5O NYfvN4N5OjRzNk[1NFU>
H792 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnmTZpRUUN3ME20OU4xPyCwTR?= MorGNlQyPjZ3MEW=
H1173 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfNTWM2OD1zMj62NkBvVQ>? MlLmNlQyPjZ3MEW=
AC3 NFPZTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm2TWM2OD1{NT65JI5O NIDIW3MzPDF4NkWwOS=>
H82 NUXBdWxETnWwY4Tpc44hSXO|YYm= MV:zNEBvVQ>? M1XDPVczKGh? MoW0bY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 M2\xVFI1OTZ4NUC1
GLC4 MWnGeY5kfGmxbjDBd5NigQ>? M3npOlMxKG6P MmXSO|IhcA>? MmK0bY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MW[yOFE3PjVyNR?=
H146  Mo[1SpVv[3Srb36gRZN{[Xl? M2f6VFMxKG6P NVnuWVl5PzJiaB?= NIryXHFqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NE\XcGkzPDF4NkWwOS=>
OVCAR-5 M3T0XGNmdGxiVnnhZoltcXS7IFHzd4F6 MYOwMVExODBibl2= MVK3NkBp MmXXbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXqyN|kxODF|Nh?=
OVCAR-8 MlLlR4VtdCCYaXHibYxqfHliQYPzZZk> M3O2RVAuOTByMDDuUS=> NWLXT|JwPzJiaB?= MYrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2LqclI{QTByMUO2
A1847 NG\QRWJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXnqPHZkOC1zMECwJI5O MX63NkBp MkT0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3KxSVI{QTByMUO2
SKOV-3 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1fOT|AuOTByMDDuUS=> MX[3NkBp NWjCT2lXcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEnhZWMzOzlyMEGzOi=>
OVCAR-5 NHvLbIpCeG:ydH;zbZMhSXO|YYm= NXn3WYZEOTBvMUCwJI5O MV2yOE81QC95MjDo NITl[I9qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M2LBbVI{QTByMUO2
OVCAR-8 M1vFbWFxd3C2b4Ppd{BCe3OjeR?= MUOxNE0yODBibl2= MVmyOE81QC95MjDo M1S0fYlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MX2yN|kxODF|Nh?=
A1847 MWXBdI9xfG:|aYOgRZN{[Xl? NHjYWlEyOC1zMECgcm0> MoHsNlQwPDhxN{KgbC=> NVzqWINwcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MmLNNlM6ODBzM{[=
H2228 Mln4R4VtdCCYaXHibYxqfHliQYPzZZk> MVWwMVExODBibl2= NVK0RW5GPzJiaB?= MlLWTWM2OD1zMzDuUS=> MWSyN|U{OzJ4NR?=
H3122 Mn7hR4VtdCCYaXHibYxqfHliQYPzZZk> M4TOVVAuOTByMDDuUS=> NY[2WYVRPzJiaB?= NF7vS4FKSzVyPUGwJI5O MYGyN|U{OzJ4NR?=
K008 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWXJR|UxRTZyIH7N Mmn4NlM1OTh3MkO=
K028 MnHwR4VtdCCYaXHibYxqfHliQYPzZZk> MVnJR|UxRTh2IH7N M{TzXFI{PDF6NUKz
K029 Mkn4R4VtdCCYaXHibYxqfHliQYPzZZk> NWDsV3Z[UUN3ME20OkBvVQ>? NHvjdVkzOzRzOEWyNy=>
M23 NFnzUIRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFnSWFdKSzVyPUO3MlUhdk1? MWiyN|QyQDV{Mx?=
K033 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYTJR|UxRTd3LkWgcm0> NUW5THhxOjN2MUi1NlM>
K008 M1K2[mZ2dmO2aX;uJGF{e2G7 NWTudHBkOjVyIH7N NVTEUYxlOjRiaB?= MVjpcoR2[2W|IFeyJIFzemW|dB?= MmnDNlM1OTh3MkO=
K028 NX7jd3FETnWwY4Tpc44hSXO|YYm= MnHrNlUxKG6P NGjKWI8zPCCq NHX6ephqdmS3Y3XzJGczKGG{cnXzeC=> NVnXcWlzOjN2MUi1NlM>
K029 Ml7FSpVv[3Srb36gRZN{[Xl? MYqyOVAhdk1? NX73TGpYOjRiaB?= MVrpcoR2[2W|IFexJIFzemW|dB?= MXiyN|QyQDV{Mx?=
M23 MUHGeY5kfGmxbjDBd5NigQ>? NFrxeJgzPTBibl2= MmnTNlQhcA>? MYnpcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= NV3F[FZvOjN2MUi1NlM>
K033 Mn7kSpVv[3Srb36gRZN{[Xl? Mm\0NlUxKG6P MmfTNlQhcA>? NGfLfGhqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36= NGXjbVkzOzRzOEWyNy=>
K008 M1XpTGFxd3C2b4Ppd{BCe3OjeR?= MmX4NVAxKG6P NWLwWlE2PzJiaB?= M4rwU5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M{DyOVI{PDF6NUKz
K028 NHzNdoJCeG:ydH;zbZMhSXO|YYm= MmexNVAxKG6P MoDQO|IhcA>? MmP5d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M3zKUVI{PDF6NUKz
K029 NYW4W4FESXCxcITvd4l{KEG|c3H5 MnXQNVAxKG6P M1zEV|czKGh? MlnWd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MUOyN|QyQDV{Mx?=
M23 NWSzbXdVSXCxcITvd4l{KEG|c3H5 NWTHclFvOTByIH7N NIXPT2g4OiCq MmDZd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MkLjNlM1OTh3MkO=
K033 MlKxRZBweHSxc3nzJGF{e2G7 NHPZc4cyODBibl2= MWm3NkBp MYjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M1;LOFI{PDF6NUKz
RD NH7zeHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRThibl2= NH;5PVUzOzNyM{e0NS=>
Rh41 MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPWTWM2OD1zMD60JI5O MUmyN|MxOzd2MR?=
Rh18 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTZVXpKSzVyPU[uNkBvVQ>? MnO5NlM{ODN5NEG=
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BT-12 NFXIdIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nqXWlEPTB;MUSuN{BvVQ>? NIfEPFMzOzNyM{e0NS=>
CHLA-266 NUjX[3psT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jPVWlEPTB;MkeuNUBvVQ>? NUfhOJFkOjN|MEO3OFE>
TC-71 NEXYfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXjXGh3UUN3ME20MlUhdk1? MVGyN|MxOzd2MR?=
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CHLA-10 M2TBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTVwNzDuUS=> MWCyN|MxOzd2MR?=
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SJ-GBM2 M2fMUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXhTWM2OD1zMj65JI5O MVGyN|MxOzd2MR?=
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CHLA-136 NXrjWmt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDQVppKSzVyPUKzMlIhdk1? NX;ufo5nOjN|MEO3OFE>
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RS4;11 MknmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17Kd2lEPTB;MUOuOUBvVQ>? NIrObW0zOzNyM{e0NS=>
MOLT-4 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;6eoduUUN3ME2xNE43KG6P NH3UbYozOzNyM{e0NS=>
CCRF-CEM (1) MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;TbFFKSzVyPUGyMlUhdk1? M4ri[|I{OzB|N{Sx
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Kasumi-1 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnuS2g4UUN3ME21Mlghdk1? MUeyN|MxOzd2MR?=
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Ramos-RA1 NXe0R5VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTdwNDDuUS=> M1vkXlI{OzB|N{Sx
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H1355 NGW3U|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXjSpFbUUN3ME21JI5O MoT3NlMxOTJ{NEi=
H157 NHzlVlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrVcm9KSzVyPUegcm0> NFjDXFMzOzBzMkK0PC=>
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IA-LM NETNV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm0WHREUUN3ME2xNEBvVQ>? MUWyN|AyOjJ2OB?=
HOP-62 Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPhZZNKSzVyPUGxJI5O M1Lh[FI{ODF{MkS4
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NCI-H1975 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fjV|czKGh? M4TrOWlEPTB;ODDuUS=> MVWyNlE1PDZ4NR?=

