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 M3jlemFxd3C2b4Ppd{BCe3OjeR?= NXHUTGhGOzBxOECvNVUxNzJ3MDDuUS=> M3;6eVI1NzR6L{eyJIg> NE[2TVBqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NVTjVZptOjV6OEK1OVA>
MV411 MnTqRZBweHSxc3nzJGF{e2G7 MlrjN|AwQDBxMUWwM|I2OCCwTR?= NHPldGUzPC92OD:3NkBp NHG5flZqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> M1r6PFI2QDh{NUWw
MGC-803 NInYWIpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUnFdZRIOC5zLUGwNFAhdk1? M1G5O|czKGh? MXrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NEfQW5IzPTV7MEiwOS=>
SGC-7901 NGjZSmxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGXkZlYxNjFvMUCwNEBvVQ>? MnXkO|IhcA>? M1HJNolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHfTb3QzPTV7MEiwOS=>
MKN-28 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGjD[pQxNjFvMUCwNEBvVQ>? NYC2OG9TPzJiaB?= NFv3fFlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NXzrPXpuOjV3OUC4NFU>
MGC-803 NX\w[25vTnWwY4Tpc44hSXO|YYm= NFfKVoQxNjFvMUCwNEBvVQ>? NFLYOWgzPCCq NXXHR45WcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NFPs[5UzPTV7MEiwOS=>
HCT-116 MWXGeY5kfGmxbjDBd5NigQ>? NVy1N5BQPTCwTR?= MnW4NlQhcA>? MXrEUXNQ M2fZfYlv\HWlZXSgS|AwTzFiYYLy[ZN1 NH63eIQzPTJzMEe5OC=>
HT-29 NFXmcVdHfW6ldHnvckBCe3OjeR?= M4i2VVUxdk1? NFXiT2YzPCCq MkGzSG1UVw>? NGHXbZVqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NIDyNoczPTJzMEe5OC=>
SCC25 NHXDTodEgXSxeHnjbZR6KEG|c3H5 M4HPeVExNzVyIH7N NI[4cG8zPCCq NYP4TJNU\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NHG0bHozPTJyNUSzNC=>
FUDA NWfiV40zS3m2b4jpZ4l1gSCDc4PhfS=> MmXBNVAwPTBibl2= M3zLSVI1KGh? Mk\0[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NVv0ZVBCOjV{MEW0N|A>
Detroit562 M32w[WN6fG:6aXPpeJkhSXO|YYm= NXXkXm0xOTBxNUCgcm0> NFP2PZczPCCq NV\HW3lb\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M{PFUlI2OjB3NEOw
CAL27 NFTOOYxEgXSxeHnjbZR6KEG|c3H5 NW\4R3NtOTBxNUCgcm0> NXLjTJhLOjRiaB?= NYr3OlM4\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M122eVI2OjB3NEOw
DSH1 Moj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nJ[WlEPTB;NjDuUS=> NEK3Z3YzPDd6NEizPS=>
SW-1710 NHrWWlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\nelRKSzVyPU[gcm0> Mki4NlQ4QDR6M{m=
T24 M33kbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTLTWx[UUN3ME23JI5O NFvuUY8zPDd6NEizPS=>
RT112 NIDoOWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTlibl2= NGLxVJUzPDd6NEizPS=>
639-V NXS5WXhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nXU2lEPTB;MUCgcm0> NInVeGczPDd6NEizPS=>
SCaBER MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFyIH7N NHK5bmkzPDd6NEizPS=>
BFTC NGHmRm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTF5IH7N Mlr6NlQ4QDR6M{m=
J82 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfHTWM2OD1zODDuUS=> NWLZT2VyOjR5OES4N|k>
HT-1376 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfoR5hXUUN3ME2yNUBvVQ>? MoHiNlQ4QDR6M{m=
647-V NXfKd|BxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\C[pZKSzVyPUK3JI5O NXHiXGY3OjR5OES4N|k>
UM-UC3 MoG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj5TWM2OD1|MzDuUS=> NGLMcZQzPDd6NEizPS=>
LB831-BLC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DEN2lEPTB;M{Sgcm0> M1\SVVI1Pzh2OEO5
KU-19-19 NGnEb45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTN4IH7N NHLwRVQzPDd6NEizPS=>
35612 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjZTWM2OD1|ODDuUS=> NIH4PXkzPDd6NEizPS=>
5637 NF7VfpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTR2IH7N Ml3mNlQ4QDR6M{m=
HT-1197 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHZUJlKSzVyPUWzJI5O MWqyOFc5PDh|OR?=
MGH-U3 NXLzNlZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGm0eolKSzVyPUWzJI5O MVuyOFc5PDh|OR?=
TCCSUP NGPsT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2H0SWlEPTB;MUSyJI5O MoPMNlQ4QDR6M{m=
