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 21 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 M1j6[2Fxd3C2b4Ppd{BCe3OjeR?= MX[zNE85OC9zNUCvNlUxKG6P MXeyOE81QC95MjDo NYSwXppJcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ Mn3lNlU5QDJ3NUC=
MV411 NUjQcGxOSXCxcITvd4l{KEG|c3H5 MXGzNE85OC9zNUCvNlUxKG6P NXLBdJd7OjRxNEivO|IhcA>? NWKxdJJ2cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ NUWz[G82OjV6OEK1OVA>
MGC-803 MnPZR4VtdCCYaXHibYxqfHliQYPzZZk> NFG4W4QxNjFvMUCwNEBvVQ>? MWK3NkBp MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NWS4[3RrOjV3OUC4NFU>
SGC-7901 MlzTR4VtdCCYaXHibYxqfHliQYPzZZk> MXSwMlEuOTByMDDuUS=> M3PBeVczKGh? MlnWbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MorRNlU2QTB6MEW=
MKN-28 M2fa[GNmdGxiVnnhZoltcXS7IFHzd4F6 M4TX[lAvOS1zMECwJI5O NEfuNpA4OiCq M{TncYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MWGyOVU6ODhyNR?=
MGC-803 MoniSpVv[3Srb36gRZN{[Xl? NGDHb5YxNjFvMUCwNEBvVQ>? MoLyNlQhcA>? MUnpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> MWGyOVU6ODhyNR?=
HCT-116 Mly2SpVv[3Srb36gRZN{[Xl? NInjbZM2OG6P M{fv[VI1KGh? NVzUNo1mTE2VTx?= MYHpcoR2[2WmIFewM2cyKGG{cnXzeC=> NGnrO|QzPTJzMEe5OC=>
HT-29 NHTYOI9HfW6ldHnvckBCe3OjeR?= MlPIOVBvVQ>? MnHONlQhcA>? NEPG[VhFVVOR M4G5N4lv\HWlZXSgS|AwTzFiYYLy[ZN1 NEm0NFEzPTJzMEe5OC=>
SCC25 Ml\tR5l1d3irY3n0fUBCe3OjeR?= M3f5fVExNzVyIH7N MUCyOEBp NHHjWmll\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MYGyOVIxPTR|MB?=
FUDA NF;tVmxEgXSxeHnjbZR6KEG|c3H5 MlvTNVAwPTBibl2= NUC1fVBHOjRiaB?= MX7k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NEXNTVMzPTJyNUSzNC=>
Detroit562 NWHGUJNiS3m2b4jpZ4l1gSCDc4PhfS=> MkHrNVAwPTBibl2= M2nmSFI1KGh? M37nc4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NX\F[IJvOjV{MEW0N|A>
CAL27 M3;FcGN6fG:6aXPpeJkhSXO|YYm= NV;kRY9VOTBxNUCgcm0> MXeyOEBp MUXk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NUWyRlBkOjV{MEW0N|A>
DSH1 NGH5TYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTZibl2= M2rDb|I1Pzh2OEO5
SW-1710 NFH1VIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTNPVFKSzVyPU[gcm0> MXeyOFc5PDh|OR?=
T24 NUnmOIdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqySmpKSzVyPUegcm0> NGjYXYozPDd6NEizPS=>
RT112 NHXVbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTlibl2= NWjhUHl6OjR5OES4N|k>
639-V MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M325RWlEPTB;MUCgcm0> MV2yOFc5PDh|OR?=
SCaBER MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm5N|ZwUUN3ME2xNEBvVQ>? NWTHXXNmOjR5OES4N|k>
BFTC NXjiU|k{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe0R4VHUUN3ME2xO{BvVQ>? NXXvboVKOjR5OES4N|k>
J82 MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7Sb5hnUUN3ME2xPEBvVQ>? M1nrXVI1Pzh2OEO5
HT-1376 NHixZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K4[GlEPTB;MkGgcm0> NULQUWV[OjR5OES4N|k>
647-V NHLHcFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW5OmxpUUN3ME2yO{BvVQ>? NGnVcpYzPDd6NEizPS=>
UM-UC3 M1LXcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nqXmlEPTB;M{Ogcm0> Mn7QNlQ4QDR6M{m=
LB831-BLC M1jNR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLyTWM2OD1|NDDuUS=> M1jX[lI1Pzh2OEO5
