Ganetespib (STA-9090) 化学構造
分子量: 364.4

高品質保証

カスタマーフィードバック(2)

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 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 M3vFfmFxd3C2b4Ppd{BCe3OjeR?= NWTQXohuOzBxOECvNVUxNzJ3MDDuUS=> M2jH[VI1NzR6L{eyJIg> Ml;KbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MlLCNlU5QDJ3NUC=
MV411 MYfBdI9xfG:|aYOgRZN{[Xl? MoDON|AwQDBxMUWwM|I2OCCwTR?= M3Oyc|I1NzR6L{eyJIg> MVfpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= NHHyZ|AzPTh6MkW1NC=>
MGC-803 NYTLNVlbS2WubDDWbYFjcWyrdImgRZN{[Xl? Mk\zNE4yNTFyMECgcm0> MXm3NkBp NYrRPJk1cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NF;vc4ozPTV7MEiwOS=>
SGC-7901 M2LxfGNmdGxiVnnhZoltcXS7IFHzd4F6 MlfsNE4yNTFyMECgcm0> M3\CdlczKGh? M2X3UYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NX3qNFcyOjV3OUC4NFU>
MKN-28 NF7DTI1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2\qflAvOS1zMECwJI5O NVrWWZBxPzJiaB?= NYDoVVUzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MY[yOVU6ODhyNR?=
MGC-803 NIPRN2hHfW6ldHnvckBCe3OjeR?= NXXMc2RmOC5zLUGwNFAhdk1? MVyyOEBp MV3pcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> NGToWoozPTV7MEiwOS=>
HCT-116 NHi4b|NHfW6ldHnvckBCe3OjeR?= MWS1NI5O MVeyOEBp M{HDPWROW09? M3rlNIlv\HWlZXSgS|AwTzFiYYLy[ZN1 NYq4fFU1OjV{MUC3PVQ>
HT-29 M{P3O2Z2dmO2aX;uJGF{e2G7 M1j3d|Uxdk1? NHryWHczPCCq NYG4R5JlTE2VTx?= NGTFV|lqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MWqyOVIyODd7NB?=
SCC25 M1rQT2N6fG:6aXPpeJkhSXO|YYm= MVGxNE82OCCwTR?= MmLlNlQhcA>? NUTHTpRP\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NU\yZnk1OjV{MEW0N|A>
FUDA NIXTZpBEgXSxeHnjbZR6KEG|c3H5 NFvxWIgyOC93MDDuUS=> NUHBfo1WOjRiaB?= M3XZ[YRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M1e5UlI2OjB3NEOw
Detroit562 MorCR5l1d3irY3n0fUBCe3OjeR?= NYm4TWo5OTBxNUCgcm0> NV2z[3RXOjRiaB?= MYrk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M3jqe|I2OjB3NEOw
CAL27 MkjaR5l1d3irY3n0fUBCe3OjeR?= MVOxNE82OCCwTR?= M{fxWVI1KGh? NEDLflRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NW\rUndKOjV{MEW0N|A>
DSH1 NH21Rm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPLTWM2OD14IH7N MmW1NlQ4QDR6M{m=
SW-1710 NEfsTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT4S2d6UUN3ME22JI5O NFnWXmUzPDd6NEizPS=>
T24 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PYSGlEPTB;NzDuUS=> NGnV[VUzPDd6NEizPS=>
RT112 MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTlibl2= Mn;hNlQ4QDR6M{m=
639-V NUmwe5ZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofUTWM2OD1zMDDuUS=> MX2yOFc5PDh|OR?=
SCaBER NWTlWlE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO1UWpKSzVyPUGwJI5O MmrENlQ4QDR6M{m=
BFTC M3PEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTkTWM2OD1zNzDuUS=> NH3BV4ozPDd6NEizPS=>
J82 M1jpVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe1SGxKSzVyPUG4JI5O M1XzcVI1Pzh2OEO5
HT-1376 NFjQUIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK5TZlPUUN3ME2yNUBvVQ>? M4HVfVI1Pzh2OEO5
647-V M1SxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHpWWRKSzVyPUK3JI5O NFraVo0zPDd6NEizPS=>
UM-UC3 M4PT[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPXOmFCUUN3ME2zN{BvVQ>? MlTuNlQ4QDR6M{m=
LB831-BLC NUTLc5I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoftTWM2OD1|NDDuUS=> MnSwNlQ4QDR6M{m=
