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 NUTodJh1SXCxcITvd4l{KEG|c3H5 NIW3XJA{OC96MD:xOVAwOjVyIH7N MmT2NlQwPDhxN{KgbC=> MWPpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= NWftOmpmOjV6OEK1OVA>
MV411 NW\vcmVNSXCxcITvd4l{KEG|c3H5 NVzMVJBwOzBxOECvNVUxNzJ3MDDuUS=> MnrVNlQwPDhxN{KgbC=> M2n3SYlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NX7pPIU{OjV6OEK1OVA>
MGC-803 NWfSOGM3S2WubDDWbYFjcWyrdImgRZN{[Xl? M360SVAvOS1zMECwJI5O NVrNbmNWPzJiaB?= M3H1SolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NW\ZVW5EOjV3OUC4NFU>
SGC-7901 M4n2V2NmdGxiVnnhZoltcXS7IFHzd4F6 MknmNE4yNTFyMECgcm0> MnnGO|IhcA>? MkTTbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M1HQUVI2PTlyOEC1
MKN-28 M2fYN2NmdGxiVnnhZoltcXS7IFHzd4F6 MY[wMlEuOTByMDDuUS=> NFnuc2o4OiCq MYHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NEHRcm8zPTV7MEiwOS=>
MGC-803 MkDjSpVv[3Srb36gRZN{[Xl? M2rwbVAvOS1zMECwJI5O NUTzOHBCOjRiaB?= M1zO[4lv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? M4PaclI2PTlyOEC1
HCT-116 MnL3SpVv[3Srb36gRZN{[Xl? MnzCOVBvVQ>? M1fEblI1KGh? NHXKeoFFVVOR NVzBUYk4cW6mdXPl[EBIOC:JMTDhdpJme3R? NYj6flA2OjV{MUC3PVQ>
HT-29 NXrHfINqTnWwY4Tpc44hSXO|YYm= NH6yfpA2OG6P MWGyOEBp NEjoNmxFVVOR MojjbY5lfWOnZDDHNE9IOSCjcoLld5Q> MUWyOVIyODd7NB?=
SCC25 MV7DfZRwgGmlaYT5JGF{e2G7 M2rvR|ExNzVyIH7N M3PtTlI1KGh? NYC5e2p6\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NFPERoYzPTJyNUSzNC=>
FUDA NX;uOVBuS3m2b4jpZ4l1gSCDc4PhfS=> NHzY[lcyOC93MDDuUS=> NYPlOlMxOjRiaB?= NIrDdohl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M2nsTlI2OjB3NEOw
Detroit562 NIH6d3hEgXSxeHnjbZR6KEG|c3H5 MYqxNE82OCCwTR?= MVOyOEBp NF61O4Vl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MVWyOVIxPTR|MB?=
CAL27 NUHPO2ZCS3m2b4jpZ4l1gSCDc4PhfS=> MX2xNE82OCCwTR?= MYWyOEBp NWDS[2pJ\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MXSyOVIxPTR|MB?=
DSH1 M1;VWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPsTWM2OD14IH7N MnnONlQ4QDR6M{m=
SW-1710 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTZibl2= M4rTNVI1Pzh2OEO5
T24 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTdibl2= NV\PboF5OjR5OES4N|k>
RT112 NFTaRZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TXUWlEPTB;OTDuUS=> NEfiUJgzPDd6NEizPS=>
639-V M{H6PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFyIH7N NIPSfVczPDd6NEizPS=>
SCaBER MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLpTWM2OD1zMDDuUS=> NUnQeWsyOjR5OES4N|k>
BFTC M{DqT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjybJpKSzVyPUG3JI5O MoPRNlQ4QDR6M{m=
J82 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPkTHZ{UUN3ME2xPEBvVQ>? Mo\5NlQ4QDR6M{m=
HT-1376 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\ZOYo{UUN3ME2yNUBvVQ>? MkjXNlQ4QDR6M{m=
647-V NEPTZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjPfG1uUUN3ME2yO{BvVQ>? NY\DZ4NFOjR5OES4N|k>
UM-UC3 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXJW5dKSzVyPUOzJI5O M2rDNVI1Pzh2OEO5
LB831-BLC MmjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;KVVdQUUN3ME2zOEBvVQ>? M{j2VlI1Pzh2OEO5
KU-19-19 NFP0RVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTN4IH7N MUGyOFc5PDh|OR?=
35612 M4joOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3XXGJKSzVyPUO4JI5O MVeyOFc5PDh|OR?=
