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 MoO1RZBweHSxc3nzJGF{e2G7 MkTTN|AwQDBxMUWwM|I2OCCwTR?= MU[yOE81QC95MjDo M3;jc4lv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> MojaNlU5QDJ3NUC=
MV411 M3fuRWFxd3C2b4Ppd{BCe3OjeR?= NVzmRWdwOzBxOECvNVUxNzJ3MDDuUS=> MlLCNlQwPDhxN{KgbC=> NV7abItncW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MXeyOVg5OjV3MB?=
MGC-803 MlHmR4VtdCCYaXHibYxqfHliQYPzZZk> MlfhNE4yNTFyMECgcm0> M4D3N|czKGh? MVzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MViyOVU6ODhyNR?=
SGC-7901 NH21WndE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWX0WVBEOC5zLUGwNFAhdk1? NXTJd4lwPzJiaB?= M3PLeYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NEnSTYQzPTV7MEiwOS=>
MKN-28 M{LvZmNmdGxiVnnhZoltcXS7IFHzd4F6 MXKwMlEuOTByMDDuUS=> NGH2Xm04OiCq MnPKbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXiyOVU6ODhyNR?=
MGC-803 NEToZWJHfW6ldHnvckBCe3OjeR?= NYC0dIw3OC5zLUGwNFAhdk1? Mnn0NlQhcA>? MVzpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> NEG4dlgzPTV7MEiwOS=>
HCT-116 NWfjdVJkTnWwY4Tpc44hSXO|YYm= Mn21OVBvVQ>? MUCyOEBp MoDUSG1UVw>? NXWycGlDcW6mdXPl[EBIOC:JMTDhdpJme3R? MmrPNlUzOTB5OUS=
HT-29 M174eGZ2dmO2aX;uJGF{e2G7 M4HHV|Uxdk1? MXWyOEBp MUHEUXNQ NY\MbFNEcW6mdXPl[EBIOC:JMTDhdpJme3R? MV:yOVIyODd7NB?=
SCC25 MYjDfZRwgGmlaYT5JGF{e2G7 NX6zPZNpOTBxNUCgcm0> NWnBcYJxOjRiaB?= Mn\i[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M1X6e|I2OjB3NEOw
FUDA M1;Fe2N6fG:6aXPpeJkhSXO|YYm= MkHXNVAwPTBibl2= NUDJPINCOjRiaB?= NVznXpJU\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MoDyNlUzODV2M{C=
Detroit562 MXzDfZRwgGmlaYT5JGF{e2G7 MojPNVAwPTBibl2= MUKyOEBp NFLmZ4Nl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NYLpOIg1OjV{MEW0N|A>
CAL27 NHHRV3VEgXSxeHnjbZR6KEG|c3H5 NIC4fWEyOC93MDDuUS=> NXq1XYtsOjRiaB?= MVnk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NFH1W3YzPTJyNUSzNC=>
DSH1 NIPZWnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnS[GpsUUN3ME22JI5O NFuwbokzPDd6NEizPS=>
SW-1710 MnTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrwZYZoUUN3ME22JI5O M{XpN|I1Pzh2OEO5
T24 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;UWHZoUUN3ME23JI5O NUfvepVUOjR5OES4N|k>
RT112 NGXDWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LJb2lEPTB;OTDuUS=> NH7qb2czPDd6NEizPS=>
639-V Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H4[mlEPTB;MUCgcm0> M3r2dlI1Pzh2OEO5
SCaBER M1zmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPRd5B3UUN3ME2xNEBvVQ>? MknLNlQ4QDR6M{m=
BFTC MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHzTWM2OD1zNzDuUS=> MVyyOFc5PDh|OR?=
J82 NGXEfY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF6IH7N NVjMdpZ7OjR5OES4N|k>
HT-1376 MknRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13M[2lEPTB;MkGgcm0> Mkf3NlQ4QDR6M{m=
647-V MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzmbZhkUUN3ME2yO{BvVQ>? NGPabI8zPDd6NEizPS=>
UM-UC3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LqTmlEPTB;M{Ogcm0> M4fp[FI1Pzh2OEO5
LB831-BLC NYi5cHdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK3TWM2OD1|NDDuUS=> MUCyOFc5PDh|OR?=
KU-19-19 M{\oRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHWTWM2OD1|NjDuUS=> MknHNlQ4QDR6M{m=
35612 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN6IH7N NWjLcGJJOjR5OES4N|k>
5637 NV\teI14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR2IH7N NG\od2czPDd6NEizPS=>
HT-1197 NUXYR5NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK5cZBKSzVyPUWzJI5O M1nNRlI1Pzh2OEO5
MGH-U3 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTV|IH7N Ml3BNlQ4QDR6M{m=
TCCSUP NHfjbFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrxV5dKUUN3ME2xOFIhdk1? NHHQTlgzPDd6NEizPS=>
RT4 NHrTNnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjhTmxKSzVyPUG3N|Mhdk1? Mn\KNlQ4QDR6M{m=
SW780 NE\veoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDoTWM2OD1|NEWxJI5O NUDmWWpJOjR5OES4N|k>
RKO NXficZNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrQW|YxUUN3ME20JI5O MlvSNlQ3QDJ5NEe=
LS-411 N M1nr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTVibl2= NGjscpQzPDZ6Mke0Oy=>
