Ganetespib (STA-9090)

Catalog No.S1159

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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Cited by 23 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 M1HEPWFxd3C2b4Ppd{BCe3OjeR?= MX[zNE85OC9zNUCvNlUxKG6P MlvLNlQwPDhxN{KgbC=> MlHQbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz M3jSSVI2QDh{NUWw
MV411 NHTENWRCeG:ydH;zbZMhSXO|YYm= MYizNE85OC9zNUCvNlUxKG6P MknyNlQwPDhxN{KgbC=> M2\abIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NGPUU5ozPTh6MkW1NC=>
MGC-803 NIPIOnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXK0PFdQOC5zLUGwNFAhdk1? NXrlcGhEPzJiaB?= MYfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NVe1U2M{OjV3OUC4NFU>
SGC-7901 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn20NE4yNTFyMECgcm0> NWTmT29FPzJiaB?= MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkHKNlU2QTB6MEW=
MKN-28 MmjGR4VtdCCYaXHibYxqfHliQYPzZZk> M4POfFAvOS1zMECwJI5O MlfjO|IhcA>? MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NWPET5dGOjV3OUC4NFU>
MGC-803 MmXuSpVv[3Srb36gRZN{[Xl? M2G2NFAvOS1zMECwJI5O MX[yOEBp NEXXOY9qdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? MkjpNlU2QTB6MEW=
HCT-116 MXPGeY5kfGmxbjDBd5NigQ>? MYe1NI5O M4\HPVI1KGh? NXPLbWVtTE2VTx?= NHv6V|hqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NEP0T5czPTJzMEe5OC=>
HT-29 Ml2xSpVv[3Srb36gRZN{[Xl? NV21c|B{PTCwTR?= NHH0N20zPCCq MWTEUXNQ NHfaUY1qdmS3Y3XkJGcxN0dzIHHydoV{fA>? NF3HcoszPTJzMEe5OC=>
SCC25 NV3VfpoxS3m2b4jpZ4l1gSCDc4PhfS=> M3v3XlExNzVyIH7N NYLhcFBLOjRiaB?= NWD6VWpP\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M4Pz[lI2OjB3NEOw
FUDA Mm\oR5l1d3irY3n0fUBCe3OjeR?= MXWxNE82OCCwTR?= M4fMTlI1KGh? MXHk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MUmyOVIxPTR|MB?=
Detroit562 NYTJfnZyS3m2b4jpZ4l1gSCDc4PhfS=> MlS5NVAwPTBibl2= NYDpXpNHOjRiaB?= MUjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M3S0dFI2OjB3NEOw
CAL27 NX60RnNPS3m2b4jpZ4l1gSCDc4PhfS=> MUexNE82OCCwTR?= MUWyOEBp NEjrXnBl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NFzLd3czPTJyNUSzNC=>
DSH1 NFjIVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTZibl2= NVq0Vo1ZOjR5OES4N|k>
SW-1710 MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDadnNKSzVyPU[gcm0> NITHXZAzPDd6NEizPS=>
T24 NYLPVoVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPMVpNKSzVyPUegcm0> NVnPU4t6OjR5OES4N|k>
RT112 MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTlibl2= NWjYdYtrOjR5OES4N|k>
639-V Ml\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFyIH7N M4W3XlI1Pzh2OEO5
SCaBER NFrEelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTGfXRKSzVyPUGwJI5O MnS3NlQ4QDR6M{m=
BFTC NEe3fGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zvbGlEPTB;MUegcm0> NFjuZ2wzPDd6NEizPS=>
J82 MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL4XYlKSzVyPUG4JI5O NVnHell6OjR5OES4N|k>
HT-1376 NVXyeZZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS3TIhKSzVyPUKxJI5O NH\xNlMzPDd6NEizPS=>
647-V M3;BXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[xTWM2OD1{NzDuUS=> MlLjNlQ4QDR6M{m=
UM-UC3 NF7uZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7mOXJKSzVyPUOzJI5O NXy2fohCOjR5OES4N|k>
LB831-BLC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTN2IH7N M1XONVI1Pzh2OEO5