KU-19-19 NUfRXmplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4m0TmlEPTB;M{[gcm0> MYGyOFc5PDh|OR?=
35612 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTN6IH7N M1KwZ|I1Pzh2OEO5
5637 NF7kO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPKd5hCUUN3ME20OEBvVQ>? NXzDWFZVOjR5OES4N|k>
HT-1197 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\tTWM2OD13MzDuUS=> MlfhNlQ4QDR6M{m=
MGH-U3 M3nuRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHjTWM2OD13MzDuUS=> MV[yOFc5PDh|OR?=
TCCSUP NHjwSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHpUFFKSzVyPUG0NkBvVQ>? NGC0UXczPDd6NEizPS=>
RT4 NETxTnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmezTWM2OD1zN{OzJI5O MnjHNlQ4QDR6M{m=
SW780 M2nkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrvTWM2OD1|NEWxJI5O MYWyOFc5PDh|OR?=
RKO MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPmOHB6UUN3ME20JI5O M2[3OVI1Pjh{N{S3
LS-411 N MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\tTWM2OD13IH7N MYKyOFY5Ojd2Nx?=
SW620 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRThibl2= NGHYWWIzPDZ6Mke0Oy=>
HCT-15 NI\te2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXa[HUzUUN3ME24JI5O MoTjNlQ3QDJ5NEe=
HuTu-80 NFPCcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF|IH7N NUXRW2NuOjR4OEK3OFc>
HCT 116 M1PJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTF2IH7N NEfJUoEzPDZ6Mke0Oy=>
COLO-205 Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jYWGlEPTB;MUSgcm0> M4XRVFI1Pjh{N{S3
NCI-H747 M3fOSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTF5IH7N NXXNOo9HOjR4OEK3OFc>
COLO-678 MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHmTWM2OD1{MTDuUS=> MYiyOFY5Ojd2Nx?=
LoVo MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIS1NYpKSzVyPUKyJI5O M3j3clI1Pjh{N{S3
LS-1034 M{XrZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj6[VFDUUN3ME2zNUBvVQ>? MmDGNlQ3QDJ5NEe=
SNU-C2B MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljDTWM2OD12NTDuUS=> MWmyOFY5Ojd2Nx?=
LS-123 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfrTWM2OD15MzDuUS=> NGr4SpczPDZ6Mke0Oy=>
SK-CO-1 NY\TOZg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRThzIH7N M3y5[|I1Pjh{N{S3
HCC2998 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF{ODDuUS=> M3vpdVI1Pjh{N{S3
MDA-MB-231 M3nSbWZ2dmO2aX;uJGF{e2G7 MXexNFAhdk1? NWn4OlZYOzBibXnu NIrPVJdqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NEn6VGIzPDJ2OEK2OS=>
MDA-MB-435 NUPuRYpXTnWwY4Tpc44hSXO|YYm= NUHwT21VOTByIH7N NVv0SGx7OzBibXnu MVLpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NFX6d2UzPDJ2OEK2OS=>
BT-20  MWTGeY5kfGmxbjDBd5NigQ>? M3LkXVExOC9{NUCgcm0> MkSyNlQhcA>? NX20XlZUemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI NHHoTXMzPDF5M{W0NS=>
MDA-MB-231 M2fPeGZ2dmO2aX;uJGF{e2G7 NXzTc5ltOTByIH7N NI\4dpQzPCCq NEnoSYxqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh M3\EdFI1OTd|NUSx
H82 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTFTWM2OD1|MD6yO{BvVQ>? MVqyOFE3PjVyNR?=
GLC4 NXHGUWc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rWWGlEPTB;MkCuOFchdk1? MYOyOFE3PjVyNR?=
H69 M1W4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf3VZI5UUN3ME24N{4{PiCwTR?= MYeyOFE3PjVyNR?=
H128 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn3XIdKSzVyPU[5MlU2KG6P MVmyOFE3PjVyNR?=