RT4 NWe5ZW5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4mxXWlEPTB;MUezN{BvVQ>? M1fGPVI1Pzh2OEO5
SW780 NWryXFBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTN2NUGgcm0> MkixNlQ4QDR6M{m=
RKO MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O3W2lEPTB;NDDuUS=> Ml\RNlQ3QDJ5NEe=
LS-411 N NXfOWFJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GzT2lEPTB;NTDuUS=> MnHJNlQ3QDJ5NEe=
SW620 NFvJS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRThibl2= M3fUcFI1Pjh{N{S3
HCT-15 NYrIO2d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXBRWxKSzVyPUigcm0> NILFWZEzPDZ6Mke0Oy=>
HuTu-80 NXnCZ|hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnvZmdHUUN3ME2xN{BvVQ>? MVmyOFY5Ojd2Nx?=
HCT 116 M{jocGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkexTWM2OD1zNDDuUS=> NHXsTYMzPDZ6Mke0Oy=>
COLO-205 NX35bXZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPze3hKSzVyPUG0JI5O NUTHcIFKOjR4OEK3OFc>
NCI-H747 M3u1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;KTWM2OD1zNzDuUS=> MlW5NlQ3QDJ5NEe=
COLO-678 M3TLOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nYcmlEPTB;MkGgcm0> NITXPXkzPDZ6Mke0Oy=>
LoVo M1fLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X4VmlEPTB;MkKgcm0> M{Lme|I1Pjh{N{S3
LS-1034 NYnqcmJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7JTWM2OD1|MTDuUS=> NUCwZoFJOjR4OEK3OFc>
SNU-C2B MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH33S21KSzVyPUS1JI5O M2TpS|I1Pjh{N{S3
LS-123 NHK0[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;VRWFYUUN3ME23N{BvVQ>? NUHoco96OjR4OEK3OFc>
SK-CO-1 NEKzXJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\5T2lEPTB;OEGgcm0> MYKyOFY5Ojd2Nx?=
HCC2998 M37sOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LzRWlEPTB;MUK4JI5O M1\DdlI1Pjh{N{S3
MDA-MB-231 Mm\uSpVv[3Srb36gRZN{[Xl? M2\melExOCCwTR?= Mmn2N|AhdWmw MXPpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MYmyOFI1QDJ4NR?=
MDA-MB-435 NEDWTpZHfW6ldHnvckBCe3OjeR?= MlzqNVAxKG6P M{HQdFMxKG2rbh?= Mnn0bY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NX:2PJdDOjR{NEiyOlU>
BT-20  M4q3e2Z2dmO2aX;uJGF{e2G7 MkG5NVAxNzJ3MDDuUS=> NIftUWwzPCCq MUjy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> M3jpbFI1OTd|NUSx
MDA-MB-231 NUL0Zol6TnWwY4Tpc44hSXO|YYm= M1TRPVExOCCwTR?= NGTwV2QzPCCq MoPJbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> NILjR|gzPDF5M{W0NS=>
H82 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrlTWM2OD1|MD6yO{BvVQ>? NXzjOZRWOjRzNk[1NFU>
GLC4 NGKz[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDSTWM2OD1{MD60O{BvVQ>? MUWyOFE3PjVyNR?=
H69 M1fTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLITWM2OD16Mz6zOkBvVQ>? MVyyOFE3PjVyNR?=
H128 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C5[WlEPTB;NkmuOVUhdk1? NHv3OngzPDF4NkWwOS=>
H146 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO1ZZNKSzVyPUK4MlUyKG6P MVGyOFE3PjVyNR?=
H187 M1T2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PCNWlEPTB;MkSuPVkhdk1? MU[yOFE3PjVyNR?=
H526 M1TFVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED1NGRKSzVyPUKxMlY1KG6P MlT0NlQyPjZ3MEW=
N592 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFuxbXhKSzVyPUG0MlEzKG6P NUGxZ3NEOjRzNk[1NFU>
H620 MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv5WWlsUUN3ME2zNk43PyCwTR?= Mn3jNlQyPjZ3MEW=
H792 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDmTWM2OD12NT6wO{BvVQ>? MVeyOFE3PjVyNR?=
H1173 MlnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTNc3pKSzVyPUGyMlYzKG6P M1PUdlI1OTZ4NUC1
AC3 M{nyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjOR49KSzVyPUK1Mlkhdk1? NFz6b4MzPDF4NkWwOS=>
H82 M17kfGZ2dmO2aX;uJGF{e2G7 Ml;pN|Ahdk1? M3vOOVczKGh? NHy1bZBqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NEWwXnMzPDF4NkWwOS=>