SW620 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\PUWtXUUN3ME24JI5O NUKxdJZPOjR4OEK3OFc>
HCT-15 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnewTWM2OD16IH7N M1jnc|I1Pjh{N{S3
HuTu-80 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF|IH7N NEjTfZozPDZ6Mke0Oy=>
HCT 116 NETkbJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXHTWM2OD1zNDDuUS=> NED3WFIzPDZ6Mke0Oy=>
COLO-205 Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TWfmlEPTB;MUSgcm0> MV[yOFY5Ojd2Nx?=
NCI-H747 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D1U2lEPTB;MUegcm0> M1nUTlI1Pjh{N{S3
COLO-678 MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC1RXBKSzVyPUKxJI5O NFTLTYQzPDZ6Mke0Oy=>
LoVo MoPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTzdGhKSzVyPUKyJI5O M1HyUlI1Pjh{N{S3
LS-1034 M4PJZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3YV2JGUUN3ME2zNUBvVQ>? NFfVeoEzPDZ6Mke0Oy=>
SNU-C2B NEfEcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTR3IH7N NHfmV4QzPDZ6Mke0Oy=>
LS-123 NFjs[ndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\M[nZ6UUN3ME23N{BvVQ>? MXmyOFY5Ojd2Nx?=
SK-CO-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\WZ2xKSzVyPUixJI5O MWCyOFY5Ojd2Nx?=
HCC2998 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MormTWM2OD1zMkigcm0> NX[z[2R5OjR4OEK3OFc>
MDA-MB-231 MXjGeY5kfGmxbjDBd5NigQ>? NWH0Zpp5OTByIH7N NHfLXY4{OCCvaX6= NGC2[JJqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= MVuyOFI1QDJ4NR?=
MDA-MB-435 MnjmSpVv[3Srb36gRZN{[Xl? MV:xNFAhdk1? MoDYN|AhdWmw NIfERWpqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= MViyOFI1QDJ4NR?=
BT-20  NI\ONWNHfW6ldHnvckBCe3OjeR?= NUTLNJlVOTByL{K1NEBvVQ>? MYCyOEBp NVK5To1jemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI NWLIW25LOjRzN{O1OFE>
MDA-MB-231 M4TCd2Z2dmO2aX;uJGF{e2G7 NXHMfIk1OTByIH7N NXPsOHVxOjRiaB?= NHvXNFZqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh M{XCTFI1OTd|NUSx
H82 M2r5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXmTWM2OD1|MD6yO{BvVQ>? M3vKU|I1OTZ4NUC1
GLC4 M4PLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJyLkS3JI5O MXyyOFE3PjVyNR?=
H69 M1LpZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTh|LkO2JI5O NXvCWGRDOjRzNk[1NFU>
H128 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTZ7LkW1JI5O M3zPSFI1OTZ4NUC1
H146 NGP3OnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfrVoNSUUN3ME2yPE42OSCwTR?= Mn;XNlQyPjZ3MEW=
H187 NYqxOGFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjUZ3ZmUUN3ME2yOE46QSCwTR?= NFm5TJczPDF4NkWwOS=>
H526 NXzFeGdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLIclRuUUN3ME2yNU43PCCwTR?= NHXGS5EzPDF4NkWwOS=>
N592 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF2LkGyJI5O Mo\WNlQyPjZ3MEW=
H620 MkXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXpTWpKSzVyPUOyMlY4KG6P MX:yOFE3PjVyNR?=
H792 M2rhcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zzTmlEPTB;NEWuNFchdk1? NXv6NoxUOjRzNk[1NFU>
H1173 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33acWlEPTB;MUKuOlIhdk1? NVjTOZdrOjRzNk[1NFU>
AC3 NVHycXh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ3Lkmgcm0> M4LueFI1OTZ4NUC1
H82 MonaSpVv[3Srb36gRZN{[Xl? M4\tcVMxKG6P NGLuU|A4OiCq MlvjbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 M4DpT|I1OTZ4NUC1
GLC4 NV\GVoh6TnWwY4Tpc44hSXO|YYm= MV:zNEBvVQ>? Mn;RO|IhcA>? NV3mOm9pcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 MXWyOFE3PjVyNR?=
H146  MYLGeY5kfGmxbjDBd5NigQ>? NH\YcIo{OCCwTR?= NFW3THM4OiCq NYS2c5hocW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NXzLUGd6OjRzNk[1NFU>
OVCAR-5 NGn2WWxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX3LR3p6OC1zMECwJI5O MYC3NkBp MV;pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mk[wNlM6ODBzM{[=
OVCAR-8 NGHrVGdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWL3eWRIOC1zMECwJI5O MmKyO|IhcA>? M1THbYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M3GzeFI{QTByMUO2
A1847 NVzsN3RTS2WubDDWbYFjcWyrdImgRZN{[Xl? M3TKW|AuOTByMDDuUS=> NIT1cmE4OiCq NUnhcIdVcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NI\pXmkzOzlyMEGzOi=>