KU-19-19 M13PR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\PVnNKSzVyPUO2JI5O MVqyOFc5PDh|OR?=
35612 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L1[WlEPTB;M{igcm0> MXuyOFc5PDh|OR?=
5637 M1LjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTR2IH7N Mn30NlQ4QDR6M{m=
HT-1197 MkDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XaW2lEPTB;NUOgcm0> MlLiNlQ4QDR6M{m=
MGH-U3 NV\EZpVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTV|IH7N MoDxNlQ4QDR6M{m=
TCCSUP Mn;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojhTWM2OD1zNEKgcm0> MX6yOFc5PDh|OR?=
RT4 Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfGUpRXUUN3ME2xO|M{KG6P NX;i[3ZpOjR5OES4N|k>
SW780 NUfaXI9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV24SodtUUN3ME2zOFUyKG6P NYfVUXJDOjR5OES4N|k>
RKO NYDsU2huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXmWYlKSzVyPUSgcm0> Mo\CNlQ3QDJ5NEe=
LS-411 N M4DPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnDWZFKSzVyPUWgcm0> MYqyOFY5Ojd2Nx?=
SW620 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4fmlEPTB;ODDuUS=> M2\NW|I1Pjh{N{S3
HCT-15 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf1To9KSzVyPUigcm0> NUXPUHYyOjR4OEK3OFc>
HuTu-80 M2K5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF|IH7N M3;CWlI1Pjh{N{S3
HCT 116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjnPXhKSzVyPUG0JI5O M4Tnc|I1Pjh{N{S3
COLO-205 M3vlSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jtemlEPTB;MUSgcm0> NETkT40zPDZ6Mke0Oy=>
NCI-H747 NXzQSI51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILlZXVKSzVyPUG3JI5O MUeyOFY5Ojd2Nx?=
COLO-678 Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFKwdHdKSzVyPUKxJI5O MVuyOFY5Ojd2Nx?=
LoVo M2jSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LpWGlEPTB;MkKgcm0> MYeyOFY5Ojd2Nx?=
LS-1034 M2TRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP5TWM2OD1|MTDuUS=> MmnvNlQ3QDJ5NEe=
SNU-C2B MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTR3IH7N NEHCXpkzPDZ6Mke0Oy=>
LS-123 NGfIOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTd|IH7N NH\XR2MzPDZ6Mke0Oy=>
SK-CO-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnYcoJSUUN3ME24NUBvVQ>? NFXhb|MzPDZ6Mke0Oy=>
HCC2998 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF{ODDuUS=> MWqyOFY5Ojd2Nx?=
MDA-MB-231 NX3sTnIxTnWwY4Tpc44hSXO|YYm= NXO5RZhQOTByIH7N MUWzNEBucW5? M1HrSIlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NYjHfll4OjR{NEiyOlU>
MDA-MB-435 NHTjO4hHfW6ldHnvckBCe3OjeR?= MWWxNFAhdk1? NVfVdGxGOzBibXnu M2fqV4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NUHi[4Z6OjR{NEiyOlU>
BT-20  Mlr0SpVv[3Srb36gRZN{[Xl? M{TR[VExOC9{NUCgcm0> NYWwZlRyOjRiaB?= Ml7WdoV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH M1ThOFI1OTd|NUSx
MDA-MB-231 M4HobmZ2dmO2aX;uJGF{e2G7 NX7TdW9iOTByIH7N NH7KRVczPCCq M1LMXYlvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> MlfFNlQyPzN3NEG=
H82 M3fwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTNyLkK3JI5O NWH2WWNIOjRzNk[1NFU>
GLC4 NHnQbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3H5PGlEPTB;MkCuOFchdk1? NXvWeJA6OjRzNk[1NFU>
H69 M1PVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\kfoR7UUN3ME24N{4{PiCwTR?= MWSyOFE3PjVyNR?=
H128 M2DZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZ7LkW1JI5O NUXqe216OjRzNk[1NFU>
