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)

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 NHXSRpNCeG:ydH;zbZMhSXO|YYm= NIT0W5c{OC96MD:xOVAwOjVyIH7N NFrPRWkzPC92OD:3NkBp MXvpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= MoPCNlU5QDJ3NUC=
MV411 NHTXVHNCeG:ydH;zbZMhSXO|YYm= MnPCN|AwQDBxMUWwM|I2OCCwTR?= NGnQXVUzPC92OD:3NkBp MoGzbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MmrINlU5QDJ3NUC=
MGC-803 NUfLRodPS2WubDDWbYFjcWyrdImgRZN{[Xl? NGrkeIkxNjFvMUCwNEBvVQ>? MoXXO|IhcA>? M3nXR4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmnwNlU2QTB6MEW=
SGC-7901 NGXmboRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXHXTW5iOC5zLUGwNFAhdk1? MX63NkBp NY\U[XZUcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NH7LeFMzPTV7MEiwOS=>
MKN-28 NGPnS3VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MU[wMlEuOTByMDDuUS=> MkPjO|IhcA>? NWLxcYZ1cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYDnW25{OjV3OUC4NFU>
MGC-803 MWHGeY5kfGmxbjDBd5NigQ>? MnXqNE4yNTFyMECgcm0> MYSyOEBp NHPHW4xqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? M4jZZ|I2PTlyOEC1
HCT-116 MmGzSpVv[3Srb36gRZN{[Xl? MnfBOVBvVQ>? MkfENlQhcA>? NHXwNYJFVVOR MUTpcoR2[2WmIFewM2cyKGG{cnXzeC=> Ml24NlUzOTB5OUS=
HT-29 NHXUXHFHfW6ldHnvckBCe3OjeR?= M2Oy[|Uxdk1? MnPnNlQhcA>? MYfEUXNQ NXfCfFhXcW6mdXPl[EBIOC:JMTDhdpJme3R? MVuyOVIyODd7NB?=
SCC25 NVPibnB1S3m2b4jpZ4l1gSCDc4PhfS=> MmHSNVAwPTBibl2= MknyNlQhcA>? NXnifHpk\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MWKyOVIxPTR|MB?=
FUDA NYPh[FNJS3m2b4jpZ4l1gSCDc4PhfS=> MWGxNE82OCCwTR?= MWGyOEBp MnTW[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M124clI2OjB3NEOw
Detroit562 M4rlW2N6fG:6aXPpeJkhSXO|YYm= NVvi[phrOTBxNUCgcm0> M3rSTlI1KGh? NEHRZZNl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NH;Pc2QzPTJyNUSzNC=>
CAL27 MkDzR5l1d3irY3n0fUBCe3OjeR?= NVPmZYd[OTBxNUCgcm0> NX6xbGRwOjRiaB?= M4WyVoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MYmyOVIxPTR|MB?=
DSH1 NUfxUHNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe0dFk1UUN3ME22JI5O NWLlV3Z5OjR5OES4N|k>
SW-1710 NHewdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3raOGlEPTB;NjDuUS=> NFW1cGUzPDd6NEizPS=>
T24 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTdibl2= M17ufVI1Pzh2OEO5
RT112 NWLqfJZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorDTWM2OD17IH7N NYrkSHZuOjR5OES4N|k>
639-V M4W1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDJTWM2OD1zMDDuUS=> M33MelI1Pzh2OEO5
SCaBER NInCbZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nWdWlEPTB;MUCgcm0> M4jGVVI1Pzh2OEO5
BFTC M2jFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO2TWM2OD1zNzDuUS=> NW\HdZh5OjR5OES4N|k>
J82 NV;YSYFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfJTWM2OD1zODDuUS=> M1\zflI1Pzh2OEO5
HT-1376 NYTWUoI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf6[3ZSUUN3ME2yNUBvVQ>? M1z1XVI1Pzh2OEO5
647-V M4X1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP0TWM2OD1{NzDuUS=> MlPZNlQ4QDR6M{m=
UM-UC3 NYTLOZduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfXTWM2OD1|MzDuUS=> M{TCUVI1Pzh2OEO5
LB831-BLC MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTN2IH7N NEP3N3AzPDd6NEizPS=>
KU-19-19 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m5RWlEPTB;M{[gcm0> NH7jfW4zPDd6NEizPS=>
