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 MnnIRZBweHSxc3nzJGF{e2G7 MmiwN|AwQDBxMUWwM|I2OCCwTR?= NIPxco0zPC92OD:3NkBp MofQbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NWLoWnZ3OjV6OEK1OVA>
MV411 MUTBdI9xfG:|aYOgRZN{[Xl? NUjOZ4U1OzBxOECvNVUxNzJ3MDDuUS=> MkWyNlQwPDhxN{KgbC=> NH\u[nVqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MUGyOVg5OjV3MB?=
MGC-803 NXjQdGNCS2WubDDWbYFjcWyrdImgRZN{[Xl? MX6wMlEuOTByMDDuUS=> MkTOO|IhcA>? MnLKbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NYfsTXZlOjV3OUC4NFU>
SGC-7901 M2fNfGNmdGxiVnnhZoltcXS7IFHzd4F6 NUflV4cxOC5zLUGwNFAhdk1? NUHvOG9tPzJiaB?= NInyemRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVKyOVU6ODhyNR?=
MKN-28 NIfqZnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYnoVY1zOC5zLUGwNFAhdk1? NFryNYM4OiCq NFrKbmNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NX33d5M3OjV3OUC4NFU>
MGC-803 M1XWRWZ2dmO2aX;uJGF{e2G7 MXqwMlEuOTByMDDuUS=> M1zvUlI1KGh? M1fBfIlv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? MljKNlU2QTB6MEW=
HCT-116 MmfFSpVv[3Srb36gRZN{[Xl? Mnv2OVBvVQ>? M4fCTFI1KGh? NUD1[GdrTE2VTx?= MXTpcoR2[2WmIFewM2cyKGG{cnXzeC=> NF;HfWwzPTJzMEe5OC=>
HT-29 MUHGeY5kfGmxbjDBd5NigQ>? NXP2ZmVLPTCwTR?= NWrJV3M{OjRiaB?= NEDyfoJFVVOR MY\pcoR2[2WmIFewM2cyKGG{cnXzeC=> M{H0eFI2OjFyN{m0
SCC25 NECxNZNEgXSxeHnjbZR6KEG|c3H5 NFTvc5MyOC93MDDuUS=> M4HPNFI1KGh? NFPj[|Vl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MXiyOVIxPTR|MB?=
FUDA MYXDfZRwgGmlaYT5JGF{e2G7 M4LyVlExNzVyIH7N NFv2UnIzPCCq NVrmSGR5\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NHLKN4YzPTJyNUSzNC=>
Detroit562 M2\HTWN6fG:6aXPpeJkhSXO|YYm= NHT2RooyOC93MDDuUS=> NUL6XJRXOjRiaB?= M3rX[YRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M3vqbFI2OjB3NEOw
CAL27 NInudIlEgXSxeHnjbZR6KEG|c3H5 NIX0VlUyOC93MDDuUS=> NEPs[WwzPCCq MVLk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MX2yOVIxPTR|MB?=
DSH1 NVPCNI9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGraTGtKSzVyPU[gcm0> NWnlPFdWOjR5OES4N|k>
SW-1710 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C1R2lEPTB;NjDuUS=> M2q0OlI1Pzh2OEO5
T24 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjmO3RKSzVyPUegcm0> MVeyOFc5PDh|OR?=
RT112 MkW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzxTWM2OD17IH7N MYCyOFc5PDh|OR?=
639-V Mne5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFyIH7N MYGyOFc5PDh|OR?=
SCaBER NUHDSFlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljDTWM2OD1zMDDuUS=> NHnSWXAzPDd6NEizPS=>
BFTC MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF5IH7N MlX5NlQ4QDR6M{m=
J82 M{XJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3aepl3UUN3ME2xPEBvVQ>? NXu0RVN6OjR5OES4N|k>
HT-1376 MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJzIH7N NFfFeoszPDd6NEizPS=>
647-V M2PFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTJ5IH7N MnXMNlQ4QDR6M{m=
UM-UC3 MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTN|IH7N NFf4d4QzPDd6NEizPS=>
LB831-BLC NHjTdXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vDTmlEPTB;M{Sgcm0> M4XkdlI1Pzh2OEO5
KU-19-19 NFewZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXISIhKSzVyPUO2JI5O NWfKZXZjOjR5OES4N|k>
35612 NGnaNphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTN6IH7N NXvuN|FQOjR5OES4N|k>
5637 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPvTWM2OD12NDDuUS=> MWWyOFc5PDh|OR?=
HT-1197 M{fDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHjXoRWUUN3ME21N{BvVQ>? MkjyNlQ4QDR6M{m=
MGH-U3 M1rifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfKVGpKSzVyPUWzJI5O NWLSU4hwOjR5OES4N|k>
TCCSUP MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTUTWM2OD1zNEKgcm0> Mkm3NlQ4QDR6M{m=
RT4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKxTWM2OD1zN{OzJI5O M4n4UFI1Pzh2OEO5
SW780 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTN2NUGgcm0> NYLSfFV2OjR5OES4N|k>