H146 M{LGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXzTWM2OD1{OD61NUBvVQ>? M2L1U|I1OTZ4NUC1
H187 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjCTopUUUN3ME2yOE46QSCwTR?= MYmyOFE3PjVyNR?=
H526 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfPRWZIUUN3ME2yNU43PCCwTR?= MofNNlQyPjZ3MEW=
N592 NUHmfYxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjTTWM2OD1zND6xNkBvVQ>? MlLrNlQyPjZ3MEW=
H620 M1LzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTN{Lk[3JI5O M3;Vc|I1OTZ4NUC1
H792 NYHP[VlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG4e5liUUN3ME20OU4xPyCwTR?= NF7O[5QzPDF4NkWwOS=>
H1173 Mn:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfDTWM2OD1zMj62NkBvVQ>? MkK3NlQyPjZ3MEW=
AC3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJ3Lkmgcm0> MmDlNlQyPjZ3MEW=
H82 M3\sOGZ2dmO2aX;uJGF{e2G7 NFLxXmc{OCCwTR?= NFnsOIY4OiCq NWXCenFYcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NH;RTngzPDF4NkWwOS=>
GLC4 NHHEZ3VHfW6ldHnvckBCe3OjeR?= NVrIfGJROzBibl2= NGG2Omo4OiCq MYPpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= MWqyOFE3PjVyNR?=
H146  NEHE[3lHfW6ldHnvckBCe3OjeR?= MVKzNEBvVQ>? MmDOO|IhcA>? NIrhU2tqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NYPXOJZyOjRzNk[1NFU>
OVCAR-5 MnfNR4VtdCCYaXHibYxqfHliQYPzZZk> MofSNE0yODByIH7N M2DpS|czKGh? M4TXNYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NEm5NlczOzlyMEGzOi=>
OVCAR-8 M4K3UmNmdGxiVnnhZoltcXS7IFHzd4F6 NEXCTmwxNTFyMECgcm0> MnzqO|IhcA>? M{jN[olvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{LRNlI{QTByMUO2
A1847 MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWmwMVExODBibl2= MVO3NkBp M2LzTIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M2PkZ|I{QTByMUO2
SKOV-3 MkjsR4VtdCCYaXHibYxqfHliQYPzZZk> M4flfFAuOTByMDDuUS=> NUnQ[3ZTPzJiaB?= MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NEDLPXEzOzlyMEGzOi=>
OVCAR-5 MX7BdI9xfG:|aYOgRZN{[Xl? NWnmPY5mOTBvMUCwJI5O MWOyOE81QC95MjDo NHu5fo5qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NHGxZXczOzlyMEGzOi=>
OVCAR-8 NHzZcWVCeG:ydH;zbZMhSXO|YYm= NHfDOGsyOC1zMECgcm0> NIXSRZUzPC92OD:3NkBp M4rSS4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MnzLNlM6ODBzM{[=
A1847 NGr5O2ZCeG:ydH;zbZMhSXO|YYm= NFP0bnkyOC1zMECgcm0> MnLRNlQwPDhxN{KgbC=> NWDaSIZucW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NIWwOoczOzlyMEGzOi=>
H2228 MnrnR4VtdCCYaXHibYxqfHliQYPzZZk> NGTqRmIxNTFyMECgcm0> MnuxO|IhcA>? M1XNVGlEPTB;MUOgcm0> NWO0V5NEOjN3M{OyOlU>
H3122 NYn3cmhnS2WubDDWbYFjcWyrdImgRZN{[Xl? NYX3UFVmOC1zMECwJI5O NXH4XJgzPzJiaB?= NG\penZKSzVyPUGwJI5O M3XlW|I{PTN|Mk[1
K008 MorPR4VtdCCYaXHibYxqfHliQYPzZZk> NX;OVG5wUUN3ME22NEBvVQ>? MYOyN|QyQDV{Mx?=
K028 NH;ITWxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEj0WmtKSzVyPUi0JI5O NV3KcotnOjN2MUi1NlM>
K029 NUHwVo1FS2WubDDWbYFjcWyrdImgRZN{[Xl? Mni0TWM2OD12NjDuUS=> MkD6NlM1OTh3MkO=
M23 Mnz5R4VtdCCYaXHibYxqfHliQYPzZZk> NXS1T4FmUUN3ME2zO{42KG6P M{KxclI{PDF6NUKz
K033 NVriUYZ3S2WubDDWbYFjcWyrdImgRZN{[Xl? NIXYfZlKSzVyPUe1MlUhdk1? MkDDNlM1OTh3MkO=
K008 MUnGeY5kfGmxbjDBd5NigQ>? NG\zfo4zPTBibl2= MXeyOEBp NVO3N4lKcW6mdXPld{BIOiCjcoLld5Q> MojQNlM1OTh3MkO=
K028 MXLGeY5kfGmxbjDBd5NigQ>? MonmNlUxKG6P NIDvb24zPCCq MVzpcoR2[2W|IFeyJIFzemW|dB?= MoD0NlM1OTh3MkO=