SKOV-3 M4e4U2NmdGxiVnnhZoltcXS7IFHzd4F6 NE\VR3kxNTFyMECgcm0> MofNO|IhcA>? NXvNUI52cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MUSyN|kxODF|Nh?=
OVCAR-5 MVrBdI9xfG:|aYOgRZN{[Xl? NXnI[Wl{OTBvMUCwJI5O NHrQN4gzPC92OD:3NkBp NFfOdlBqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NVX2eYF2OjN7MECxN|Y>
OVCAR-8 NFLCeGRCeG:ydH;zbZMhSXO|YYm= NIPnfHoyOC1zMECgcm0> NYTVfm1uOjRxNEivO|IhcA>? MlT4bY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NIHtNFczOzlyMEGzOi=>
A1847 M2Lmb2Fxd3C2b4Ppd{BCe3OjeR?= MX:xNE0yODBibl2= MV6yOE81QC95MjDo NV;VZpZLcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NYfOe4c1OjN7MECxN|Y>
H2228 MoTWR4VtdCCYaXHibYxqfHliQYPzZZk> MoXiNE0yODByIH7N NELO[XM4OiCq NFnEO5RKSzVyPUGzJI5O NUnsb3VYOjN3M{OyOlU>
H3122 NW\VTlJ4S2WubDDWbYFjcWyrdImgRZN{[Xl? NVroNVdTOC1zMECwJI5O NFPBVWM4OiCq NVTFd2xOUUN3ME2xNEBvVQ>? NUixRXR4OjN3M{OyOlU>
K008 NFm0N4RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MonKTWM2OD14MDDuUS=> NF\qeYczOzRzOEWyNy=>
K028 MmTSR4VtdCCYaXHibYxqfHliQYPzZZk> M3\oZWlEPTB;OESgcm0> M3rXdFI{PDF6NUKz
K029 M37wVWNmdGxiVnnhZoltcXS7IFHzd4F6 MWDJR|UxRTR4IH7N MVqyN|QyQDV{Mx?=
M23 M{L1VGNmdGxiVnnhZoltcXS7IFHzd4F6 M1m0SGlEPTB;M{euOUBvVQ>? NF;QbGszOzRzOEWyNy=>
K033 NUi0dXV1S2WubDDWbYFjcWyrdImgRZN{[Xl? NX2w[m11UUN3ME23OU42KG6P MUiyN|QyQDV{Mx?=
K008 MYHGeY5kfGmxbjDBd5NigQ>? NYrJbHp2OjVyIH7N NHrwVIkzPCCq MXLpcoR2[2W|IFeyJIFzemW|dB?= MmTMNlM1OTh3MkO=
K028 NV7PdW1kTnWwY4Tpc44hSXO|YYm= MUeyOVAhdk1? NYriVpVJOjRiaB?= MkXNbY5lfWOnczDHNkBienKnc4S= NWniXHFwOjN2MUi1NlM>
K029 Mof4SpVv[3Srb36gRZN{[Xl? M{Ph[VI2OCCwTR?= MmjTNlQhcA>? MlnDbY5lfWOnczDHNUBienKnc4S= M{fEVVI{PDF6NUKz
M23 NYfQNFR7TnWwY4Tpc44hSXO|YYm= M13OSlI2OCCwTR?= M3\xbVI1KGh? Mn65bY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= M2LWXVI{PDF6NUKz
K033 MXzGeY5kfGmxbjDBd5NigQ>? MVSyOVAhdk1? M3T0SFI1KGh? MmG0bY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NUC3TpcyOjN2MUi1NlM>
K008 MVjBdI9xfG:|aYOgRZN{[Xl? MmTxNVAxKG6P NYXk[HhyPzJiaB?= NFLaXWp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NIW4Z20zOzRzOEWyNy=>
K028 M3jCXWFxd3C2b4Ppd{BCe3OjeR?= NUfvbIgxOTByIH7N M1r0fFczKGh? MmLYd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MnK1NlM1OTh3MkO=
K029 NGfvPItCeG:ydH;zbZMhSXO|YYm= MkXRNVAxKG6P MneyO|IhcA>? NIjh[4Z{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NF22WI8zOzRzOEWyNy=>
M23 NWLw[2Y5SXCxcITvd4l{KEG|c3H5 M3TSWFExOCCwTR?= NFmxVWQ4OiCq MmHWd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M1XYSFI{PDF6NUKz
K033 Mle1RZBweHSxc3nzJGF{e2G7 Mlv5NVAxKG6P NFTWdXY4OiCq Mk\Qd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MUGyN|QyQDV{Mx?=
RD Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRThibl2= NYH6b2dJOjN|MEO3OFE>
Rh41 NFS5cmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\aTWM2OD1zMD60JI5O M3q2TFI{OzB|N{Sx
Rh18 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknzTWM2OD14LkKgcm0> NF3tOWszOzNyM{e0NS=>
Rh30 NVnzN|Q2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoOyTWM2OD13Lk[gcm0> M13XV|I{OzB|N{Sx
BT-12 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTHeXlSUUN3ME2xOE4{KG6P NInsSnUzOzNyM{e0NS=>
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TC-71 NFPSTmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTRwNTDuUS=> M1PxWVI{OzB|N{Sx
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CHLA-10 NY\xXG9rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGwTWM2OD13Lkegcm0> NYrE[oh3OjN|MEO3OFE>
CHLA-258 NIKxUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTZwNDDuUS=> M3rGNlI{OzB|N{Sx
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H2212 M4H1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK4TJRJUUN3ME2xO{BvVQ>? MlfRNlMxOTJ{NEi=
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H2009 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonETWM2OD1zOTDuUS=> MnTpNlMxOTJ{NEi=
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COR-L23 NUXD[JdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ{IH7N M2HnXVI{ODF{MkS4
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... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/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