GLC4 M1KwNmZ2dmO2aX;uJGF{e2G7 NEDlXGI{OCCwTR?= NF3w[4M4OiCq M4r5[Ilv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MknKNlQyPjZ3MEW=
H146  M4fCfGZ2dmO2aX;uJGF{e2G7 M2TFNVMxKG6P MVK3NkBp M1TVXolv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M{\ldVI1OTZ4NUC1
OVCAR-5 MmPVR4VtdCCYaXHibYxqfHliQYPzZZk> NWTESotmOC1zMECwJI5O M2D5XlczKGh? NYTPXHc4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MoLkNlM6ODBzM{[=
OVCAR-8 M{T5OmNmdGxiVnnhZoltcXS7IFHzd4F6 MlWzNE0yODByIH7N NUjpbG5YPzJiaB?= MnPpbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUKw[41lOjN7MECxN|Y>
A1847 MkL4R4VtdCCYaXHibYxqfHliQYPzZZk> MYWwMVExODBibl2= NHHCT204OiCq NETaRY1qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVGyN|kxODF|Nh?=
SKOV-3 MlnHR4VtdCCYaXHibYxqfHliQYPzZZk> NInOOpAxNTFyMECgcm0> NYnXOlh7PzJiaB?= MVjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MXiyN|kxODF|Nh?=
OVCAR-5 MlLERZBweHSxc3nzJGF{e2G7 MlPJNVAuOTByIH7N M4LQdVI1NzR6L{eyJIg> NG\sS3ZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MWqyN|kxODF|Nh?=
OVCAR-8 NX3ZcIlKSXCxcITvd4l{KEG|c3H5 M1raeVExNTFyMDDuUS=> NFXhS4szPC92OD:3NkBp NXrFOnlLcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> Ml;tNlM6ODBzM{[=
A1847 MVLBdI9xfG:|aYOgRZN{[Xl? NFTFepoyOC1zMECgcm0> NVexT3k3OjRxNEivO|IhcA>? MU\pcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MYWyN|kxODF|Nh?=
H2228 MmH5R4VtdCCYaXHibYxqfHliQYPzZZk> NX6xZmw2OC1zMECwJI5O M1vUSFczKGh? NFrzflBKSzVyPUGzJI5O M33tbFI{PTN|Mk[1
H3122 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlPqNE0yODByIH7N NEHV[no4OiCq MoTBTWM2OD1zMDDuUS=> NYjYPIh1OjN3M{OyOlU>
K008 NFO1VpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkDrTWM2OD14MDDuUS=> NWS2Sm5FOjN2MUi1NlM>
K028 NFvrb2dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHjrV3pKSzVyPUi0JI5O Mlr1NlM1OTh3MkO=
K029 MkToR4VtdCCYaXHibYxqfHliQYPzZZk> Mln0TWM2OD12NjDuUS=> M3G3R|I{PDF6NUKz
M23 MmHLR4VtdCCYaXHibYxqfHliQYPzZZk> NUXO[nlMUUN3ME2zO{42KG6P NFHvb2MzOzRzOEWyNy=>
K033 NGTMdmxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYHJR|UxRTd3LkWgcm0> NFnWU2kzOzRzOEWyNy=>
K008 M37VfWZ2dmO2aX;uJGF{e2G7 M3vNV|I2OCCwTR?= M3;iVVI1KGh? MnP6bY5lfWOnczDHNkBienKnc4S= NY[wOHBEOjN2MUi1NlM>
K028 NYnOZZo6TnWwY4Tpc44hSXO|YYm= MoTaNlUxKG6P MmnVNlQhcA>? MmPJbY5lfWOnczDHNkBienKnc4S= MUmyN|QyQDV{Mx?=
K029 MmLuSpVv[3Srb36gRZN{[Xl? M1ruTlI2OCCwTR?= Mn3QNlQhcA>? NVX1b4JscW6mdXPld{BIOSCjcoLld5Q> MXiyN|QyQDV{Mx?=
M23 MWLGeY5kfGmxbjDBd5NigQ>? NFzmRWgzPTBibl2= M3PyZlI1KGh? M1nCZYlv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 M4DjWVI{PDF6NUKz
K033 MWPGeY5kfGmxbjDBd5NigQ>? NEPYZ28zPTBibl2= NVn1fIdNOjRiaB?= MUXpcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? MlXJNlM1OTh3MkO=
K008 MU\BdI9xfG:|aYOgRZN{[Xl? M4LFV|ExOCCwTR?= NWTyXXVwPzJiaB?= MmDEd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NYHKZnZTOjN2MUi1NlM>
K028 NYXpNlhNSXCxcITvd4l{KEG|c3H5 NFvTfmsyODBibl2= NWXpT49RPzJiaB?= MoPud4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M1;EflI{PDF6NUKz
K029 M4fkTmFxd3C2b4Ppd{BCe3OjeR?= M4DDRVExOCCwTR?= NWnjZppzPzJiaB?= MWXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NU\EU5UzOjN2MUi1NlM>
M23 MmXrRZBweHSxc3nzJGF{e2G7 NHvpS4gyODBibl2= NVjn[GZ[PzJiaB?= MWPzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MlHZNlM1OTh3MkO=
K033 M13xemFxd3C2b4Ppd{BCe3OjeR?= NYTES4U2OTByIH7N MX[3NkBp NV;STJVye2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MlHJNlM1OTh3MkO=
RD MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjJTWM2OD16IH7N MUiyN|MxOzd2MR?=
Rh41 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFyLkSgcm0> MkXvNlM{ODN5NEG=
Rh18 NWTS[IdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\CTWM2OD14LkKgcm0> NEfuZoEzOzNyM{e0NS=>
Rh30 NEnNcXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe5NmRKSzVyPUWuOkBvVQ>? MmPsNlM{ODN5NEG=