35612 NEe5fY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnntTWM2OD1|ODDuUS=> MnfENlQ4QDR6M{m=
5637 NV3xO2xTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHmTWM2OD12NDDuUS=> MVKyOFc5PDh|OR?=
HT-1197 NXrPXJNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjl[IhKSzVyPUWzJI5O MXWyOFc5PDh|OR?=
MGH-U3 MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDJUohKSzVyPUWzJI5O MWiyOFc5PDh|OR?=
TCCSUP MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPHTWM2OD1zNEKgcm0> MnG5NlQ4QDR6M{m=
RT4 NUm2UXJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHOzV29KSzVyPUG3N|Mhdk1? NWXZTGJKOjR5OES4N|k>
SW780 NGjXcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nkSmlEPTB;M{S1NUBvVQ>? NHX0XlAzPDd6NEizPS=>
RKO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S3VGlEPTB;NDDuUS=> M3TtWVI1Pjh{N{S3
LS-411 N M1ewT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r4[mlEPTB;NTDuUS=> NEjxSmYzPDZ6Mke0Oy=>
SW620 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LNNGlEPTB;ODDuUS=> MorFNlQ3QDJ5NEe=
HCT-15 NWfWbFBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRThibl2= MWeyOFY5Ojd2Nx?=
HuTu-80 NInJSo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTF|IH7N NFSyN4czPDZ6Mke0Oy=>
HCT 116 NXj0WZFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTF2IH7N MVyyOFY5Ojd2Nx?=
COLO-205 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\xN2lEPTB;MUSgcm0> MX6yOFY5Ojd2Nx?=
NCI-H747 NUTpeXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLCdnFKSzVyPUG3JI5O MV6yOFY5Ojd2Nx?=
COLO-678 NYHKNng4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\3OG5MUUN3ME2yNUBvVQ>? NGD5[|QzPDZ6Mke0Oy=>
LoVo MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLrTY1MUUN3ME2yNkBvVQ>? NYO5PHg{OjR4OEK3OFc>
LS-1034 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOxO2NWUUN3ME2zNUBvVQ>? NW\zT29COjR4OEK3OFc>
SNU-C2B NH\LWYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR3IH7N M1\6V|I1Pjh{N{S3
LS-123 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjpNIJxUUN3ME23N{BvVQ>? MXqyOFY5Ojd2Nx?=
SK-CO-1 MoL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni4TWM2OD16MTDuUS=> MonKNlQ3QDJ5NEe=
HCC2998 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF{ODDuUS=> M1nxPFI1Pjh{N{S3
MDA-MB-231 M1z1dGZ2dmO2aX;uJGF{e2G7 MoD2NVAxKG6P NV;hepZ4OzBibXnu M3\wWIlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z Mo\VNlQzPDh{NkW=
MDA-MB-435 M4SzPWZ2dmO2aX;uJGF{e2G7 Mm[zNVAxKG6P NHPp[5o{OCCvaX6= MWHpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? M16yNVI1OjR6Mk[1
BT-20  MX\GeY5kfGmxbjDBd5NigQ>? NF75[W8yODBxMkWwJI5O MlSzNlQhcA>? NFu4epZz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? NWDVW2pSOjRzN{O1OFE>
MDA-MB-231 M{jOe2Z2dmO2aX;uJGF{e2G7 NGrxRncyODBibl2= NVnuSGhMOjRiaB?= MVXpcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg M13ERVI1OTd|NUSx
H82 NYTNVoxiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnlRYZoUUN3ME2zNE4zPyCwTR?= MYKyOFE3PjVyNR?=
GLC4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe3OVVvUUN3ME2yNE41PyCwTR?= NYfa[Vd1OjRzNk[1NFU>
H69 M3rMZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\jTWM2OD16Mz6zOkBvVQ>? MmTlNlQyPjZ3MEW=
H128 NGjx[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjzNnB5UUN3ME22PU42PSCwTR?= M3vmb|I1OTZ4NUC1