RKO NXyzNGNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\rTWM2OD12IH7N MYmyOFY5Ojd2Nx?=
LS-411 N NVLsboJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPUVmhKSzVyPUWgcm0> MnzENlQ3QDJ5NEe=
SW620 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLvTWM2OD16IH7N NWXUe2hsOjR4OEK3OFc>
HCT-15 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRThibl2= MoPrNlQ3QDJ5NEe=
HuTu-80 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7KNGszUUN3ME2xN{BvVQ>? NVTse5ZNOjR4OEK3OFc>
HCT 116 M{fYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rW[mlEPTB;MUSgcm0> NF;u[lczPDZ6Mke0Oy=>
COLO-205 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni1TWM2OD1zNDDuUS=> M4O2blI1Pjh{N{S3
NCI-H747 NI[1[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF5IH7N NH;aUVQzPDZ6Mke0Oy=>
COLO-678 NILZWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DrUWlEPTB;MkGgcm0> NYXDSFZ1OjR4OEK3OFc>
LoVo MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ{IH7N M{L1S|I1Pjh{N{S3
LS-1034 M3nKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfibGpKSzVyPUOxJI5O NFjoc3gzPDZ6Mke0Oy=>
SNU-C2B M1f3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO5Z5RXUUN3ME20OUBvVQ>? MY[yOFY5Ojd2Nx?=
LS-123 NF\3V|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrEWHVEUUN3ME23N{BvVQ>? M1z1ZlI1Pjh{N{S3
SK-CO-1 NYL3[VN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTETWM2OD16MTDuUS=> NU[4clI{OjR4OEK3OFc>
HCC2998 NFTtOoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETTXHVKSzVyPUGyPEBvVQ>? M3PmRlI1Pjh{N{S3
MDA-MB-231 MUPGeY5kfGmxbjDBd5NigQ>? NYDL[3g{OTByIH7N NW\FWWdUOzBibXnu MV3pcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? M{TqO|I1OjR6Mk[1
MDA-MB-435 NXi1fnFJTnWwY4Tpc44hSXO|YYm= NIXPXmEyODBibl2= NXPp[HZzOzBibXnu MYXpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? M4XHOVI1OjR6Mk[1
BT-20  MnH5SpVv[3Srb36gRZN{[Xl? NWrnRodHOTByL{K1NEBvVQ>? NVLKcnVoOjRiaB?= NHnwU|hz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? NIfEdWkzPDF5M{W0NS=>
MDA-MB-231 MonvSpVv[3Srb36gRZN{[Xl? NUnv[XhYOTByIH7N MW[yOEBp NEfEZ3VqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh M2S4U|I1OTd|NUSx
H82 NGjLdWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS0TWM2OD1|MD6yO{BvVQ>? MWmyOFE3PjVyNR?=
GLC4 NV7CbpJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPiSWFKSzVyPUKwMlQ4KG6P NEnVPGczPDF4NkWwOS=>
H69 NGDobJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP0VXdWUUN3ME24N{4{PiCwTR?= M{n5WlI1OTZ4NUC1
H128 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPDTWM2OD14OT61OUBvVQ>? MV6yOFE3PjVyNR?=
H146 NFux[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXHfYQ{UUN3ME2yPE42OSCwTR?= Ml\GNlQyPjZ3MEW=
H187 NFnsd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7pbVl2UUN3ME2yOE46QSCwTR?= MYqyOFE3PjVyNR?=
H526 M3PUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP3UnRKSzVyPUKxMlY1KG6P NFS2VJIzPDF4NkWwOS=>
N592 M4nhXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDMTWM2OD1zND6xNkBvVQ>? NXLt[odQOjRzNk[1NFU>
H620 NELET3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzrTWM2OD1|Mj62O{BvVQ>? MXyyOFE3PjVyNR?=
H792 NHLrfmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4S5TGlEPTB;NEWuNFchdk1? MYOyOFE3PjVyNR?=
H1173 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjq[ldKSzVyPUGyMlYzKG6P NGPXcXAzPDF4NkWwOS=>
AC3 M1\1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r3bWlEPTB;MkWuPUBvVQ>? M4fWSlI1OTZ4NUC1
H82 NYjTU442TnWwY4Tpc44hSXO|YYm= NYjaTYs6OzBibl2= MYq3NkBp MUTpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NH\BS2MzPDF4NkWwOS=>
GLC4 NEXONmtHfW6ldHnvckBCe3OjeR?= M1ywZVMxKG6P MWG3NkBp NYrtR5JVcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NXnaUHNROjRzNk[1NFU>
H146  NH:0bVJHfW6ldHnvckBCe3OjeR?= MUSzNEBvVQ>? NILvXpQ4OiCq M1LVOYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NEjEeHAzPDF4NkWwOS=>
OVCAR-5 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXSwMVExODBibl2= M1v4N|czKGh? M13ZfYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NEK1PI4zOzlyMEGzOi=>
