Ganetespib (STA-9090)

For research use only.

Catalog No.S1159

31 publications

Ganetespib (STA-9090) Chemical Structure

Molecular Weight(MW): 364.4

Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.

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Selleck's Ganetespib (STA-9090) has been cited by 31 publications

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Description Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Targets
HSP90 [1]
(OSA 8 cells)
4 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 MXLBdI9xfG:|aYOgRZN{[Xl? MYGzNE85OC9zNUCvNlUxKG6P NVXXOJloOjRxNEivO|IhcA>? NVX3ZYgxcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MXuyOVg5OjV3MB?=
MV411 NWrIcGY4SXCxcITvd4l{KEG|c3H5 Mn3nN|AwQDBxMUWwM|I2OCCwTR?= NUftXYpQOjRxNEivO|IhcA>? M4TldIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> M2C5WVI2QDh{NUWw
MGC-803 NXrQe2VwS2WubDDWbYFjcWyrdImgRZN{[Xl? M1jnd|AvOS1zMECwJI5O MUO3NkBp MWrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFrKflczPTV7MEiwOS=>
SGC-7901 Mlr3R4VtdCCYaXHibYxqfHliQYPzZZk> M1XWclAvOS1zMECwJI5O NYXXNIV{PzJiaB?= Mk[zbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M2jZdlI2PTlyOEC1
MKN-28 Ml23R4VtdCCYaXHibYxqfHliQYPzZZk> NVPpcZF[OC5zLUGwNFAhdk1? NVjxVWY5PzJiaB?= NXe5RYNJcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXLmZ4prOjV3OUC4NFU>
MGC-803 MULGeY5kfGmxbjDBd5NigQ>? NV62Z3VsOC5zLUGwNFAhdk1? MUGyOEBp NHrOTVdqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? MUCyOVU6ODhyNR?=
HCT-116 MYrGeY5kfGmxbjDBd5NigQ>? MlzrOVBvVQ>? NInOO5EzPCCq M{\mVmROW09? NELYfopqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NFnXc3gzPTJzMEe5OC=>
HT-29 NVO2XGp5TnWwY4Tpc44hSXO|YYm= NE\DXYU2OG6P Ml;SNlQhcA>? NG\pXZVFVVOR NHjDW|RqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MYKyOVIyODd7NB?=
SCC25 Mny5R5l1d3irY3n0fUBCe3OjeR?= NHfCTHgyOC93MDDuUS=> M2OxTVI1KGh? Ml3k[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NV;N[nFTOjV{MEW0N|A>
FUDA NHfhOGtEgXSxeHnjbZR6KEG|c3H5 NHvjfG0yOC93MDDuUS=> NEK0dZMzPCCq NIfWdFVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MXuyOVIxPTR|MB?=
Detroit562 M321fGN6fG:6aXPpeJkhSXO|YYm= MVOxNE82OCCwTR?= MoXmNlQhcA>? M1nvPYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MlzRNlUzODV2M{C=
CAL27 NELS[YhEgXSxeHnjbZR6KEG|c3H5 NEL6WYgyOC93MDDuUS=> Mm[xNlQhcA>? NYm1OlZQ\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M1;iXlI2OjB3NEOw
DSH1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3ibHNWUUN3ME22JI5O M1;NUFI1Pzh2OEO5
SW-1710 NXTDfXZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\hS2VrUUN3ME22JI5O NHK1SZgzPDd6NEizPS=>
T24 M{XPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTdibl2= MYOyOFc5PDh|OR?=
RT112 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTlibl2= NIC4W4wzPDd6NEizPS=>
639-V NX\aTI9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33nZ2lEPTB;MUCgcm0> NYDiOpA1OjR5OES4N|k>
SCaBER NXjwZVhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3Fd5ZUUUN3ME2xNEBvVQ>? M3n5RlI1Pzh2OEO5
BFTC NXXjfZZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXHV2NGUUN3ME2xO{BvVQ>? NFy0W3kzPDd6NEizPS=>
J82 MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlOyTWM2OD1zODDuUS=> MV[yOFc5PDh|OR?=
HT-1376 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXVTWM2OD1{MTDuUS=> NYPSdXY2OjR5OES4N|k>