H146 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LQdWlEPTB;MkiuOVEhdk1? MmSzNlQyPjZ3MEW=
H187 Mm\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfhV4NlUUN3ME2yOE46QSCwTR?= NF\McIczPDF4NkWwOS=>
H526 NFjJV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjMZphKSzVyPUKxMlY1KG6P M4XUWVI1OTZ4NUC1
N592 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF2LkGyJI5O NWXXSJZQOjRzNk[1NFU>
H620 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rYfWlEPTB;M{KuOlchdk1? M1nrS|I1OTZ4NUC1
H792 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy4bGlKSzVyPUS1MlA4KG6P MX6yOFE3PjVyNR?=
H1173 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF{Lk[yJI5O M1:5fVI1OTZ4NUC1
AC3 NYnz[lljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nnNmlEPTB;MkWuPUBvVQ>? MlvtNlQyPjZ3MEW=
H82 M1TseWZ2dmO2aX;uJGF{e2G7 NGPTcZQ{OCCwTR?= NV;qOHl[PzJiaB?= NHHyWlJqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NXLPe3FJOjRzNk[1NFU>
GLC4 MX3GeY5kfGmxbjDBd5NigQ>? NF;xNVE{OCCwTR?= NGTKdoM4OiCq NVLDPWhUcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NYDUfG9iOjRzNk[1NFU>
H146  NUDhU3NzTnWwY4Tpc44hSXO|YYm= M1ju[FMxKG6P MV63NkBp NGfsSVFqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> Mm\YNlQyPjZ3MEW=
OVCAR-5 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1XqVVAuOTByMDDuUS=> MlTXO|IhcA>? NGX1NGtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWH5OHhEOjN7MECxN|Y>
OVCAR-8 NYrkbGc6S2WubDDWbYFjcWyrdImgRZN{[Xl? M2fyb|AuOTByMDDuUS=> M2T2[VczKGh? MWTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2ToV|I{QTByMUO2
A1847 M1XCOGNmdGxiVnnhZoltcXS7IFHzd4F6 M4TBd|AuOTByMDDuUS=> NGfqSFk4OiCq MVLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYKyN|kxODF|Nh?=
SKOV-3 NUX2SZNQS2WubDDWbYFjcWyrdImgRZN{[Xl? MnXlNE0yODByIH7N M1PnXlczKGh? NFz4O2FqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoOyNlM6ODBzM{[=
OVCAR-5 M4\TVmFxd3C2b4Ppd{BCe3OjeR?= NIP6VXYyOC1zMECgcm0> MnvTNlQwPDhxN{KgbC=> MlGzbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MVyyN|kxODF|Nh?=
OVCAR-8 Mnz0RZBweHSxc3nzJGF{e2G7 Mo\1NVAuOTByIH7N MVeyOE81QC95MjDo MVPpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 M{DpR|I{QTByMUO2
A1847 NXPTWIlUSXCxcITvd4l{KEG|c3H5 M2nxRlExNTFyMDDuUS=> M2TrNVI1NzR6L{eyJIg> NF3VXGtqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MWeyN|kxODF|Nh?=
H2228 M2XhTmNmdGxiVnnhZoltcXS7IFHzd4F6 NXW0cWpUOC1zMECwJI5O NX3pW49[PzJiaB?= M3XTNGlEPTB;MUOgcm0> NXPafGVDOjN3M{OyOlU>
H3122 NYLWdmp6S2WubDDWbYFjcWyrdImgRZN{[Xl? MV[wMVExODBibl2= MmnVO|IhcA>? MmLwTWM2OD1zMDDuUS=> NWPLfZRFOjN3M{OyOlU>
K008 NEewZYlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3fEWGlEPTB;NkCgcm0> NHzkT|IzOzRzOEWyNy=>
K028 Mmq1R4VtdCCYaXHibYxqfHliQYPzZZk> MWjJR|UxRTh2IH7N Mmm0NlM1OTh3MkO=
K029 M2\TSmNmdGxiVnnhZoltcXS7IFHzd4F6 NYDtUVlDUUN3ME20OkBvVQ>? MWCyN|QyQDV{Mx?=
M23 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYKzTIFMUUN3ME2zO{42KG6P NFTS[2ozOzRzOEWyNy=>
K033 NFXyS2tE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3nPNWlEPTB;N{WuOUBvVQ>? M3fMXVI{PDF6NUKz
K008 MY\GeY5kfGmxbjDBd5NigQ>? NEf2XmkzPTBibl2= NVW1[5lZOjRiaB?= NGXRbVBqdmS3Y3XzJGczKGG{cnXzeC=> M{TWV|I{PDF6NUKz
K028 NVPIPGd2TnWwY4Tpc44hSXO|YYm= NXrHenRmOjVyIH7N NGPDeZQzPCCq Mlq2bY5lfWOnczDHNkBienKnc4S= NVzvOotLOjN2MUi1NlM>