K029 M17MfmZ2dmO2aX;uJGF{e2G7 NWL6foxuOjVyIH7N NX;VXVB1OjRiaB?= MVfpcoR2[2W|IFexJIFzemW|dB?= NUHhVJpPOjN2MUi1NlM>
M23 MV3GeY5kfGmxbjDBd5NigQ>? NXK2XHRQOjVyIH7N M1rYWVI1KGh? NXHaeWlycW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> M3;EOlI{PDF6NUKz
K033 M4nib2Z2dmO2aX;uJGF{e2G7 NFrHZlgzPTBibl2= Ml7LNlQhcA>? NITzcHpqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36= MYOyN|QyQDV{Mx?=
K008 MmXzRZBweHSxc3nzJGF{e2G7 M2mwZVExOCCwTR?= Mmr6O|IhcA>? NXjsXGVne2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NGHqOWszOzRzOEWyNy=>
K028 MXHBdI9xfG:|aYOgRZN{[Xl? NU\tRmpVOTByIH7N M1HLb|czKGh? NF;MWHh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| Ml3oNlM1OTh3MkO=
K029 NXnCeXFFSXCxcITvd4l{KEG|c3H5 MWqxNFAhdk1? MUS3NkBp NWexcGxTe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MnmzNlM1OTh3MkO=
M23 NVWyOXQ4SXCxcITvd4l{KEG|c3H5 NV3nbIM{OTByIH7N M1L6bVczKGh? MXfzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M{DhdVI{PDF6NUKz
K033 NV;XXm05SXCxcITvd4l{KEG|c3H5 NE\6WmUyODBibl2= M1rwVVczKGh? MUnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MXKyN|QyQDV{Mx?=
RD M33wWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC0VXRKSzVyPUigcm0> NV;OS29mOjN|MEO3OFE>
Rh41 MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonJTWM2OD1zMD60JI5O NYLSUHhwOjN|MEO3OFE>
Rh18 M1nQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTZwMjDuUS=> NVzFNYJ6OjN|MEO3OFE>
Rh30 M{[2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPJbJNKSzVyPUWuOkBvVQ>? NV7ETnJSOjN|MEO3OFE>
BT-12 NUX0e2E{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXmTWM2OD1zND6zJI5O NWrGVXUxOjN|MEO3OFE>
CHLA-266 M2faZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf2TWM2OD1{Nz6xJI5O M4m5NlI{OzB|N{Sx
TC-71 NFTvdGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{T0VWlEPTB;ND61JI5O MVKyN|MxOzd2MR?=
CHLA-9 M1v3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m2UWlEPTB;ND62JI5O NX:4OJl1OjN|MEO3OFE>
CHLA-10 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXOflR{UUN3ME21Mlchdk1? MoK2NlM{ODN5NEG=
CHLA-258 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjqTWM2OD14LkSgcm0> MWqyN|MxOzd2MR?=
SJ-GBM2 NIHDNWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LjbmlEPTB;MUKuPUBvVQ>? NWDRTXJQOjN|MEO3OFE>
NB-1643 M4XQXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmG5TWM2OD15LkSgcm0> M4LWSlI{OzB|N{Sx
NB-EBc1 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL1TWM2OD1zNj64JI5O Ml\TNlM{ODN5NEG=
CHLA-90 NED2cZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG2VWdKSzVyPUKyMlMhdk1? Mn23NlM{ODN5NEG=
CHLA-136 NVT1dVZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTJ|LkKgcm0> M3u5blI{OzB|N{Sx
NALM-6 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7BRVJlUUN3ME2xNU44KG6P MmDhNlM{ODN5NEG=
COG-LL-317 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj1cXF1UUN3ME20MlQhdk1? MXKyN|MxOzd2MR?=
RS4;11 M3fiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TuTGlEPTB;MUOuOUBvVQ>? NX3nNolWOjN|MEO3OFE>
MOLT-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXsfmhKSzVyPUGwMlYhdk1? MUCyN|MxOzd2MR?=
CCRF-CEM (1) NVfuOVlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPXOZdKSzVyPUGyMlUhdk1? NV;UXJZuOjN|MEO3OFE>
CCRF-CEM (2) NFHR[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTdwMjDuUS=> M4\ON|I{OzB|N{Sx