647-V NWHDUHlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzDTWM2OD1{NzDuUS=> NFjpNIEzPDd6NEizPS=>
UM-UC3 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\STWM2OD1|MzDuUS=> NGnuNWkzPDd6NEizPS=>
LB831-BLC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTN2IH7N MXeyOFc5PDh|OR?=
KU-19-19 M4rVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHTTWM2OD1|NjDuUS=> M2LhcVI1Pzh2OEO5
35612 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTN6IH7N NHrXb4IzPDd6NEizPS=>
5637 Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\ZTWM2OD12NDDuUS=> M4K2cVI1Pzh2OEO5
HT-1197 M3;0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorqTWM2OD13MzDuUS=> M371UVI1Pzh2OEO5
MGH-U3 NITwXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTWRnlPUUN3ME21N{BvVQ>? MVyyOFc5PDh|OR?=
TCCSUP M1PJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rFUGlEPTB;MUSyJI5O NHvFcWozPDd6NEizPS=>
RT4 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHZTWM2OD1zN{OzJI5O NFjaUlczPDd6NEizPS=>
SW780 M{LRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnniTWM2OD1|NEWxJI5O MV[yOFc5PDh|OR?=
RKO M1u1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXK2ZW14UUN3ME20JI5O NWPYcFlSOjR4OEK3OFc>
LS-411 N MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2CzN2lEPTB;NTDuUS=> NYflZmh2OjR4OEK3OFc>
SW620 NVPyZoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRThibl2= NHzxNHEzPDZ6Mke0Oy=>
HCT-15 NHHBbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17LbGlEPTB;ODDuUS=> MlLYNlQ3QDJ5NEe=
HuTu-80 NHXpdZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P0UmlEPTB;MUOgcm0> NWS0eodKOjR4OEK3OFc>
HCT 116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTF2IH7N NWLuZ2U6OjR4OEK3OFc>
COLO-205 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfvOplIUUN3ME2xOEBvVQ>? M{\4UFI1Pjh{N{S3
NCI-H747 NGH4TWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF5IH7N MlS5NlQ3QDJ5NEe=
COLO-678 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJzIH7N MViyOFY5Ojd2Nx?=
LoVo NEm2VGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XvUWlEPTB;MkKgcm0> M1\HblI1Pjh{N{S3
LS-1034 NVK1eIwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDmOmdKSzVyPUOxJI5O MVKyOFY5Ojd2Nx?=
SNU-C2B NYWzWoZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmntTWM2OD12NTDuUS=> NUDQNHk4OjR4OEK3OFc>
LS-123 NYLNUHpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTd|IH7N M{XXWlI1Pjh{N{S3
SK-CO-1 M2ewWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRThzIH7N NIO2OFkzPDZ6Mke0Oy=>
HCC2998 MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jHVGlEPTB;MUK4JI5O NWfGXVN[OjR4OEK3OFc>
MDA-MB-231 NUTzc3I6TnWwY4Tpc44hSXO|YYm= NEO4bXMyODBibl2= MWqzNEBucW5? M1;2R4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MoWwNlQzPDh{NkW=
MDA-MB-435 M3jRZ2Z2dmO2aX;uJGF{e2G7 NIrVUpQyODBibl2= NGjSb4c{OCCvaX6= NILZZolqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= MUSyOFI1QDJ4NR?=
BT-20  M3nGTmZ2dmO2aX;uJGF{e2G7 NXi1VIY{OTByL{K1NEBvVQ>? M3LEVVI1KGh? NFr3Xm9z\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? MUSyOFE4OzV2MR?=
MDA-MB-231 NWTOdIo5TnWwY4Tpc44hSXO|YYm= M2DUXVExOCCwTR?= NXX6c4p5OjRiaB?= MnjDbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> M3fTd|I1OTd|NUSx