BT-12 NGf1bFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH4WnFKSzVyPUG0MlMhdk1? M1;KWVI{OzB|N{Sx
CHLA-266 NXTiWmRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrzOY8{UUN3ME2yO{4yKG6P NWTodINbOjN|MEO3OFE>
TC-71 MlvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTRwNTDuUS=> NFnE[W4zOzNyM{e0NS=>
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CHLA-10 M1rndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTVwNzDuUS=> MoTjNlM{ODN5NEG=
CHLA-258 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEX5PIVKSzVyPU[uOEBvVQ>? MU[yN|MxOzd2MR?=
SJ-GBM2 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXrTWM2OD1zMj65JI5O MnTJNlM{ODN5NEG=
NB-1643 M1zISWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTdwNDDuUS=> NWTYXGZoOjN|MEO3OFE>
NB-EBc1 MofHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF4Lkigcm0> MX[yN|MxOzd2MR?=
CHLA-90 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2m3V2lEPTB;MkKuN{BvVQ>? MnHWNlM{ODN5NEG=
CHLA-136 Mn[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHRTWM2OD1{Mz6yJI5O MWGyN|MxOzd2MR?=
NALM-6 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFzLkegcm0> MYCyN|MxOzd2MR?=
COG-LL-317 Mo[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HhdmlEPTB;ND60JI5O MUGyN|MxOzd2MR?=
RS4;11 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTF|LkWgcm0> MmTvNlM{ODN5NEG=
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CCRF-CEM (1) M1u1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTF{LkWgcm0> NWXnWnV7OjN|MEO3OFE>
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Kasumi-1 M3;2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTVwODDuUS=> M3HMW|I{OzB|N{Sx
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LNCaP NH;2dGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HIVWlEPTB;ODDuUS=> MWOyN|E2OjByNB?=
VCaP NYPGcohwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP3OXBuUUN3ME23JI5O NHXje5gzOzF3MkCwOC=>
H1355 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTVibl2= MkPSNlMxOTJ{NEi=
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H460 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTBZ4hUUUN3ME24JI5O MUeyN|AyOjJ2OB?=
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HOP-62 NGX3NpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[1TWM2OD1zMTDuUS=> NHzrTmszOzBzMkK0PC=>
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H2212 Mli0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rSPGlEPTB;MUegcm0> NIrPfI0zOzBzMkK0PC=>
SK-LU-1 M4i1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF6IH7N M1W3NFI{ODF{MkS4
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COR-L23 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LuNmlEPTB;MkKgcm0> MoTmNlMxOTJ{NEi=
H727 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H5d2lEPTB;Mkigcm0> NIDYeFEzOzBzMkK0PC=>
H1734 NFPBTYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkmyTWM2OD1{ODDuUS=> NYf2eGxuOjNyMUKyOFg>
H358 NV[yNFVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:wTWM2OD1{OTDuUS=> NXX2W2JNOjNyMUKyOFg>
A549 NH\nZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoWxTWM2OD12MzDuUS=> MWqyN|AyOjJ2OB?=
H2122 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTQ[VE6UUN3ME21N{BvVQ>? NF3mTmYzOzBzMkK0PC=>
Calu-1 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHQTWM2OD13ODDuUS=> NGrvXXMzOzBzMkK0PC=>
Calu-6 NVeycHlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LBN2lEPTB;NkSgcm0> NUTtSIZ3OjNyMUKyOFg>
NCI-H1975 M{LUTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImyeHE1QCCq NHniRoRKSzVyPUG2JI5O NGftc3MzOjF2NE[2OS=>
NCI-H1975 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHuO|IhcA>? M2nnRmlEPTB;ODDuUS=> MlP3NlIyPDR4NkW=

... 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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