OVCAR-8 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnSyNE0yODByIH7N Ml\jO|IhcA>? NILZdodqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NF\OWo0zOzlyMEGzOi=>
A1847 NGfKNG5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXewMVExODBibl2= MW[3NkBp M2POU4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWr0SnZLOjN7MECxN|Y>
SKOV-3 NGrMfndE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHLTbHQxNTFyMECgcm0> NEj6[o84OiCq M2LTNYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MVWyN|kxODF|Nh?=
OVCAR-5 MWTBdI9xfG:|aYOgRZN{[Xl? Mk\uNVAuOTByIH7N M4fLNFI1NzR6L{eyJIg> Mn6wbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NFjZdmgzOzlyMEGzOi=>
OVCAR-8 M4XXfmFxd3C2b4Ppd{BCe3OjeR?= NVXYN2FJOTBvMUCwJI5O MXmyOE81QC95MjDo MXvpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 M2SyNFI{QTByMUO2
A1847 MV\BdI9xfG:|aYOgRZN{[Xl? MXmxNE0yODBibl2= NV74NY1SOjRxNEivO|IhcA>? MWrpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 NVnLRZVwOjN7MECxN|Y>
H2228 NIjNPHVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4WyVFAuOTByMDDuUS=> NWHidXZkPzJiaB?= NXPCTIlFUUN3ME2xN{BvVQ>? NUfmW4NsOjN3M{OyOlU>
H3122 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mo\yNE0yODByIH7N MV23NkBp NVjvZYVrUUN3ME2xNEBvVQ>? M{HybFI{PTN|Mk[1
K008 NIHGNlBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV\JR|UxRTZyIH7N M{PUU|I{PDF6NUKz
K028 M371UGNmdGxiVnnhZoltcXS7IFHzd4F6 MVvJR|UxRTh2IH7N MnG5NlM1OTh3MkO=
K029 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MX7JR|UxRTR4IH7N NH7EWIQzOzRzOEWyNy=>
M23 NVTDXmRqS2WubDDWbYFjcWyrdImgRZN{[Xl? NETZdoVKSzVyPUO3MlUhdk1? M4TEZ|I{PDF6NUKz
K033 NWfhZXlGS2WubDDWbYFjcWyrdImgRZN{[Xl? NYnZNnpYUUN3ME23OU42KG6P NYfrZ|l[OjN2MUi1NlM>
K008 MXzGeY5kfGmxbjDBd5NigQ>? MU[yOVAhdk1? NHP3OWIzPCCq NFv6NGJqdmS3Y3XzJGczKGG{cnXzeC=> NUe1Rot2OjN2MUi1NlM>
K028 M4HoVWZ2dmO2aX;uJGF{e2G7 M3fhNlI2OCCwTR?= NUTzOWlROjRiaB?= NX\lcXdJcW6mdXPld{BIOiCjcoLld5Q> NV3OTVIzOjN2MUi1NlM>
K029 Ml;5SpVv[3Srb36gRZN{[Xl? MWWyOVAhdk1? NYLLWodsOjRiaB?= NX3m[IExcW6mdXPld{BIOSCjcoLld5Q> MX[yN|QyQDV{Mx?=
M23 M3LpemZ2dmO2aX;uJGF{e2G7 MVGyOVAhdk1? MW[yOEBp MlLObY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= MV:yN|QyQDV{Mx?=
K033 NWL0Z2ZXTnWwY4Tpc44hSXO|YYm= M3\1UFI2OCCwTR?= MmPwNlQhcA>? NXPXd2V3cW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u NV3uOXF1OjN2MUi1NlM>
K008 NXTDV3FLSXCxcITvd4l{KEG|c3H5 MV6xNFAhdk1? NFrBdHc4OiCq NUHTO457e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= M1e1RlI{PDF6NUKz
K028 NVXOcJQxSXCxcITvd4l{KEG|c3H5 MnTVNVAxKG6P M{\aTVczKGh? MmD1d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? Mo\2NlM1OTh3MkO=
K029 MUjBdI9xfG:|aYOgRZN{[Xl? NED1NWUyODBibl2= MYm3NkBp MWHzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MVeyN|QyQDV{Mx?=
M23 M1\WXWFxd3C2b4Ppd{BCe3OjeR?= MYCxNFAhdk1? MXu3NkBp MYLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NHLzXFMzOzRzOEWyNy=>
K033 NIe3cGJCeG:ydH;zbZMhSXO|YYm= M37ze|ExOCCwTR?= M2LkTlczKGh? MmG1d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? Mki5NlM1OTh3MkO=
RD MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6xTWM2OD16IH7N NUDBZ4R{OjN|MEO3OFE>
Rh41 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFyLkSgcm0> MkX4NlM{ODN5NEG=
Rh18 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\3[2lEPTB;Nj6yJI5O Mk\QNlM{ODN5NEG=
Rh30 NGTwe3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLxTWM2OD13Lk[gcm0> NX3wW5lCOjN|MEO3OFE>
BT-12 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrPbY1iUUN3ME2xOE4{KG6P M1vJelI{OzB|N{Sx
CHLA-266 M3;j[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[5TWM2OD1{Nz6xJI5O NH\TVnAzOzNyM{e0NS=>
TC-71 MkfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHB[GcyUUN3ME20MlUhdk1? MVmyN|MxOzd2MR?=
CHLA-9 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33Ub2lEPTB;ND62JI5O Ml;PNlM{ODN5NEG=