カスタマーフィードバック (2)


Click to enlarge
Rating
Source Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1017. Ganetespib (STA-9090) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231, SKM1, PaTu2, A549, HCT-116 cells
Concentrations 0-1.0 uM
Incubation Time 24 h
Results To investigate whether PRKD2 stability is affected after pharmacologic HSP90 inhibition, eight human cancer cell lines representing six different tumor types (breast cancer, pancreatic cancer, lung cancer, colon cancer, acutemyeloid leukemia, and glioblastoma) were incubated for 24 hours with increasing concentrations of two different compounds: PU-H71, an optimized water soluble member of the purine class of HSP90 inhibitors and STA-9090, a resor-cinol-containing triazole molecule with a novel chemical structure, both unrelated to the geldanamycin class of HSP90 inhibitors. Both inhibitors caused dose-dependent degradation of PRKD2 in all tumor cell lines. STA-9090 was associated with increased apoptosis as revealed by augmented PARP and caspase-9 cleavage in all tumor cell lines.

Click to enlarge
Rating
Source , , Hum Mol Genet, 2015, 10.1093/hmg/ddv136. Ganetespib (STA-9090) purchased from Selleck
Method Western Blot
Cell Lines Pkd1 null MEK cells、Pkd1 mutant PN24 cells
Concentrations 0-200 nM
Incubation Time 0-24 h
Results Treatment with STA9090, a second generation Hsp90 inhibitor that binds to ATP binding domain at the N-terminal of Hsp90, decreased the levels of Brd4 protein in Pkd1 mutant MEK cells and PN24 cells in a dose- and time-dependent manner.

文献中の引用 (5)

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.

  • 17-AAG (Tanespimycin)

    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。

    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。

  • 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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