Ganetespib (STA-9090) 化学構造
分子量: 364.4

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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 NFKyUVRCeG:ydH;zbZMhSXO|YYm= NFXzU4U{OC96MD:xOVAwOjVyIH7N MY[yOE81QC95MjDo NYXZSZlrcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MX2yOVg5OjV3MB?=
MV411 MVPBdI9xfG:|aYOgRZN{[Xl? MoPjN|AwQDBxMUWwM|I2OCCwTR?= NW\4dmFKOjRxNEivO|IhcA>? NIDZU5hqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MWSyOVg5OjV3MB?=
MGC-803 M{foeWNmdGxiVnnhZoltcXS7IFHzd4F6 NYDiOWF7OC5zLUGwNFAhdk1? NETVSI84OiCq NV\t[oc{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Ml3ENlU2QTB6MEW=
SGC-7901 NFzlO4RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXrxUolWOC5zLUGwNFAhdk1? MmXsO|IhcA>? NEDQem1qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MUCyOVU6ODhyNR?=
MKN-28 M3rzVmNmdGxiVnnhZoltcXS7IFHzd4F6 NGHFOWcxNjFvMUCwNEBvVQ>? Mmr1O|IhcA>? MkHsbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3Xi[|I2PTlyOEC1
MGC-803 NXT5WnF6TnWwY4Tpc44hSXO|YYm= NV[1c2QxOC5zLUGwNFAhdk1? MXuyOEBp MV\pcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> MUKyOVU6ODhyNR?=
HCT-116 MUPGeY5kfGmxbjDBd5NigQ>? NX\ldIFrPTCwTR?= MmCwNlQhcA>? M1vUUWROW09? MnHIbY5lfWOnZDDHNE9IOSCjcoLld5Q> Ml;VNlUzOTB5OUS=
HT-29 NIDBdoRHfW6ldHnvckBCe3OjeR?= MXq1NI5O NWfrTmZ3OjRiaB?= MUnEUXNQ NYSwbZVzcW6mdXPl[EBIOC:JMTDhdpJme3R? M4W0c|I2OjFyN{m0
SCC25 NWniZZV6S3m2b4jpZ4l1gSCDc4PhfS=> MnXONVAwPTBibl2= MXiyOEBp NYnaeXV4\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MkXNNlUzODV2M{C=
FUDA M1W0ZmN6fG:6aXPpeJkhSXO|YYm= NYf5WFF6OTBxNUCgcm0> M3vjZVI1KGh? M2PzV4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MX2yOVIxPTR|MB?=
Detroit562 MlrJR5l1d3irY3n0fUBCe3OjeR?= MnHVNVAwPTBibl2= M1rRVFI1KGh? NV\yfYtL\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MkPyNlUzODV2M{C=
CAL27 MXrDfZRwgGmlaYT5JGF{e2G7 M4n6NFExNzVyIH7N NIrp[WUzPCCq MmT0[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M1zkdlI2OjB3NEOw
DSH1 NIDVNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHJXXpKSzVyPU[gcm0> NFn2RXQzPDd6NEizPS=>
SW-1710 NG[xN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTZibl2= MYCyOFc5PDh|OR?=
T24 NWrYfpVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7h[pVKSzVyPUegcm0> M1fKblI1Pzh2OEO5
RT112 M4jBWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PZUWlEPTB;OTDuUS=> NH\BZ3ozPDd6NEizPS=>
639-V NW\rOHF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTRWY1oUUN3ME2xNEBvVQ>? NXu0VohQOjR5OES4N|k>
SCaBER MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFyIH7N NHrUXmQzPDd6NEizPS=>
BFTC M1uxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq1eVJQUUN3ME2xO{BvVQ>? MWOyOFc5PDh|OR?=
J82 NXWxSW9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TDVGlEPTB;MUigcm0> MUeyOFc5PDh|OR?=
HT-1376 NIS5UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJzIH7N NIfjS5ozPDd6NEizPS=>
647-V MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPHTWM2OD1{NzDuUS=> Mnr4NlQ4QDR6M{m=
UM-UC3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;qTWM2OD1|MzDuUS=> NEXjO3YzPDd6NEizPS=>
LB831-BLC NHXNZZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHuPIZKSzVyPUO0JI5O M3nRW|I1Pzh2OEO5
KU-19-19 NWPlSXk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;VSldbUUN3ME2zOkBvVQ>? M1:zTFI1Pzh2OEO5
35612 MnjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLiSGlKSzVyPUO4JI5O NXn5cGpPOjR5OES4N|k>
5637 M1fQVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfaTWM2OD12NDDuUS=> NU\HcnNCOjR5OES4N|k>
HT-1197 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PDbmlEPTB;NUOgcm0> M{LjW|I1Pzh2OEO5