H82 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrtNlZKSzVyPUOwMlI4KG6P MnPRNlQyPjZ3MEW=
GLC4 M4fuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJyLkS3JI5O MnPMNlQyPjZ3MEW=
H69 NEfF[YJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmxR5hPUUN3ME24N{4{PiCwTR?= NGLs[GozPDF4NkWwOS=>
H128 M3OzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrneHl[UUN3ME22PU42PSCwTR?= M1:wVFI1OTZ4NUC1
H146 M{GzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3nZZZPUUN3ME2yPE42OSCwTR?= M{\xe|I1OTZ4NUC1
H187 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlywTWM2OD1{ND65PUBvVQ>? NXG4N5RJOjRzNk[1NFU>
H526 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTJzLk[0JI5O MXmyOFE3PjVyNR?=
N592 Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknkTWM2OD1zND6xNkBvVQ>? M4XsTlI1OTZ4NUC1
H620 NIHmVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofKTWM2OD1|Mj62O{BvVQ>? NUDR[YZiOjRzNk[1NFU>
H792 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPJd4RKSzVyPUS1MlA4KG6P MUCyOFE3PjVyNR?=
H1173 NYn2VZhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:zfWFKSzVyPUGyMlYzKG6P NXraPXg1OjRzNk[1NFU>
AC3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuwVJRKSzVyPUK1Mlkhdk1? MXeyOFE3PjVyNR?=
H82 MWXGeY5kfGmxbjDBd5NigQ>? M3LTdFMxKG6P NYLDSm1bPzJiaB?= NWPMOXFTcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M1\UeFI1OTZ4NUC1
GLC4 MonGSpVv[3Srb36gRZN{[Xl? NFGzS2o{OCCwTR?= M3z0[lczKGh? MlvjbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MnrTNlQyPjZ3MEW=
H146  M2DG[GZ2dmO2aX;uJGF{e2G7 NH\FflA{OCCwTR?= NXLINlhRPzJiaB?= NUXN[YNzcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NHrw[|kzPDF4NkWwOS=>
OVCAR-5 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUnjXo0yOC1zMECwJI5O NHr6bpc4OiCq NI\0XGtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYDLOlRYOjN7MECxN|Y>
OVCAR-8 NXPrdGNTS2WubDDWbYFjcWyrdImgRZN{[Xl? Ml[yNE0yODByIH7N Ml3vO|IhcA>? NX[1VHl{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmOwNlM6ODBzM{[=
A1847 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUTBZ2QzOC1zMECwJI5O NHzoNnM4OiCq MWnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mn7wNlM6ODBzM{[=
SKOV-3 NV\PRZZqS2WubDDWbYFjcWyrdImgRZN{[Xl? MXSwMVExODBibl2= MnPqO|IhcA>? MX3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MnPBNlM6ODBzM{[=
OVCAR-5 NXe4WHhKSXCxcITvd4l{KEG|c3H5 M4q1c|ExNTFyMDDuUS=> MlvENlQwPDhxN{KgbC=> MWnpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MlzLNlM6ODBzM{[=
OVCAR-8 NX3IW|lKSXCxcITvd4l{KEG|c3H5 NWnzOZNPOTBvMUCwJI5O NEP4dGYzPC92OD:3NkBp NGfsdWNqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NWnBW2VkOjN7MECxN|Y>
A1847 Mne3RZBweHSxc3nzJGF{e2G7 M4DjRVExNTFyMDDuUS=> NW\veWFTOjRxNEivO|IhcA>? MXfpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 NWPrU21wOjN7MECxN|Y>
H2228 NFf5bm5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1q3TlAuOTByMDDuUS=> MXi3NkBp MlrkTWM2OD1zMzDuUS=> NYXhSZVFOjN3M{OyOlU>
H3122 M1XHS2NmdGxiVnnhZoltcXS7IFHzd4F6 MmTENE0yODByIH7N NHK1Uow4OiCq M3;rZmlEPTB;MUCgcm0> NVPPNZZPOjN3M{OyOlU>
K008 NUDGUIRSS2WubDDWbYFjcWyrdImgRZN{[Xl? M3Hyc2lEPTB;NkCgcm0> NGDqdW4zOzRzOEWyNy=>
K028 MlnPR4VtdCCYaXHibYxqfHliQYPzZZk> M3XQR2lEPTB;OESgcm0> M1fGWlI{PDF6NUKz
K029 NELlUmdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MorZTWM2OD12NjDuUS=> NUXnSFV6OjN2MUi1NlM>