K029 M3:3XmZ2dmO2aX;uJGF{e2G7 MX[yOVAhdk1? Mn7tNlQhcA>? NXn5flBjcW6mdXPld{BIOSCjcoLld5Q> NVHlPWoxOjN2MUi1NlM>
M23 NHTq[pBHfW6ldHnvckBCe3OjeR?= NYfBTYpiOjVyIH7N M1HMPVI1KGh? M37XfYlv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 NFn6c2czOzRzOEWyNy=>
K033 M4Pjd2Z2dmO2aX;uJGF{e2G7 M4roO|I2OCCwTR?= MoTwNlQhcA>? MmeybY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w MWWyN|QyQDV{Mx?=
K008 M3XlU2Fxd3C2b4Ppd{BCe3OjeR?= M4rSbFExOCCwTR?= Mm\QO|IhcA>? NFrZdo1{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NYT6OW9sOjN2MUi1NlM>
K028 MmPFRZBweHSxc3nzJGF{e2G7 MVexNFAhdk1? Mn;MO|IhcA>? MVnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M3K4[lI{PDF6NUKz
K029 M{PpbGFxd3C2b4Ppd{BCe3OjeR?= MkHxNVAxKG6P MnW5O|IhcA>? M1e5O5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M3rNO|I{PDF6NUKz
M23 MVXBdI9xfG:|aYOgRZN{[Xl? MkTpNVAxKG6P MY[3NkBp M4Xoc5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NFzCT20zOzRzOEWyNy=>
K033 MVfBdI9xfG:|aYOgRZN{[Xl? NXflVpRPOTByIH7N M3TjZ|czKGh? NFO2[3R{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NH\1XXUzOzRzOEWyNy=>
RD M2LJcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonlTWM2OD16IH7N M3\GZ|I{OzB|N{Sx
Rh41 Ml;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHXTWM2OD1zMD60JI5O MUCyN|MxOzd2MR?=
Rh18 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;BeGlEPTB;Nj6yJI5O MVGyN|MxOzd2MR?=
Rh30 NYSxd5d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3n[|FKSzVyPUWuOkBvVQ>? NWqzdmFQOjN|MEO3OFE>
BT-12 M1rXdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rO[2lEPTB;MUSuN{BvVQ>? NGHFRYUzOzNyM{e0NS=>
CHLA-266 M1zLfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ5LkGgcm0> MYiyN|MxOzd2MR?=
TC-71 M13ocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1m0RWlEPTB;ND61JI5O NH:2PJgzOzNyM{e0NS=>
CHLA-9 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LYfGlEPTB;ND62JI5O NETiZXgzOzNyM{e0NS=>
CHLA-10 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nlSmlEPTB;NT63JI5O Ml;aNlM{ODN5NEG=
CHLA-258 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnFPZhTUUN3ME22MlQhdk1? NUDxVFJnOjN|MEO3OFE>
SJ-GBM2 M{Xnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL2TWM2OD1zMj65JI5O NHrYU5ozOzNyM{e0NS=>
NB-1643 M3zKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHQbndCUUN3ME23MlQhdk1? NEDOfHYzOzNyM{e0NS=>
NB-EBc1 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF4Lkigcm0> M3rzelI{OzB|N{Sx
CHLA-90 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDnZ5NKSzVyPUKyMlMhdk1? MUCyN|MxOzd2MR?=
CHLA-136 NIDXZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jpeWlEPTB;MkOuNkBvVQ>? MWWyN|MxOzd2MR?=
NALM-6 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvveoZKSzVyPUGxMlchdk1? NEjoTmIzOzNyM{e0NS=>
COG-LL-317 M4rQeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzHTWM2OD12LkSgcm0> MlT4NlM{ODN5NEG=
RS4;11 NUTDephJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH3NWxKSzVyPUGzMlUhdk1? NETYeWEzOzNyM{e0NS=>
MOLT-4 NEKySmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P2UGlEPTB;MUCuOkBvVQ>? NVmyXoZyOjN|MEO3OFE>
CCRF-CEM (1) MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rveGlEPTB;MUKuOUBvVQ>? NYTEdYQ4OjN|MEO3OFE>