MGH-U3 NHT5XI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nQWGlEPTB;NUOgcm0> NH7mcJczPDd6NEizPS=>
TCCSUP NUPiXZZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrUdGdKSzVyPUG0NkBvVQ>? NIDTdFQzPDd6NEizPS=>
RT4 M1zGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfCTWM2OD1zN{OzJI5O NWe2NIdjOjR5OES4N|k>
SW780 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTN2NUGgcm0> MVyyOFc5PDh|OR?=
RKO Moe3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1n5eWlEPTB;NDDuUS=> NFnMS28zPDZ6Mke0Oy=>
LS-411 N MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP0e5M2UUN3ME21JI5O NFr3bGUzPDZ6Mke0Oy=>
SW620 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LmfWlEPTB;ODDuUS=> NIfXNFgzPDZ6Mke0Oy=>
HCT-15 NWHKcYZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[zeY5YUUN3ME24JI5O NVW2d4NQOjR4OEK3OFc>
HuTu-80 M{TDTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DLVGlEPTB;MUOgcm0> NF7lUG8zPDZ6Mke0Oy=>
HCT 116 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkj1TWM2OD1zNDDuUS=> M4XHRlI1Pjh{N{S3
COLO-205 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:0TYxYUUN3ME2xOEBvVQ>? MV2yOFY5Ojd2Nx?=
NCI-H747 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DKdmlEPTB;MUegcm0> NUTRRolqOjR4OEK3OFc>
COLO-678 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fYPGlEPTB;MkGgcm0> NX\wOXJTOjR4OEK3OFc>
LoVo NYTpd2xST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjkSYdLUUN3ME2yNkBvVQ>? M2jnUFI1Pjh{N{S3
LS-1034 M{nMVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTNzIH7N MV2yOFY5Ojd2Nx?=
SNU-C2B NE\ZV3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LDUGlEPTB;NEWgcm0> NXrQTm4zOjR4OEK3OFc>
LS-123 NIDjd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTd|IH7N MXyyOFY5Ojd2Nx?=
SK-CO-1 Ml:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLaT5JQUUN3ME24NUBvVQ>? MonuNlQ3QDJ5NEe=
HCC2998 M2rCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHT1Z4VKSzVyPUGyPEBvVQ>? NHrUXZozPDZ6Mke0Oy=>
MDA-MB-231 M1T5OGZ2dmO2aX;uJGF{e2G7 NHzVO|YyODBibl2= M4O0N|MxKG2rbh?= M2TYR4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MnnqNlQzPDh{NkW=
MDA-MB-435 M2i3ZmZ2dmO2aX;uJGF{e2G7 NF;LbJAyODBibl2= MkjRN|AhdWmw MnjCbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NVHV[nNKOjR{NEiyOlU>
BT-20  MljhSpVv[3Srb36gRZN{[Xl? M{T1fVExOC9{NUCgcm0> NWrpUIpXOjRiaB?= MYny[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> M3nZXFI1OTd|NUSx
MDA-MB-231 NX\uO214TnWwY4Tpc44hSXO|YYm= M2fhOFExOCCwTR?= NEnPO5gzPCCq MXTpcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg NWD5SZdSOjRzN{O1OFE>
H82 M1jjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLiTWM2OD1|MD6yO{BvVQ>? Mk\wNlQyPjZ3MEW=
GLC4 NYHI[JRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\aNW1ZUUN3ME2yNE41PyCwTR?= NV\VRW5rOjRzNk[1NFU>
H69 NXPHdIdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmj5TWM2OD16Mz6zOkBvVQ>? NFnqPJMzPDF4NkWwOS=>
H128 MmLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPBdGFKSzVyPU[5MlU2KG6P Moe1NlQyPjZ3MEW=
H146 M{nQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TiZWlEPTB;MkiuOVEhdk1? MXyyOFE3PjVyNR?=
H187 NWLLOGw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\YTWM2OD1{ND65PUBvVQ>? NWD1OHllOjRzNk[1NFU>
H526 NWPvepFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL1TWM2OD1{MT62OEBvVQ>? NWrC[ndJOjRzNk[1NFU>
N592 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF2LkGyJI5O MorKNlQyPjZ3MEW=
H620 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN{Lk[3JI5O M1e1blI1OTZ4NUC1
H792 NXzW[mQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHLb49KSzVyPUS1MlA4KG6P MXOyOFE3PjVyNR?=