H146 NGjJXIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fGfmlEPTB;MkiuOVEhdk1? M33vSlI1OTZ4NUC1
H187 M1Xrbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJ2Lkm5JI5O M13vRlI1OTZ4NUC1
H526 MlLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HPdmlEPTB;MkGuOlQhdk1? NYfIWWdmOjRzNk[1NFU>
N592 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfUXow4UUN3ME2xOE4yOiCwTR?= NXX3N2t7OjRzNk[1NFU>
H620 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\lXYFKSzVyPUOyMlY4KG6P NGfVOIozPDF4NkWwOS=>
H792 NHP6U3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom0TWM2OD12NT6wO{BvVQ>? M2O0W|I1OTZ4NUC1
H1173 M4e1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF{Lk[yJI5O MkXONlQyPjZ3MEW=
AC3 M{HrcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GzWGlEPTB;MkWuPUBvVQ>? MkLhNlQyPjZ3MEW=
H82 MXjGeY5kfGmxbjDBd5NigQ>? MVmzNEBvVQ>? M{TEclczKGh? M3u5NIlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> Mn7MNlQyPjZ3MEW=
GLC4 NEe2No5HfW6ldHnvckBCe3OjeR?= NE\Bb|I{OCCwTR?= NGXvdlg4OiCq NXT2R3pPcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M2\IZVI1OTZ4NUC1
H146  NX\wSYp2TnWwY4Tpc44hSXO|YYm= MXuzNEBvVQ>? Mo\TO|IhcA>? M4\6e4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M4TncVI1OTZ4NUC1
OVCAR-5 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2fnXFAuOTByMDDuUS=> MmHiO|IhcA>? M2\QbolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlzlNlM6ODBzM{[=
OVCAR-8 NF\KVVhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkHSNE0yODByIH7N NYTBU5FLPzJiaB?= Mnf2bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUDGToF{OjN7MECxN|Y>
A1847 NX\NWVhFS2WubDDWbYFjcWyrdImgRZN{[Xl? NHrWS|YxNTFyMECgcm0> NEfLc5M4OiCq NFPxXHRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MYSyN|kxODF|Nh?=
SKOV-3 NYOxOI12S2WubDDWbYFjcWyrdImgRZN{[Xl? NYTadFR{OC1zMECwJI5O MWO3NkBp NEXD[4ZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MkDhNlM6ODBzM{[=
OVCAR-5 NYi0THZUSXCxcITvd4l{KEG|c3H5 MVexNE0yODBibl2= MXiyOE81QC95MjDo MXXpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MoLBNlM6ODBzM{[=
OVCAR-8 M{H6[GFxd3C2b4Ppd{BCe3OjeR?= NYLi[FJPOTBvMUCwJI5O MmrJNlQwPDhxN{KgbC=> NEjuUFlqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MkHZNlM6ODBzM{[=
A1847 NGfGe4lCeG:ydH;zbZMhSXO|YYm= NWjrcHlbOTBvMUCwJI5O NYTJT3FuOjRxNEivO|IhcA>? NFvMNHJqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M4fNd|I{QTByMUO2
H2228 NHTxcVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXLLbJFqOC1zMECwJI5O NYjBeolLPzJiaB?= M3;OSGlEPTB;MUOgcm0> M2HBXFI{PTN|Mk[1
H3122 M3X6WGNmdGxiVnnhZoltcXS7IFHzd4F6 NYfs[|h6OC1zMECwJI5O M3yxflczKGh? MlHKTWM2OD1zMDDuUS=> MUCyN|U{OzJ4NR?=
K008 NYmxUIx3S2WubDDWbYFjcWyrdImgRZN{[Xl? NHPmWnJKSzVyPU[wJI5O MoL4NlM1OTh3MkO=
K028 MmDsR4VtdCCYaXHibYxqfHliQYPzZZk> MWDJR|UxRTh2IH7N MWSyN|QyQDV{Mx?=
K029 M4TpSGNmdGxiVnnhZoltcXS7IFHzd4F6 MljOTWM2OD12NjDuUS=> Mkn6NlM1OTh3MkO=
M23 MlSzR4VtdCCYaXHibYxqfHliQYPzZZk> M4jpSGlEPTB;M{euOUBvVQ>? M2PtWVI{PDF6NUKz
K033 NUPkdlJFS2WubDDWbYFjcWyrdImgRZN{[Xl? NHqweXFKSzVyPUe1MlUhdk1? Ml:zNlM1OTh3MkO=
K008 NGXKUnRHfW6ldHnvckBCe3OjeR?= NU\VWYNQOjVyIH7N MXmyOEBp MUDpcoR2[2W|IFeyJIFzemW|dB?= MXeyN|QyQDV{Mx?=
K028 M1zJRmZ2dmO2aX;uJGF{e2G7 MnrQNlUxKG6P MVmyOEBp NFfuOIJqdmS3Y3XzJGczKGG{cnXzeC=> NVrUcGE1OjN2MUi1NlM>