CCRF-CEM (2) MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXQ[FdKSzVyPUeuNkBvVQ>? NYnxVoVNOjN|MEO3OFE>
Kasumi-1 MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfV[4NKSzVyPUWuPEBvVQ>? MlK1NlM{ODN5NEG=
Karpas-299 NEKxVoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj4WGJKSzVyPUmuOkBvVQ>? NVHnTllLOjN|MEO3OFE>
Ramos-RA1 MmjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTdwNDDuUS=> NGPaO|kzOzNyM{e0NS=>
LNCaP MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr4VodKSzVyPUigcm0> NH7RXoozOzF3MkCwOC=>
VCaP NIfsSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\BSJpKSzVyPUegcm0> MmjTNlMyPTJyMES=
H1355 NV\DWJE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:wTWM2OD13IH7N NEDYXZkzOzBzMkK0PC=>
H157 M1rWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq3TWM2OD15IH7N MWKyN|AyOjJ2OB?=
H460 NV22d4ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D4fmlEPTB;ODDuUS=> M1f4TVI{ODF{MkS4
IA-LM MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHPTWM2OD1zMDDuUS=> NHXwTnAzOzBzMkK0PC=>
HOP-62 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXUcVlKSzVyPUGxJI5O NHjjdnEzOzBzMkK0PC=>
H23 MnjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTFzIH7N NFyzU3gzOzBzMkK0PC=>
H2030 MnTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfWTWM2OD1zMjDuUS=> MnXoNlMxOTJ{NEi=
H441 NUTue2p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn2c4Y2UUN3ME2xOEBvVQ>? MVWyN|AyOjJ2OB?=
H2212 NHvCU3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF5IH7N M4q1c|I{ODF{MkS4
SK-LU-1 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XUZmlEPTB;MUigcm0> NH7DTI4zOzBzMkK0PC=>
H2009 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\yWHBJUUN3ME2xPUBvVQ>? M1rjOVI{ODF{MkS4
H1792 MoPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:3UZlYUUN3ME2yNEBvVQ>? NEXKdYozOzBzMkK0PC=>
COR-L23 NXizXmJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPnV2hKSzVyPUKyJI5O M{TQU|I{ODF{MkS4
H727 NYPrT|ZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fidGlEPTB;Mkigcm0> MlPNNlMxOTJ{NEi=
H1734 MmLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\6TWM2OD1{ODDuUS=> MXOyN|AyOjJ2OB?=
H358 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJ7IH7N MnvWNlMxOTJ{NEi=
A549 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nacmlEPTB;NEOgcm0> NVLMO|R7OjNyMUKyOFg>
H2122 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DEV2lEPTB;NUOgcm0> NXX6NXRqOjNyMUKyOFg>
Calu-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fiWmlEPTB;NUigcm0> M4W3XFI{ODF{MkS4
Calu-6 NHPnWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPDTWM2OD14NDDuUS=> MV6yN|AyOjJ2OB?=
NCI-H1975 M2HLbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGzV5c1QCCq NEPMd5dKSzVyPUG2JI5O MknlNlIyPDR4NkW=
NCI-H1975 NYLBUIp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrNZmpTPzJiaB?= Mmr0TWM2OD16IH7N MXqyNlE1PDZ4NR?=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 (6)

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。

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は1種のパン(pan)- HSP 阻害剤で、誘導HSPsの合成(HSP105、 HSP72,と HSP40を含める)を抑制します。

  • 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

    Geldanamycinは一種の天然なHSP90阻害剤で、Kd値が1.2μMですが、糖質ステロイド受容体(GR)/HSP連合を特異性的に妨害します。

  • 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