H1173 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF{Lk[yJI5O M3naOFI1OTZ4NUC1
AC3 MoKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjwSJhlUUN3ME2yOU46KG6P MViyOFE3PjVyNR?=
H82 NXjHW3o2TnWwY4Tpc44hSXO|YYm= MmrlN|Ahdk1? Mmf0O|IhcA>? MVzpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= MXyyOFE3PjVyNR?=
GLC4 MYfGeY5kfGmxbjDBd5NigQ>? MYmzNEBvVQ>? NGjUVoQ4OiCq M{\NZolv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NY\xdoV4OjRzNk[1NFU>
H146  MYXGeY5kfGmxbjDBd5NigQ>? NU\Hb5B7OzBibl2= MoCwO|IhcA>? M2LmT4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NX;DeJh[OjRzNk[1NFU>
OVCAR-5 NGrmTnJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVnZXHdXOC1zMECwJI5O M2DkTFczKGh? M1exXIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnHLNlM6ODBzM{[=
OVCAR-8 NIHjVoRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlLrNE0yODByIH7N M2PwZ|czKGh? M1\sTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlLKNlM6ODBzM{[=
A1847 M2f3UmNmdGxiVnnhZoltcXS7IFHzd4F6 NX3Ye3JmOC1zMECwJI5O NUThdoRjPzJiaB?= MkTPbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NWHXeZN5OjN7MECxN|Y>
SKOV-3 MlSyR4VtdCCYaXHibYxqfHliQYPzZZk> M1G3W|AuOTByMDDuUS=> MX:3NkBp M2HaSolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MXmyN|kxODF|Nh?=
OVCAR-5 M372emFxd3C2b4Ppd{BCe3OjeR?= M4CyUlExNTFyMDDuUS=> NXPl[mh6OjRxNEivO|IhcA>? MnzVbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= Moj6NlM6ODBzM{[=
OVCAR-8 NGjrN2FCeG:ydH;zbZMhSXO|YYm= M3zpdlExNTFyMDDuUS=> MnTtNlQwPDhxN{KgbC=> MUnpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 M3THUVI{QTByMUO2
A1847 M3OzeGFxd3C2b4Ppd{BCe3OjeR?= NIf6ToQyOC1zMECgcm0> MXmyOE81QC95MjDo MYfpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MWSyN|kxODF|Nh?=
H2228 NX;xfZl2S2WubDDWbYFjcWyrdImgRZN{[Xl? MmXaNE0yODByIH7N Mn;2O|IhcA>? NETaOXRKSzVyPUGzJI5O NVnVcHdYOjN3M{OyOlU>
H3122 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUDyPXVDOC1zMECwJI5O MWC3NkBp MmXkTWM2OD1zMDDuUS=> M3nUcFI{PTN|Mk[1
K008 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGPlRmlKSzVyPU[wJI5O MoPzNlM1OTh3MkO=
K028 M4TUO2NmdGxiVnnhZoltcXS7IFHzd4F6 MV7JR|UxRTh2IH7N MXGyN|QyQDV{Mx?=
K029 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYnJR|UxRTR4IH7N M2TV[VI{PDF6NUKz
M23 NHq4OndE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVjrWlF1UUN3ME2zO{42KG6P NI\yRogzOzRzOEWyNy=>
K033 Mn:yR4VtdCCYaXHibYxqfHliQYPzZZk> NXf5TplmUUN3ME23OU42KG6P NW\ZU2V2OjN2MUi1NlM>
K008 MmjlSpVv[3Srb36gRZN{[Xl? M2nENVI2OCCwTR?= M{PJVFI1KGh? M4LBcYlv\HWlZYOgS|Ih[XK{ZYP0 NXHDUpRYOjN2MUi1NlM>
K028 M4jlRmZ2dmO2aX;uJGF{e2G7 NV3WNYxNOjVyIH7N NVzGVpYxOjRiaB?= NYHBSnRWcW6mdXPld{BIOiCjcoLld5Q> MV2yN|QyQDV{Mx?=
K029 NUjpR5lqTnWwY4Tpc44hSXO|YYm= MWCyOVAhdk1? Ml7WNlQhcA>? Mlv3bY5lfWOnczDHNUBienKnc4S= Mk\uNlM1OTh3MkO=
M23 M3OzTWZ2dmO2aX;uJGF{e2G7 MmLJNlUxKG6P M1;WO|I1KGh? MojSbY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= MlLqNlM1OTh3MkO=
K033 MWPGeY5kfGmxbjDBd5NigQ>? M4nkZVI2OCCwTR?= M{LMUVI1KGh? M3jUUYlv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= MX[yN|QyQDV{Mx?=
K008 MYHBdI9xfG:|aYOgRZN{[Xl? NUPncmc2OTByIH7N NXvNe5QzPzJiaB?= M{PzdJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M2HWXFI{PDF6NUKz
K028 NGfncWxCeG:ydH;zbZMhSXO|YYm= MlHSNVAxKG6P NHHQZoM4OiCq M{Tzc5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MX[yN|QyQDV{Mx?=
K029 NH[2VFFCeG:ydH;zbZMhSXO|YYm= NUn0XY8xOTByIH7N M1m0dFczKGh? NGLO[FZ{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MnX2NlM1OTh3MkO=