Kasumi-1 NHuzc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXrTWM2OD13Lkigcm0> MViyN|MxOzd2MR?=
Karpas-299 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLRUHNKSzVyPUmuOkBvVQ>? NH32coIzOzNyM{e0NS=>
Ramos-RA1 Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLRe|ZvUUN3ME23MlQhdk1? MmnGNlM{ODN5NEG=
LNCaP NVTHN5BTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojVTWM2OD16IH7N M2[zc|I{OTV{MEC0
VCaP MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HvSWlEPTB;NzDuUS=> NUDQN4t4OjNzNUKwNFQ>
H1355 M1rWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW1[GFGUUN3ME21JI5O MkKyNlMxOTJ{NEi=
H157 MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTdibl2= M3HwVVI{ODF{MkS4
H460 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;WOXdZUUN3ME24JI5O NYL1SGZvOjNyMUKyOFg>
IA-LM M2jmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLIPFJuUUN3ME2xNEBvVQ>? MkLoNlMxOTJ{NEi=
HOP-62 NFXuUpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFzIH7N MmXCNlMxOTJ{NEi=
H23 NGmwbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH24fGlKSzVyPUGxJI5O NHvTRY8zOzBzMkK0PC=>
H2030 M{TKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH4cFdxUUN3ME2xNkBvVQ>? MlTXNlMxOTJ{NEi=
H441 NX;T[Hl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjTVWJLUUN3ME2xOEBvVQ>? NGjSbVEzOzBzMkK0PC=>
H2212 M{PKT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF5IH7N NW\BZnFoOjNyMUKyOFg>
SK-LU-1 NFfzToxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z2NWlEPTB;MUigcm0> MlnDNlMxOTJ{NEi=
H2009 NUixTZFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF7IH7N M33NOFI{ODF{MkS4
H1792 MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWzemFKUUN3ME2yNEBvVQ>? NFrBfmgzOzBzMkK0PC=>
COR-L23 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;GUnBzUUN3ME2yNkBvVQ>? M4n6eVI{ODF{MkS4
H727 MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTOTWM2OD1{ODDuUS=> MViyN|AyOjJ2OB?=
H1734 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTZTWM2OD1{ODDuUS=> NEPxS2wzOzBzMkK0PC=>
H358 NEjRfIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX0TWM2OD1{OTDuUS=> NWfzdJg2OjNyMUKyOFg>
A549 NEO1OJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDqTWM2OD12MzDuUS=> NFPKdYszOzBzMkK0PC=>
H2122 MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[xTWM2OD13MzDuUS=> NHv3RpkzOzBzMkK0PC=>
Calu-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCzTGNkUUN3ME21PEBvVQ>? M{jFeVI{ODF{MkS4
Calu-6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLqVIdKSzVyPU[0JI5O MYiyN|AyOjJ2OB?=
NCI-H1975 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\iOFghcA>? NGP4eZVKSzVyPUG2JI5O NEHvSVIzOjF2NE[2OS=>
NCI-H1975 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPsO|IhcA>? M37ZNGlEPTB;ODDuUS=> MkTyNlIyPDR4NkW=

... 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
  • Formulation: In DMSO and diluted 1:10 with 20% Cremophor RH 40
  • 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

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).

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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

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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.

  • * Indicates a Required Field

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