5637 M3vuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnRUZp3UUN3ME20OEBvVQ>? MYCyOFc5PDh|OR?=
HT-1197 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXS[nlrUUN3ME21N{BvVQ>? M3jxW|I1Pzh2OEO5
MGH-U3 MkOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzZeZlKSzVyPUWzJI5O M1rzflI1Pzh2OEO5
TCCSUP M2DFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF2MjDuUS=> Ml3xNlQ4QDR6M{m=
RT4 M1XkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LQc2lEPTB;MUezN{BvVQ>? NXe1Tok2OjR5OES4N|k>
SW780 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTN2NUGgcm0> MnuwNlQ4QDR6M{m=
RKO M3fNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNT2lEPTB;NDDuUS=> MVeyOFY5Ojd2Nx?=
LS-411 N MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTTendGUUN3ME21JI5O MV2yOFY5Ojd2Nx?=
SW620 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrzTWM2OD16IH7N MlvHNlQ3QDJ5NEe=
HCT-15 M1nBPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfYbZNWUUN3ME24JI5O NX22XZdZOjR4OEK3OFc>
HuTu-80 NYW5e5VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHr[5BPUUN3ME2xN{BvVQ>? NEPNV5EzPDZ6Mke0Oy=>
HCT 116 M4PH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r4WWlEPTB;MUSgcm0> MXuyOFY5Ojd2Nx?=
COLO-205 Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF2IH7N NV:2VnhnOjR4OEK3OFc>
NCI-H747 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF5IH7N Mnf6NlQ3QDJ5NEe=
COLO-678 NYTXT2FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTFZppKUUN3ME2yNUBvVQ>? NUHNdVJzOjR4OEK3OFc>
LoVo MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2eyXGlEPTB;MkKgcm0> NYLkOlR[OjR4OEK3OFc>
LS-1034 NY\GfpRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTNzIH7N NUXxNYx3OjR4OEK3OFc>
SNU-C2B NUXmfWZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTR3IH7N NFL2TIszPDZ6Mke0Oy=>
LS-123 NEGzV3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfGTWM2OD15MzDuUS=> M1LUSFI1Pjh{N{S3
SK-CO-1 M4nrTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fhPGlEPTB;OEGgcm0> NFW2fYQzPDZ6Mke0Oy=>
HCC2998 MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TmVWlEPTB;MUK4JI5O M4rVOFI1Pjh{N{S3
MDA-MB-231 M4HDfGZ2dmO2aX;uJGF{e2G7 NHO1NnkyODBibl2= NGHYToQ{OCCvaX6= M1vobYlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NYDLSnpTOjR{NEiyOlU>
MDA-MB-435 NWP1WVJjTnWwY4Tpc44hSXO|YYm= NVrLXZkyOTByIH7N MVezNEBucW5? MV7pcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NUizWXpEOjR{NEiyOlU>
BT-20  MXfGeY5kfGmxbjDBd5NigQ>? MYixNFAwOjVyIH7N MWeyOEBp M2XpdJJme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? NFfmdngzPDF5M{W0NS=>
MDA-MB-231 NH3BV|hHfW6ldHnvckBCe3OjeR?= MVyxNFAhdk1? NWLUSHBPOjRiaB?= MU\pcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg MYWyOFE4OzV2MR?=
H82 MnnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml64TWM2OD1|MD6yO{BvVQ>? MXiyOFE3PjVyNR?=
GLC4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJyLkS3JI5O M2XLUFI1OTZ4NUC1
H69 NHzEXHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LkbmlEPTB;OEOuN|Yhdk1? Mn;3NlQyPjZ3MEW=
H128 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHUTWM2OD14OT61OUBvVQ>? MYeyOFE3PjVyNR?=
H146 NHiwclFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\STWM2OD1{OD61NUBvVQ>? NIH4c3YzPDF4NkWwOS=>