... Click to View More Cell Line Experimental Data

In vivo試験 Administration of Ganetespib leads to significant tumor shrinkage in several tumor xenograft models in mice and appears to be less toxic. Furthermore Ganetespib demonstrated better tumor penetration compared with tanespimycin.[2] Ganetespib inhibits in vivo tumor growth in both malignant mast cell and OSA xenograft models. Ganetespib significantly inhibits tumor growth when dosed with two repeating cycles of 25 mg/kg/day for 3 days, with a %T/C value of 18. Ganetespib is well-tolerated, with the vehicle and Ganetespib groups having average bodyweight changes relative to the start of the study of +0.3% and -8.1% on day 17, respectively.[4]
臨床試験 Ganetespib has entered in a phase II clinical trials in the treatment of non small cell lung cancer.
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 OSA cells
濃度 0.001-1μM
反応時間 5 days
実験の流れ A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.

動物実験: [4]

動物モデル Female severe combined immune-deficient (SCID) mice
製剤 In DMSO and diluted 1:10 with 20% Cremophor RH 40
投薬量 25 mg/kg/day for 3 days
投与方法 Tail vein injection

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 Ganetespib (STA-9090) SDF
分子量 364.4
化学式

C20H20N4O3

CAS No. 888216-25-9
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+45% PEG 300+ddH2O 11mg/mL
* <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 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one

文献中の引用 (6)

Frequently Asked Questions

  • Question 1
    Does this inhibitor inhibit both isoforms of HSP90?

    Answer: We don't have the information now and it is not very clear in the literature either. From following two references, it indicates that Ganetespib might be specific to the alpha form “Ganetespib binds to the ATP binding site of Hsp90 alpha with a Kd of 110 nM” http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3477583/

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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* 必須

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は1種のパン(pan)- HSP 阻害剤で、誘導HSPsの合成(HSP105、 HSP72,と HSP40を含める)を抑制します。

  • 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.

  • Tanespimycin (17-AAG)

    Tanespimycin (17-AAG)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。

    Features:Displays very low toxicity toward normal cells.

  • 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。

  • Alvespimycin (17-DMAG) HCl

    Alvespimycin (17-DMAG) 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

    Geldanamycinは一種の天然なHSP90阻害剤で、Kd値が1.2μMですが、糖質ステロイド受容体(GR)/HSP連合を特異性的に妨害します。

  • 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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