M23 MWPBdI9xfG:|aYOgRZN{[Xl? NFnUeJIyODBibl2= M2j5elczKGh? MnS3d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MkLqNlM1OTh3MkO=
K033 NIjKZY9CeG:ydH;zbZMhSXO|YYm= Mn;VNVAxKG6P Mof6O|IhcA>? NYfiR2NXe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NIDMZ|czOzRzOEWyNy=>
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Rh41 NGDDfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjmOlJGUUN3ME2xNE41KG6P MlfmNlM{ODN5NEG=
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Rh30 M4jLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfUS|JKSzVyPUWuOkBvVQ>? MXuyN|MxOzd2MR?=
BT-12 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfCZ3FKSzVyPUG0MlMhdk1? NYPlWXVIOjN|MEO3OFE>
CHLA-266 M2rQd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHEV5lKSzVyPUK3MlEhdk1? NFXQb2gzOzNyM{e0NS=>
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CHLA-10 Ml6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTVwNzDuUS=> MXyyN|MxOzd2MR?=
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NB-1643 NHfOWoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX33NmdXUUN3ME23MlQhdk1? NG\EPZEzOzNyM{e0NS=>
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CHLA-90 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ{LkOgcm0> MkG1NlM{ODN5NEG=
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NALM-6 M3z2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PJOmlEPTB;MUGuO{BvVQ>? NEP4[FgzOzNyM{e0NS=>
COG-LL-317 NGD3SopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojRTWM2OD12LkSgcm0> MnvrNlM{ODN5NEG=
RS4;11 NX;TOZg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zFdmlEPTB;MUOuOUBvVQ>? NVGxOGJ1OjN|MEO3OFE>
MOLT-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rxT2lEPTB;MUCuOkBvVQ>? NYnDRlI5OjN|MEO3OFE>
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CCRF-CEM (2) NHiwUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK3TWM2OD15LkKgcm0> MWKyN|MxOzd2MR?=
Kasumi-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTueoxKSzVyPUWuPEBvVQ>? NED3T4UzOzNyM{e0NS=>
Karpas-299 NH7JWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXryZ3Q4UUN3ME25MlYhdk1? MVeyN|MxOzd2MR?=
Ramos-RA1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;BUGlEPTB;Nz60JI5O M37yb|I{OzB|N{Sx
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HOP-62 M2LqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnkR5VHUUN3ME2xNUBvVQ>? NEDKOokzOzBzMkK0PC=>
H23 NXfofmFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTFzIH7N M4HQ[lI{ODF{MkS4
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COR-L23 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m1W2lEPTB;MkKgcm0> MkeyNlMxOTJ{NEi=
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H358 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ7IH7N M1jo[lI{ODF{MkS4
A549 MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi1e2VKSzVyPUSzJI5O NU\ySlFzOjNyMUKyOFg>
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Calu-6 NETUe3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnxbGdWUUN3ME22OEBvVQ>? MnT4NlMxOTJ{NEi=
NCI-H1975 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHLWY81QCCq NH\6SYVKSzVyPUG2JI5O MViyNlE1PDZ4NR?=
NCI-H1975 M333Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LnTlczKGh? NWO1[ppEUUN3ME24JI5O NEHRZ2IzOjF2NE[2OS=>

... 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

文献中の引用 (5)

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)

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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 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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