M23 M{jGO2NmdGxiVnnhZoltcXS7IFHzd4F6 NWfZco1iUUN3ME2zO{42KG6P MVeyN|QyQDV{Mx?=
K033 MmPDR4VtdCCYaXHibYxqfHliQYPzZZk> M1;veGlEPTB;N{WuOUBvVQ>? NIS3bnYzOzRzOEWyNy=>
K008 MY\GeY5kfGmxbjDBd5NigQ>? MYeyOVAhdk1? MkLwNlQhcA>? MUnpcoR2[2W|IFeyJIFzemW|dB?= M2Dkc|I{PDF6NUKz
K028 MYjGeY5kfGmxbjDBd5NigQ>? M4fJTVI2OCCwTR?= M1PJ[FI1KGh? NU\XPWdscW6mdXPld{BIOiCjcoLld5Q> MWOyN|QyQDV{Mx?=
K029 Mle3SpVv[3Srb36gRZN{[Xl? MXyyOVAhdk1? M1joW|I1KGh? Ml:5bY5lfWOnczDHNUBienKnc4S= MVqyN|QyQDV{Mx?=
M23 NHTER3BHfW6ldHnvckBCe3OjeR?= NVvUNJhHOjVyIH7N NWLuNmN4OjRiaB?= MVnpcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= MYqyN|QyQDV{Mx?=
K033 MonHSpVv[3Srb36gRZN{[Xl? MYiyOVAhdk1? MVuyOEBp NWiybIRYcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u NEfQNJEzOzRzOEWyNy=>
K008 MWPBdI9xfG:|aYOgRZN{[Xl? NEHp[ngyODBibl2= MWS3NkBp MWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NWnXZ|BkOjN2MUi1NlM>
K028 NYK1SGJSSXCxcITvd4l{KEG|c3H5 Mo\MNVAxKG6P M4\FWVczKGh? MoTod4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M3PkWVI{PDF6NUKz
K029 MYrBdI9xfG:|aYOgRZN{[Xl? M1nqR|ExOCCwTR?= NEXLOFE4OiCq Ml;Zd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MX6yN|QyQDV{Mx?=
M23 MVnBdI9xfG:|aYOgRZN{[Xl? M1\GbVExOCCwTR?= NVjP[WhPPzJiaB?= M{i4PZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M1eyTVI{PDF6NUKz
K033 NUn1[3d7SXCxcITvd4l{KEG|c3H5 M1fzeFExOCCwTR?= MYW3NkBp MmTod4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MUSyN|QyQDV{Mx?=
RD M3voT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjwSXZKSzVyPUigcm0> NIX6NHAzOzNyM{e0NS=>
Rh41 NY\BfXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjsb5VGUUN3ME2xNE41KG6P M3vIb|I{OzB|N{Sx
Rh18 NVnDSpRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PEemlEPTB;Nj6yJI5O NUL1fpBWOjN|MEO3OFE>
Rh30 M{OyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPYcYdKSzVyPUWuOkBvVQ>? MkHINlM{ODN5NEG=
BT-12 NVnCcpgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnLPJdKSzVyPUG0MlMhdk1? M1\vPFI{OzB|N{Sx
CHLA-266 NEPQ[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHBSGJqUUN3ME2yO{4yKG6P NIHKbnkzOzNyM{e0NS=>
TC-71 MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTRwNTDuUS=> NIPPN5QzOzNyM{e0NS=>
CHLA-9 NYXxfVVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfIR21JUUN3ME20MlYhdk1? MWKyN|MxOzd2MR?=
CHLA-10 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1KxeWlEPTB;NT63JI5O NG\nboczOzNyM{e0NS=>
CHLA-258 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTZwNDDuUS=> MX[yN|MxOzd2MR?=
SJ-GBM2 M3Tyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF{Lkmgcm0> M3:3VlI{OzB|N{Sx
NB-1643 M1u4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETxcYpKSzVyPUeuOEBvVQ>? NIDSe4wzOzNyM{e0NS=>
NB-EBc1 NVnrSYFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF4Lkigcm0> NH3HdogzOzNyM{e0NS=>
CHLA-90 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTJ{LkOgcm0> M{GyfVI{OzB|N{Sx
CHLA-136 NUDEc3Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXRTWM2OD1{Mz6yJI5O NFK0dZUzOzNyM{e0NS=>
NALM-6 NGrwdYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFewdnJKSzVyPUGxMlchdk1? NY\0Nmc{OjN|MEO3OFE>
COG-LL-317 NEX5OIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX61OHA6UUN3ME20MlQhdk1? M3Tjb|I{OzB|N{Sx