H187 NIixPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDkbohbUUN3ME2yOE46QSCwTR?= MlHaNlQyPjZ3MEW=
H526 M1fXfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PPSmlEPTB;MkGuOlQhdk1? NYPMT3RrOjRzNk[1NFU>
N592 Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXBc|ZKSzVyPUG0MlEzKG6P MoTwNlQyPjZ3MEW=
H620 M1zkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S1U2lEPTB;M{KuOlchdk1? NYWyOWx{OjRzNk[1NFU>
H792 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR3LkC3JI5O MXGyOFE3PjVyNR?=
H1173 M4XSeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDNcItLUUN3ME2xNk43OiCwTR?= NIKyRpYzPDF4NkWwOS=>
AC3 Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJ3Lkmgcm0> NF\vfYkzPDF4NkWwOS=>
H82 M2HTR2Z2dmO2aX;uJGF{e2G7 NW\mN4RKOzBibl2= MUe3NkBp MWDpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= MV2yOFE3PjVyNR?=
GLC4 NFTaOopHfW6ldHnvckBCe3OjeR?= MkO5N|Ahdk1? NFvQZog4OiCq NGfFUVhqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MkLxNlQyPjZ3MEW=
H146  NV[5Z4E2TnWwY4Tpc44hSXO|YYm= NV;UVldNOzBibl2= MWe3NkBp MnLFbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NXGzfYZWOjRzNk[1NFU>
OVCAR-5 NYrSRYtbS2WubDDWbYFjcWyrdImgRZN{[Xl? NFn4fHgxNTFyMECgcm0> NW\Nb|QxPzJiaB?= NIL6e2hqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MWiyN|kxODF|Nh?=
OVCAR-8 Mm\nR4VtdCCYaXHibYxqfHliQYPzZZk> NHLHbo0xNTFyMECgcm0> M2jt[|czKGh? MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4[4RVI{QTByMUO2
A1847 NXrmfG92S2WubDDWbYFjcWyrdImgRZN{[Xl? NV7SZ5VkOC1zMECwJI5O MkXZO|IhcA>? NVuze2VjcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmnqNlM6ODBzM{[=
SKOV-3 NF3Vb2RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWSwMVExODBibl2= NG\RN3g4OiCq MWHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3vVclI{QTByMUO2
OVCAR-5 MlfBRZBweHSxc3nzJGF{e2G7 NVTLPJJROTBvMUCwJI5O M1myclI1NzR6L{eyJIg> NUTVe5VjcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NHW0bZgzOzlyMEGzOi=>
OVCAR-8 MX7BdI9xfG:|aYOgRZN{[Xl? MWKxNE0yODBibl2= NHfyflQzPC92OD:3NkBp MUjpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MVKyN|kxODF|Nh?=
A1847 M2XNdGFxd3C2b4Ppd{BCe3OjeR?= MUixNE0yODBibl2= NEKwNWozPC92OD:3NkBp MWfpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MojlNlM6ODBzM{[=
H2228 NHzROWFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWnO[Xo4OC1zMECwJI5O M{nZeFczKGh? NHrWW4JKSzVyPUGzJI5O NXTSfXg2OjN3M{OyOlU>
H3122 NIriOVNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3TRR|AuOTByMDDuUS=> NIK5cJk4OiCq NUHuOWgzUUN3ME2xNEBvVQ>? NFLuPWczOzV|M{K2OS=>
K008 MnOxR4VtdCCYaXHibYxqfHliQYPzZZk> MXnJR|UxRTZyIH7N NGn5OWozOzRzOEWyNy=>
K028 M4DlR2NmdGxiVnnhZoltcXS7IFHzd4F6 MYnJR|UxRTh2IH7N NWGy[lk1OjN2MUi1NlM>
K029 MmjXR4VtdCCYaXHibYxqfHliQYPzZZk> NEHrS4pKSzVyPUS2JI5O NECw[oUzOzRzOEWyNy=>
M23 NXGyd4tkS2WubDDWbYFjcWyrdImgRZN{[Xl? NX23SnZwUUN3ME2zO{42KG6P Ml3ONlM1OTh3MkO=
K033 MnPyR4VtdCCYaXHibYxqfHliQYPzZZk> M3r0[2lEPTB;N{WuOUBvVQ>? NWLYRnE5OjN2MUi1NlM>
K008 NXO5XlNmTnWwY4Tpc44hSXO|YYm= NX;4UWo4OjVyIH7N MkPKNlQhcA>? MWTpcoR2[2W|IFeyJIFzemW|dB?= MUOyN|QyQDV{Mx?=
K028 NF35N2RHfW6ldHnvckBCe3OjeR?= MVqyOVAhdk1? M2HteFI1KGh? NWPWbIFncW6mdXPld{BIOiCjcoLld5Q> NGLQXFEzOzRzOEWyNy=>