K029 MYTGeY5kfGmxbjDBd5NigQ>? M{DxSlI2OCCwTR?= NGfjeWUzPCCq NXr6VpJicW6mdXPld{BIOSCjcoLld5Q> NUDGcJJKOjN2MUi1NlM>
M23 M3HqeGZ2dmO2aX;uJGF{e2G7 NGjrTmEzPTBibl2= MUCyOEBp MWjpcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= NF3p[YUzOzRzOEWyNy=>
K033 Mn3FSpVv[3Srb36gRZN{[Xl? Mli0NlUxKG6P MVWyOEBp NFHUdlBqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36= MlLTNlM1OTh3MkO=
K008 NYnkfXFOSXCxcITvd4l{KEG|c3H5 MY[xNFAhdk1? NEfvbpQ4OiCq NEnURZp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NWnZSZMxOjN2MUi1NlM>
K028 MX3BdI9xfG:|aYOgRZN{[Xl? M{XJbVExOCCwTR?= NIizcpM4OiCq MlvDd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MXeyN|QyQDV{Mx?=
K029 NFz6VW5CeG:ydH;zbZMhSXO|YYm= MmO2NVAxKG6P MUi3NkBp NGP6T4h{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NUDtOohpOjN2MUi1NlM>
M23 MWHBdI9xfG:|aYOgRZN{[Xl? NWTo[HV6OTByIH7N MX63NkBp NGX1T41{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MUKyN|QyQDV{Mx?=
K033 M1nLTWFxd3C2b4Ppd{BCe3OjeR?= MVSxNFAhdk1? NYrwd2xLPzJiaB?= MX7zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MoPrNlM1OTh3MkO=
RD MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml21TWM2OD16IH7N Ml\YNlM{ODN5NEG=
Rh41 M{Tq[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fsV2lEPTB;MUCuOEBvVQ>? M4q1UFI{OzB|N{Sx
Rh18 NIC2flNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTBNYJKUUN3ME22MlIhdk1? MknENlM{ODN5NEG=
Rh30 NEDXPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIL4fXRKSzVyPUWuOkBvVQ>? NH36TFkzOzNyM{e0NS=>
BT-12 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn5bWlKSzVyPUG0MlMhdk1? M3;oUFI{OzB|N{Sx
CHLA-266 M2niT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrTTWM2OD1{Nz6xJI5O NYHFPVlQOjN|MEO3OFE>
TC-71 NH3MZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HKPGlEPTB;ND61JI5O NXyyZ3djOjN|MEO3OFE>
CHLA-9 NIL0Z41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HXOGlEPTB;ND62JI5O M2Hxd|I{OzB|N{Sx
CHLA-10 Moj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XLcWlEPTB;NT63JI5O M3\0UVI{OzB|N{Sx
CHLA-258 M{X2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnOTFdFUUN3ME22MlQhdk1? NITacIczOzNyM{e0NS=>
SJ-GBM2 M2XKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnBWoVKSzVyPUGyMlkhdk1? MmXwNlM{ODN5NEG=
NB-1643 NHnPPJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnwbIZvUUN3ME23MlQhdk1? M131VFI{OzB|N{Sx
NB-EBc1 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XiTGlEPTB;MU[uPEBvVQ>? M1XicVI{OzB|N{Sx
CHLA-90 NUHtR|JyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTtTWM2OD1{Mj6zJI5O NVX6WVZoOjN|MEO3OFE>
CHLA-136 NX;POWZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJ|LkKgcm0> MUKyN|MxOzd2MR?=
NALM-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fSPWlEPTB;MUGuO{BvVQ>? NF\xS4EzOzNyM{e0NS=>
COG-LL-317 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTRwNDDuUS=> NGi4XGwzOzNyM{e0NS=>
RS4;11 MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF|LkWgcm0> M{jZclI{OzB|N{Sx
MOLT-4 NUfkcW84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnsWmJKSzVyPUGwMlYhdk1? MnfPNlM{ODN5NEG=
CCRF-CEM (1) MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\PXXlGUUN3ME2xNk42KG6P MXKyN|MxOzd2MR?=
CCRF-CEM (2) MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnhSnJXUUN3ME23MlIhdk1? M3[3Z|I{OzB|N{Sx