RS4;11 NYT2XppzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTZdXlKSzVyPUGzMlUhdk1? MnjRNlM{ODN5NEG=
MOLT-4 NUT3dlg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPQTWM2OD1zMD62JI5O NYLuXnl5OjN|MEO3OFE>
CCRF-CEM (1) NULq[2pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF{LkWgcm0> NX3neHlkOjN|MEO3OFE>
CCRF-CEM (2) M{\DXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K4ZmlEPTB;Nz6yJI5O NX3OZVF3OjN|MEO3OFE>
Kasumi-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjTNGtKSzVyPUWuPEBvVQ>? NVnSRYVTOjN|MEO3OFE>
Karpas-299 NXv3PWo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\ZZVhKSzVyPUmuOkBvVQ>? NHX0XYkzOzNyM{e0NS=>
Ramos-RA1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3tcnZFUUN3ME23MlQhdk1? M2\zXVI{OzB|N{Sx
LNCaP M3K4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXYbHNKSzVyPUigcm0> Moe0NlMyPTJyMES=
VCaP NFjwbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4C0bGlEPTB;NzDuUS=> NFHzTHMzOzF3MkCwOC=>
H1355 NI\MbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmySYZKSzVyPUWgcm0> M1vPXlI{ODF{MkS4
H157 M1f3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTdibl2= MXKyN|AyOjJ2OB?=
H460 MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfodmp4UUN3ME24JI5O NULPdFlEOjNyMUKyOFg>
IA-LM NFjDNZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13Ob2lEPTB;MUCgcm0> NXLIflVvOjNyMUKyOFg>
HOP-62 NGH3WmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXHTFNjUUN3ME2xNUBvVQ>? MmHJNlMxOTJ{NEi=
H23 NInKZ|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLzTWM2OD1zMTDuUS=> NV3VNpdWOjNyMUKyOFg>
H2030 M1W0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTF{IH7N NX3sPVJGOjNyMUKyOFg>
H441 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT6WY1oUUN3ME2xOEBvVQ>? NX\OUYdJOjNyMUKyOFg>
H2212 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH3TWM2OD1zNzDuUS=> NFfX[oYzOzBzMkK0PC=>
SK-LU-1 NVvGZZN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDhTlI1UUN3ME2xPEBvVQ>? NVPqWIkyOjNyMUKyOFg>
H2009 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPRN29ZUUN3ME2xPUBvVQ>? NHHOPGMzOzBzMkK0PC=>
H1792 Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTsTWM2OD1{MDDuUS=> Mn32NlMxOTJ{NEi=
COR-L23 NXfRV4FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPvXlc3UUN3ME2yNkBvVQ>? MXuyN|AyOjJ2OB?=
H727 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ6IH7N Mn\rNlMxOTJ{NEi=
H1734 M3HVXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETCOZNKSzVyPUK4JI5O MXmyN|AyOjJ2OB?=
H358 NECx[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXG0b3ZVUUN3ME2yPUBvVQ>? MojmNlMxOTJ{NEi=
A549 M3\EVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rIOWlEPTB;NEOgcm0> MkLvNlMxOTJ{NEi=
H2122 M3TrU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTnTWM2OD13MzDuUS=> MkXUNlMxOTJ{NEi=
Calu-1 M2\BWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrTVmdKSzVyPUW4JI5O MVeyN|AyOjJ2OB?=
Calu-6 M1vt[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHoXHJKSzVyPU[0JI5O M2PRXFI{ODF{MkS4
NCI-H1975 M3SzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLLSJh1PDhiaB?= M1:1cmlEPTB;MU[gcm0> M2O5[VIzOTR2Nk[1
NCI-H1975 M2DDN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjD[XVFPzJiaB?= Mn3OTWM2OD16IH7N M3\6e|IzOTR2Nk[1