K029 NF73OItHfW6ldHnvckBCe3OjeR?= NXvvVldROjVyIH7N NYP3N3Y4OjRiaB?= NIn2doJqdmS3Y3XzJGcyKGG{cnXzeC=> NVTScI1UOjN2MUi1NlM>
M23 MnPpSpVv[3Srb36gRZN{[Xl? MYOyOVAhdk1? MVWyOEBp NHXZeW9qdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> NH:yW5IzOzRzOEWyNy=>
K033 NFjwSGVHfW6ldHnvckBCe3OjeR?= NVPxVnVQOjVyIH7N M2npZVI1KGh? Mn;hbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w MWOyN|QyQDV{Mx?=
K008 NWr5U21OSXCxcITvd4l{KEG|c3H5 MV[xNFAhdk1? NEXGN5E4OiCq NGrvO|l{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MkDlNlM1OTh3MkO=
K028 NGrJZm9CeG:ydH;zbZMhSXO|YYm= MVuxNFAhdk1? NXvYXVJKPzJiaB?= NYHr[5Z3e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MmPHNlM1OTh3MkO=
K029 M373[WFxd3C2b4Ppd{BCe3OjeR?= NWjGeHdlOTByIH7N MX63NkBp NUm4SWpQe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NVzmdlZFOjN2MUi1NlM>
M23 M2OxOWFxd3C2b4Ppd{BCe3OjeR?= MYGxNFAhdk1? MWC3NkBp NIPCNWR{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NHjwSJYzOzRzOEWyNy=>
K033 MoLCRZBweHSxc3nzJGF{e2G7 NUPUc3JuOTByIH7N MkHBO|IhcA>? MYnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MWCyN|QyQDV{Mx?=
RD MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7KTWM2OD16IH7N MX2yN|MxOzd2MR?=
Rh41 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjrc41KSzVyPUGwMlQhdk1? NF33bZUzOzNyM{e0NS=>
Rh18 MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyzTWM2OD14LkKgcm0> MXyyN|MxOzd2MR?=
Rh30 M3HEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTOTWM2OD13Lk[gcm0> M3;XT|I{OzB|N{Sx
BT-12 M37EW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTF2LkOgcm0> NVnpV3hYOjN|MEO3OFE>
CHLA-266 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TRe2lEPTB;MkeuNUBvVQ>? MViyN|MxOzd2MR?=
TC-71 NFLzcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTySJhKSzVyPUSuOUBvVQ>? MXWyN|MxOzd2MR?=
CHLA-9 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nJPGlEPTB;ND62JI5O MXOyN|MxOzd2MR?=
CHLA-10 Ml\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2zbm1KSzVyPUWuO{BvVQ>? NW[xXYxFOjN|MEO3OFE>
CHLA-258 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[4NHJjUUN3ME22MlQhdk1? NUfyNGU{OjN|MEO3OFE>
SJ-GBM2 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknCTWM2OD1zMj65JI5O MnXnNlM{ODN5NEG=
NB-1643 MnjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPuTWM2OD15LkSgcm0> M3HZ[lI{OzB|N{Sx
NB-EBc1 NFPSeIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILDeZlKSzVyPUG2Mlghdk1? NELhZnYzOzNyM{e0NS=>
CHLA-90 M4XCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEizRldKSzVyPUKyMlMhdk1? NVO1S5R3OjN|MEO3OFE>
CHLA-136 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7veZJKSzVyPUKzMlIhdk1? MUWyN|MxOzd2MR?=
NALM-6 NVX4NWdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXkUI1OUUN3ME2xNU44KG6P NHPsXYQzOzNyM{e0NS=>
COG-LL-317 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTRwNDDuUS=> NIf2VIIzOzNyM{e0NS=>
RS4;11 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrqTWM2OD1zMz61JI5O MVGyN|MxOzd2MR?=
MOLT-4 NUHDPFdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFyLk[gcm0> MXSyN|MxOzd2MR?=
CCRF-CEM (1) NX;PSpFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYThPWs5UUN3ME2xNk42KG6P NV;YZmlHOjN|MEO3OFE>
CCRF-CEM (2) MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljlTWM2OD15LkKgcm0> M2TObVI{OzB|N{Sx