Kasumi-1 M{HiXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP3N|JKSzVyPUWuPEBvVQ>? NXP0emNCOjN|MEO3OFE>
Karpas-299 NXzPO4dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zwbWlEPTB;OT62JI5O NHzQcGYzOzNyM{e0NS=>
Ramos-RA1 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTdwNDDuUS=> Ml;QNlM{ODN5NEG=
LNCaP MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfvcJVKSzVyPUigcm0> MUKyN|E2OjByNB?=
VCaP MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvtcGlKSzVyPUegcm0> MWCyN|E2OjByNB?=
H1355 NX\tbJdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{juXmlEPTB;NTDuUS=> MX6yN|AyOjJ2OB?=
H157 M4LKXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;zOW84UUN3ME23JI5O NFr1RpIzOzBzMkK0PC=>
H460 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTXTWM2OD16IH7N MYiyN|AyOjJ2OB?=
IA-LM MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFyIH7N MlrsNlMxOTJ{NEi=
HOP-62 MkK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fU[GlEPTB;MUGgcm0> NH3X[2ozOzBzMkK0PC=>
H23 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknpTWM2OD1zMTDuUS=> MnvoNlMxOTJ{NEi=
H2030 NWrXfHNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz1WZJvUUN3ME2xNkBvVQ>? MV[yN|AyOjJ2OB?=
H441 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS3dm5XUUN3ME2xOEBvVQ>? MkXVNlMxOTJ{NEi=
H2212 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LVS2lEPTB;MUegcm0> Ml7YNlMxOTJ{NEi=
SK-LU-1 NVzzUIVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jvUmlEPTB;MUigcm0> NH7h[JozOzBzMkK0PC=>
H2009 NXy0WHVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF7IH7N M2\jUlI{ODF{MkS4
H1792 Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP0O2ZKSzVyPUKwJI5O NFXhXZUzOzBzMkK0PC=>
COR-L23 M3HSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjoXllKSzVyPUKyJI5O M4jIcVI{ODF{MkS4
H727 M{H0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;zc5NKSzVyPUK4JI5O NXPsUnI2OjNyMUKyOFg>
H1734 MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofRTWM2OD1{ODDuUS=> NXPvSVh4OjNyMUKyOFg>
H358 M1LNc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\me2lEPTB;Mkmgcm0> NYnjXphYOjNyMUKyOFg>
A549 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y1ZmlEPTB;NEOgcm0> MlvrNlMxOTJ{NEi=
H2122 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfTSpR[UUN3ME21N{BvVQ>? NUSyZoZHOjNyMUKyOFg>
Calu-1 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjMZmhKSzVyPUW4JI5O Mlq4NlMxOTJ{NEi=
Calu-6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm4TWM2OD14NDDuUS=> NHzRR4czOzBzMkK0PC=>
NCI-H1975 MnToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILyU5g1QCCq MoHhTWM2OD1zNjDuUS=> MXyyNlE1PDZ4NR?=
NCI-H1975 NFXUVnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:3NkBp NFna[VlKSzVyPUigcm0> MmO4NlIyPDR4NkW=

... 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)

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。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 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 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.

最近チェックしたアイテム

Tags: Ganetespib (STA-9090)を買う | Ganetespib (STA-9090)供給者 | Ganetespib (STA-9090)を購入する | Ganetespib (STA-9090)費用 | Ganetespib (STA-9090)生産者 | オーダーGanetespib (STA-9090) | Ganetespib (STA-9090)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