CHLA-10 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZT2lEPTB;NT63JI5O M1PZcVI{OzB|N{Sx
CHLA-258 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLDPYtKSzVyPU[uOEBvVQ>? NULoS4g5OjN|MEO3OFE>
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NB-1643 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\0SIdrUUN3ME23MlQhdk1? MYWyN|MxOzd2MR?=
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CHLA-90 MnTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJ{LkOgcm0> M2TqfFI{OzB|N{Sx
CHLA-136 NF\CSohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJ|LkKgcm0> MUOyN|MxOzd2MR?=
NALM-6 NIXYRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\BNGlEPTB;MUGuO{BvVQ>? MVOyN|MxOzd2MR?=
COG-LL-317 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTRwNDDuUS=> MmOyNlM{ODN5NEG=
RS4;11 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrONlJKSzVyPUGzMlUhdk1? NEfaVlYzOzNyM{e0NS=>
MOLT-4 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLsTWM2OD1zMD62JI5O M1zobVI{OzB|N{Sx
CCRF-CEM (1) NEHoSG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmW2TWM2OD1zMj61JI5O NHzydnIzOzNyM{e0NS=>
CCRF-CEM (2) NHywXm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTdwMjDuUS=> MoHoNlM{ODN5NEG=
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LNCaP M2njcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRThibl2= MUeyN|E2OjByNB?=
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H1355 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfGR4lJUUN3ME21JI5O NFPOd3czOzBzMkK0PC=>
H157 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;TSlVKSzVyPUegcm0> NF24OHAzOzBzMkK0PC=>
H460 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{SyVWlEPTB;ODDuUS=> NIraT5QzOzBzMkK0PC=>
IA-LM NGf4fYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC0XZlKSzVyPUGwJI5O MlrUNlMxOTJ{NEi=
HOP-62 NX\5dHI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnxO2liUUN3ME2xNUBvVQ>? NEnXZ4wzOzBzMkK0PC=>
H23 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnQXFRNUUN3ME2xNUBvVQ>? MXiyN|AyOjJ2OB?=
H2030 Mn62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF{IH7N NVjSeZMzOjNyMUKyOFg>
H441 MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37YU2lEPTB;MUSgcm0> M4X5[|I{ODF{MkS4
H2212 M{HuWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXzOnJKSzVyPUG3JI5O NW\2ZpQ4OjNyMUKyOFg>
SK-LU-1 NYfnenpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHSN|FKSzVyPUG4JI5O MoTENlMxOTJ{NEi=
H2009 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnKTWM2OD1zOTDuUS=> M4TpRVI{ODF{MkS4
H1792 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3RTWM2OD1{MDDuUS=> MVeyN|AyOjJ2OB?=
COR-L23 MknnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknHTWM2OD1{MjDuUS=> NX;ZUGpCOjNyMUKyOFg>
H727 Mn[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:2[pFkUUN3ME2yPEBvVQ>? MlHYNlMxOTJ{NEi=
H1734 NXLkRmZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrR[45XUUN3ME2yPEBvVQ>? M3TkVVI{ODF{MkS4
H358 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rZdmlEPTB;Mkmgcm0> NFvoW5YzOzBzMkK0PC=>
A549 NUXPbGd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fOPGlEPTB;NEOgcm0> NYDzNYZOOjNyMUKyOFg>
H2122 M1rnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfZNoF1UUN3ME21N{BvVQ>? NVi2NI5WOjNyMUKyOFg>
Calu-1 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTV6IH7N NYHQT3BUOjNyMUKyOFg>
Calu-6 MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfjN5F{UUN3ME22OEBvVQ>? MoDXNlMxOTJ{NEi=
NCI-H1975 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjoSZA3PDhiaB?= MYLJR|UxRTF4IH7N M4i1OVIzOTR2Nk[1
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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

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)

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。

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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