Kasumi-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LsPGlEPTB;NT64JI5O MoKyNlM{ODN5NEG=
Karpas-299 M2f5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkCxTWM2OD17Lk[gcm0> NFfWcVYzOzNyM{e0NS=>
Ramos-RA1 MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PHTGlEPTB;Nz60JI5O MWSyN|MxOzd2MR?=
LNCaP NIPkXW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z6cGlEPTB;ODDuUS=> M3\aWlI{OTV{MEC0
VCaP M3[3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{i0WGlEPTB;NzDuUS=> M{nad|I{OTV{MEC0
H1355 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ywemlEPTB;NTDuUS=> MWWyN|AyOjJ2OB?=
H157 NHnuUphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7qelBKSzVyPUegcm0> NEPGO|czOzBzMkK0PC=>
H460 MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjSS4prUUN3ME24JI5O MkXrNlMxOTJ{NEi=
IA-LM Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\vfWlEPTB;MUCgcm0> M3vNU|I{ODF{MkS4
HOP-62 NH;IeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTtbnBTUUN3ME2xNUBvVQ>? NF\CW3UzOzBzMkK0PC=>
H23 MmLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXhV2hKSzVyPUGxJI5O NGr0N|YzOzBzMkK0PC=>
H2030 NH3uZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3JS21RUUN3ME2xNkBvVQ>? MmXJNlMxOTJ{NEi=
H441 NUHvT45qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHB[YZKSzVyPUG0JI5O NUPMNGRtOjNyMUKyOFg>
H2212 NIrmWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fM[WlEPTB;MUegcm0> NET3Z40zOzBzMkK0PC=>
SK-LU-1 MkK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrrN4Q5UUN3ME2xPEBvVQ>? M1\oflI{ODF{MkS4
H2009 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInLfnVKSzVyPUG5JI5O MW[yN|AyOjJ2OB?=
H1792 NY\kR3NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7iS5h5UUN3ME2yNEBvVQ>? NUXFNIR[OjNyMUKyOFg>
COR-L23 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHZc2xKSzVyPUKyJI5O NUTzU45[OjNyMUKyOFg>
H727 M3Kz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjGcHVmUUN3ME2yPEBvVQ>? NGLJOIMzOzBzMkK0PC=>
H1734 NVvtNFBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPJXmJKSzVyPUK4JI5O NWezb|RFOjNyMUKyOFg>
H358 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDP[Gd2UUN3ME2yPUBvVQ>? M{PDOVI{ODF{MkS4
A549 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ezU2lEPTB;NEOgcm0> NFXzUpgzOzBzMkK0PC=>
H2122 NXzydJBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPHXYsyUUN3ME21N{BvVQ>? MXqyN|AyOjJ2OB?=
Calu-1 M2XYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\SVWlEPTB;NUigcm0> M2XP[FI{ODF{MkS4
Calu-6 MoDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fjNWlEPTB;NkSgcm0> NX7UOVRGOjNyMUKyOFg>
NCI-H1975 M3XwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXaOFghcA>? NIHMN2RKSzVyPUG2JI5O MXOyNlE1PDZ4NR?=
NCI-H1975 NX;XdWlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TUPFczKGh? M1Lv[2lEPTB;ODDuUS=> MX6yNlE1PDZ4NR?=

... 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 (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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* 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

    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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