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK; 

PubMed: 23418523     


Downregulation of multiple signaling pathways by ganetespib in melanoma cells.A. Cells were treated with indicated amounts of ganetespib for 24 h. B-RAF and N-RAS mutational status of each cell line is indicated.

p27(Kip1) / p21 (Cip1) / Cyclin D1 / Cyclin E / Cyclin B1 / CDK1 / CDK2 / CDK4; 

PubMed: 23418523     


Alterations in expression of multiple cell cycle regulating proteins induced by ganetespib. Cells were treated with indicated amounts of ganetespib for 48 h and analyzed by Western blot analysis. Relative expression levels of proteins (treated vs. control䲧疝Ỵ疞㧀疜膉痘 

Survivin / Bcl-2 / Bcl-xl / Mcl-1; 

PubMed: 23418523     


Effect of ganetespib on the expression of antiapoptotic proteins. Cells were treated with ganetespib for 48 h and analyzed using Western blot analysis. Relative expression levels of proteins are indicated.

B-RAF / C-RAF / N-RAS ; 

PubMed: 23418523     


Effect of ganetespib on B-RAF, C-RAF and N-RAS expression in melanoma cells.Cells were treated with indicated amounts of ganetespib for 48 h and subjected to Western blot analysis.

HER2 / p-STAT3 / BIM ; 

PubMed: 25077897     


NCI-H1975 cells were incubated with the indicated concentrations of ganetespib for 24 h. Cell lysates were analyzed by Western blotting.

CDK1 / Cyclin D1 / Cyclin B1 / p27; 

PubMed: 29717218     


Cropped Western blot images of the indicated cell cycle regulators are shown in ganetespib-treated (0–300 nM for 16 hours) BT474 and SKBR3 cells. 

c-PARP / c-caspase 3 / caspase 8 / c-caspase 8 / caspase 9 / c-caspase 9; 

PubMed: 29717218     


Cropped images of Western blots at the target molecular weights for the indicated apoptotic markers are shown in ganetespib-treated (0, 10, 30, 100, 300 nM for 16 hours) BT474 and SKBR3 cells. 

ErbB2 / pErbB2 / Src / pSrc / mTOR / pmTOR / Bad / pBad / GSK3 / pGSK3; 

PubMed: 29717218     


Ganetespib inhibits RTK signaling in ErbB2+ breast cancer cells. BT474 and SKBR3 cells were treated with ganetespib (0, 10, 30, 100, or 300 nM) for 16 hours, followed by Western blot analysis (cropped images) of the expression and activation/phosphorylati䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖

Wee1 / p-Wee1 / Chk1 / p-Chk1; 

PubMed: 27834954     


Hsp90 inhibition degrades the G2/M checkpoint kinases Wee1 and Chk1. The cells were treated with 200 nM ganetespib and 75 μM carboplatin for 24 h followed by immunoblot analysis. Carboplatin treatment leads to the activation of Chk1, indicated by phospho—䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ

23418523 25077897 29717218 27834954
Growth inhibition assay
Cell viability ; 

PubMed: 23418523     


A. Ganetespib reduced viability. Cells were treated with varying amounts of ganetespib for 72 h and subjected to MTS assay. Data are expressed as mean±SD of three independent experiments. B. Mutational status and ganetespib IC50 of cell lines.

23418523
In vivo 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]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: OSA cells
  • Concentrations: 0.001-1μM
  • Incubation Time: 5 days
  • Method: 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.
    (Only for Reference)
Animal Research:[4]
- Collapse
  • Animal Models: Female severe combined immune-deficient (SCID) mice
  • Dosages: 25 mg/kg/day for 3 days
  • Administration: Tail vein injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (109.76 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.
11mg/mL

* 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.

Chemical Information

Molecular Weight 364.4
Formula

C20H20N4O3

CAS No. 888216-25-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)C1=C(O)C=C(O)C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)[N](C)C=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Terminated Drug: Ziv-Aflibercept|Drug: Ganetespib Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 2 2014 Phase 1
NCT02008877 Completed Drug: ganetespib|Drug: Sirolimus Malignant Peripheral Nerve Sheath Tumors (MPNST)|Sarcoma Sarcoma Alliance for Research through Collaboration|Synta Pharmaceuticals Corp.|United States Department of Defense December 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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/

HSP (e.g. HSP90) Signaling Pathway Map

HSP (e.g. HSP90) Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID