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 NXvpfoprSXCxcITvd4l{KEG|c3H5 NYfjU|lqOzBxOECvNVUxNzJ3MDDuUS=> MWqyOE81QC95MjDo MUDpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= MV[yOVg5OjV3MB?=
MV411 MVnBdI9xfG:|aYOgRZN{[Xl? NFnGV24{OC96MD:xOVAwOjVyIH7N M37zTVI1NzR6L{eyJIg> MlfBbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NFznPYQzPTh6MkW1NC=>
MGC-803 MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYKwMlEuOTByMDDuUS=> NULTSlFsPzJiaB?= MYPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NIfoOW4zPTV7MEiwOS=>
SGC-7901 M{H2TmNmdGxiVnnhZoltcXS7IFHzd4F6 M1W0[VAvOS1zMECwJI5O MYW3NkBp NIjLSmRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2n4WFI2PTlyOEC1
MKN-28 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVziOZRZOC5zLUGwNFAhdk1? MVm3NkBp MU\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmfYNlU2QTB6MEW=
MGC-803 M33qTGZ2dmO2aX;uJGF{e2G7 Mn;QNE4yNTFyMECgcm0> MoK3NlQhcA>? NV:5e|VzcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NWn6Wo0zOjV3OUC4NFU>
HCT-116 NWWzRVI3TnWwY4Tpc44hSXO|YYm= NHSyVVM2OG6P NF7RVmwzPCCq M4XaR2ROW09? M2TYeIlv\HWlZXSgS|AwTzFiYYLy[ZN1 NH\SfYYzPTJzMEe5OC=>
HT-29 M1zmfmZ2dmO2aX;uJGF{e2G7 NU\tR2oxPTCwTR?= Mnq2NlQhcA>? MVzEUXNQ NWWycXoxcW6mdXPl[EBIOC:JMTDhdpJme3R? M3HIeFI2OjFyN{m0
SCC25 NEizcllEgXSxeHnjbZR6KEG|c3H5 NYDOPWdEOTBxNUCgcm0> MkjxNlQhcA>? NWfVeGJE\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NHnHUFYzPTJyNUSzNC=>
FUDA M4LTW2N6fG:6aXPpeJkhSXO|YYm= NV;Cc|dwOTBxNUCgcm0> MmP3NlQhcA>? MlXt[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MUiyOVIxPTR|MB?=
Detroit562 MljvR5l1d3irY3n0fUBCe3OjeR?= MY[xNE82OCCwTR?= NVXFW|VMOjRiaB?= M2TNS4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NU[yTWxtOjV{MEW0N|A>
CAL27 NWW2Tm9VS3m2b4jpZ4l1gSCDc4PhfS=> NITPTVIyOC93MDDuUS=> M1[2XFI1KGh? NYK1e2I6\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NH;BZmIzPTJyNUSzNC=>
DSH1 Mn;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyzSJIxUUN3ME22JI5O NE\wOHozPDd6NEizPS=>
SW-1710 M{jRVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7VTWM2OD14IH7N MoPzNlQ4QDR6M{m=
T24 NEj6SlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm1bGVKSzVyPUegcm0> NWnGbXoxOjR5OES4N|k>
RT112 NVXHemc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTlibl2= NULUUlhVOjR5OES4N|k>
639-V NHXieXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjF[nhKSzVyPUGwJI5O M{HOclI1Pzh2OEO5
SCaBER M2\ufWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFyIH7N MlnXNlQ4QDR6M{m=
BFTC MmH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTkVG11UUN3ME2xO{BvVQ>? NVS3NVNPOjR5OES4N|k>
J82 NVS5bFd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF6IH7N MljWNlQ4QDR6M{m=
HT-1376 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrnTWM2OD1{MTDuUS=> M3TKV|I1Pzh2OEO5
647-V NHjQSnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfSV2ZKSzVyPUK3JI5O NIfMSFMzPDd6NEizPS=>
UM-UC3 M{jXXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi0UnZKSzVyPUOzJI5O MYiyOFc5PDh|OR?=
LB831-BLC NXvCdW15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPFVXVKSzVyPUO0JI5O MmDmNlQ4QDR6M{m=
KU-19-19 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLJR|c1UUN3ME2zOkBvVQ>? NIHGbmQzPDd6NEizPS=>
35612 NVzNOodOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTN6IH7N MVGyOFc5PDh|OR?=
5637 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\5NmtvUUN3ME20OEBvVQ>? NF20XZczPDd6NEizPS=>
HT-1197 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTkfnRKSzVyPUWzJI5O M{\WOFI1Pzh2OEO5
MGH-U3 NGfve2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrNWxPUUN3ME21N{BvVQ>? MYWyOFc5PDh|OR?=
TCCSUP MnzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYqydJl5UUN3ME2xOFIhdk1? NV\LdVJ6OjR5OES4N|k>
RT4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXjTWM2OD1zN{OzJI5O NV;kRmRMOjR5OES4N|k>
SW780 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnI[Yp4UUN3ME2zOFUyKG6P MXiyOFc5PDh|OR?=
RKO NID6eVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWGyT|F4UUN3ME20JI5O NGi0WmQzPDZ6Mke0Oy=>
LS-411 N MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTVibl2= NF:4VW4zPDZ6Mke0Oy=>
SW620 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPDTWM2OD16IH7N MnLXNlQ3QDJ5NEe=
HCT-15 M3izTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrJWWs5UUN3ME24JI5O MUmyOFY5Ojd2Nx?=
HuTu-80 M3vvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PqNWlEPTB;MUOgcm0> MlXHNlQ3QDJ5NEe=
HCT 116 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7qTWM2OD1zNDDuUS=> NVPlXGY1OjR4OEK3OFc>
COLO-205 NX:1ZnE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPCVJBKSzVyPUG0JI5O M3rBNFI1Pjh{N{S3
NCI-H747 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHKTWM2OD1zNzDuUS=> M{XmcVI1Pjh{N{S3
COLO-678 NIG0R2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv2e|NKSzVyPUKxJI5O NES5eoUzPDZ6Mke0Oy=>
LoVo NWPITVdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n1V2lEPTB;MkKgcm0> MWmyOFY5Ojd2Nx?=
LS-1034 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrBTYw4UUN3ME2zNUBvVQ>? MoDINlQ3QDJ5NEe=
SNU-C2B NXLLZoRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;RTWM2OD12NTDuUS=> NXHmTXViOjR4OEK3OFc>
LS-123 NWHybpJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTd|IH7N Mn7aNlQ3QDJ5NEe=
SK-CO-1 MoCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfY[XFKSzVyPUixJI5O M4\qdFI1Pjh{N{S3
HCC2998 NYrY[It7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPrZmxKSzVyPUGyPEBvVQ>? MmHKNlQ3QDJ5NEe=
MDA-MB-231 MVvGeY5kfGmxbjDBd5NigQ>? MYKxNFAhdk1? NEXyNVc{OCCvaX6= MlO5bY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MVSyOFI1QDJ4NR?=
MDA-MB-435 NWHndZYzTnWwY4Tpc44hSXO|YYm= M2fCXlExOCCwTR?= NUPUe3hQOzBibXnu NHLJbZVqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NX35ZphIOjR{NEiyOlU>
BT-20  MkLBSpVv[3Srb36gRZN{[Xl? NWnUT4pUOTByL{K1NEBvVQ>? NVfH[oZEOjRiaB?= NFXoWopz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? M{D4[|I1OTd|NUSx
MDA-MB-231 M2XV[2Z2dmO2aX;uJGF{e2G7 MkTkNVAxKG6P NYfTO|dVOjRiaB?= NGnrdHBqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh NIL2b5czPDF5M{W0NS=>
H82 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoC1TWM2OD1|MD6yO{BvVQ>? NYXOVolKOjRzNk[1NFU>
GLC4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJyLkS3JI5O Ml\ZNlQyPjZ3MEW=
H69 NYPF[Gw4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S0TWlEPTB;OEOuN|Yhdk1? MVKyOFE3PjVyNR?=
H128 MmDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTZ7LkW1JI5O NGn3SJEzPDF4NkWwOS=>
H146 M3XwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPnTWM2OD1{OD61NUBvVQ>? MUOyOFE3PjVyNR?=
H187 MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG5eXAxUUN3ME2yOE46QSCwTR?= NYHxUnVjOjRzNk[1NFU>
H526 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPjTWM2OD1{MT62OEBvVQ>? NV[zdY5EOjRzNk[1NFU>
N592 M3X4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnob5FtUUN3ME2xOE4yOiCwTR?= MnPpNlQyPjZ3MEW=
H620 NED1U21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnleWFKSzVyPUOyMlY4KG6P MV6yOFE3PjVyNR?=
H792 NHTSe4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvmPVE2UUN3ME20OU4xPyCwTR?= NVvSOoQ4OjRzNk[1NFU>
H1173 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\WRXVKSzVyPUGyMlYzKG6P NV7EVWVnOjRzNk[1NFU>
AC3 M12yUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDkXnppUUN3ME2yOU46KG6P MXmyOFE3PjVyNR?=
H82 MUXGeY5kfGmxbjDBd5NigQ>? MnPHN|Ahdk1? MV[3NkBp M3vPdYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NFfGfFIzPDF4NkWwOS=>
GLC4 Mm\rSpVv[3Srb36gRZN{[Xl? NIDxdFI{OCCwTR?= M4HUNlczKGh? M2PX[4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MlnjNlQyPjZ3MEW=
H146  NUDXdIdOTnWwY4Tpc44hSXO|YYm= MnrBN|Ahdk1? NHnqepk4OiCq MmLCbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NI\i[|UzPDF4NkWwOS=>
OVCAR-5 MlHjR4VtdCCYaXHibYxqfHliQYPzZZk> MnHDNE0yODByIH7N NU\nXYNoPzJiaB?= M{LxPYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MY[yN|kxODF|Nh?=
OVCAR-8 NEPlemxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYOwMVExODBibl2= NYjpcYJRPzJiaB?= MU\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NUWzcYZOOjN7MECxN|Y>
A1847 NEHL[pBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{DYXFAuOTByMDDuUS=> M1fW[|czKGh? NUPEOZRWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYDMNlkxOjN7MECxN|Y>
SKOV-3 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV2wMVExODBibl2= M321cVczKGh? MnvmbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVWyN2xQOjN7MECxN|Y>
OVCAR-5 NGnVU4xCeG:ydH;zbZMhSXO|YYm= NUn2Wmo2OTBvMUCwJI5O MX[yOE81QC95MjDo NX7N[4lycW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M3\yN|I{QTByMUO2
OVCAR-8 M1uyVWFxd3C2b4Ppd{BCe3OjeR?= MmmyNVAuOTByIH7N MXWyOE81QC95MjDo MlXJbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NXjHepd3OjN7MECxN|Y>
A1847 NX;HTZpbSXCxcITvd4l{KEG|c3H5 MXqxNE0yODBibl2= MnHkNlQwPDhxN{KgbC=> MXPpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MXiyN|kxODF|Nh?=
H2228 M4Tkd2NmdGxiVnnhZoltcXS7IFHzd4F6 M2DNO|AuOTByMDDuUS=> NF3iTJM4OiCq M4\TcWlEPTB;MUOgcm0> NISzOWszOzV|M{K2OS=>
H3122 NH7JOIxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmXFNE0yODByIH7N NG\1T3I4OiCq M4D2UmlEPTB;MUCgcm0> MofLNlM2OzN{NkW=
K008 MkTOR4VtdCCYaXHibYxqfHliQYPzZZk> NUXmZoRJUUN3ME22NEBvVQ>? NHTDfWUzOzRzOEWyNy=>
K028 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF[1TlJKSzVyPUi0JI5O NXPicINDOjN2MUi1NlM>
K029 M{nmO2NmdGxiVnnhZoltcXS7IFHzd4F6 NGP5N5pKSzVyPUS2JI5O MWeyN|QyQDV{Mx?=
M23 NETMdoVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGLLemNKSzVyPUO3MlUhdk1? M4\1V|I{PDF6NUKz
K033 NILuPHJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWLDTHdwUUN3ME23OU42KG6P M2PoVlI{PDF6NUKz
K008 NWrrb|VwTnWwY4Tpc44hSXO|YYm= NWjPOYdiOjVyIH7N NXvZTpRSOjRiaB?= NITaUXRqdmS3Y3XzJGczKGG{cnXzeC=> MWGyN|QyQDV{Mx?=
K028 MoOySpVv[3Srb36gRZN{[Xl? MlntNlUxKG6P MXmyOEBp NIf3T3dqdmS3Y3XzJGczKGG{cnXzeC=> NYTlOph2OjN2MUi1NlM>
K029 MVvGeY5kfGmxbjDBd5NigQ>? M1TwSFI2OCCwTR?= Mn[wNlQhcA>? MmO5bY5lfWOnczDHNUBienKnc4S= NYTnT4dxOjN2MUi1NlM>
M23 M1T0emZ2dmO2aX;uJGF{e2G7 MknINlUxKG6P MVqyOEBp Ml6wbY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= NHXCOmgzOzRzOEWyNy=>
K033 NX[zS2llTnWwY4Tpc44hSXO|YYm= NF7zVVczPTBibl2= NVPKfYNFOjRiaB?= MmH2bY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w MYOyN|QyQDV{Mx?=
K008 M37WTmFxd3C2b4Ppd{BCe3OjeR?= M4HXRlExOCCwTR?= M4TVdlczKGh? MX3zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NUTIZohqOjN2MUi1NlM>
K028 NGf2WFBCeG:ydH;zbZMhSXO|YYm= MmrTNVAxKG6P NVjD[|hKPzJiaB?= MWnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MYGyN|QyQDV{Mx?=
K029 MVLBdI9xfG:|aYOgRZN{[Xl? M3rWSVExOCCwTR?= NFHS[2w4OiCq MX7zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MYmyN|QyQDV{Mx?=
M23 MXjBdI9xfG:|aYOgRZN{[Xl? NF;1fJoyODBibl2= M2fRV|czKGh? NIXjWGp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NVqzVZhnOjN2MUi1NlM>
K033 M37ZNWFxd3C2b4Ppd{BCe3OjeR?= MV6xNFAhdk1? MXO3NkBp M{myNZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MWSyN|QyQDV{Mx?=
RD M2jwRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXye3JKSzVyPUigcm0> MUSyN|MxOzd2MR?=
Rh41 NX:2V3o4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFyLkSgcm0> NX7Ee5F[OjN|MEO3OFE>
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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 (4)

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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