KU-19-19 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTN4IH7N NYPnRXBmOjR5OES4N|k>
35612 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;NTWM2OD1|ODDuUS=> NIDlSoozPDd6NEizPS=>
5637 NXXqZVY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTR2IH7N NYLSRm5LOjR5OES4N|k>
HT-1197 NV;EPHdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTV|IH7N NV[wSnBSOjR5OES4N|k>
MGH-U3 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELuN4RKSzVyPUWzJI5O MojTNlQ4QDR6M{m=
TCCSUP NUP6N25kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fyR2lEPTB;MUSyJI5O MUGyOFc5PDh|OR?=
RT4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFG2WGhKSzVyPUG3N|Mhdk1? NH\5RlYzPDd6NEizPS=>
SW780 MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjuNJR4UUN3ME2zOFUyKG6P NYrDSZpoOjR5OES4N|k>
RKO MojBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nuXWlEPTB;NDDuUS=> NV[0fHZTOjR4OEK3OFc>
LS-411 N MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXNV4xKSzVyPUWgcm0> NFTaSI4zPDZ6Mke0Oy=>
SW620 M{f6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX0TWM2OD16IH7N NXvEcWxHOjR4OEK3OFc>
HCT-15 NF60W4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrUd4hPUUN3ME24JI5O NIq5[24zPDZ6Mke0Oy=>
HuTu-80 Mo[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF|IH7N NXvwT3RLOjR4OEK3OFc>
HCT 116 M2jpW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\ZOG1KSzVyPUG0JI5O MX[yOFY5Ojd2Nx?=
COLO-205 NFXCSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF2IH7N MmH3NlQ3QDJ5NEe=
NCI-H747 NXnGU5JmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXITWM2OD1zNzDuUS=> M{PqPFI1Pjh{N{S3
COLO-678 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJzIH7N MoHQNlQ3QDJ5NEe=
LoVo MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPZN213UUN3ME2yNkBvVQ>? NWXpSlR4OjR4OEK3OFc>
LS-1034 MnjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf6WYFCUUN3ME2zNUBvVQ>? M{X2VVI1Pjh{N{S3
SNU-C2B M1qzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTR3IH7N Ml\wNlQ3QDJ5NEe=
LS-123 NEH1WY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFS4boxKSzVyPUezJI5O NUC4clc1OjR4OEK3OFc>
SK-CO-1 M1XnZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknUTWM2OD16MTDuUS=> NF\3T|kzPDZ6Mke0Oy=>
HCC2998 M1:1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT6bm5KSzVyPUGyPEBvVQ>? MXyyOFY5Ojd2Nx?=
MDA-MB-231 Mnm4SpVv[3Srb36gRZN{[Xl? Mn7qNVAxKG6P M1rJZ|MxKG2rbh?= NVvmWmlVcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NUD4T4VtOjR{NEiyOlU>
MDA-MB-435 NGrkfWFHfW6ldHnvckBCe3OjeR?= MVKxNFAhdk1? NXHGWpJ4OzBibXnu MWfpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MXGyOFI1QDJ4NR?=
BT-20  NGW1bFdHfW6ldHnvckBCe3OjeR?= NFzQd4gyODBxMkWwJI5O M3;xflI1KGh? MYXy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> MV[yOFE4OzV2MR?=
MDA-MB-231 MXXGeY5kfGmxbjDBd5NigQ>? MWSxNFAhdk1? NX3UO2RZOjRiaB?= MknDbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> NUPURpJ[OjRzN{O1OFE>
H82 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD1eIlSUUN3ME2zNE4zPyCwTR?= M2H5W|I1OTZ4NUC1
GLC4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJyLkS3JI5O M{HlfVI1OTZ4NUC1
H69 NEfqfolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDHc3BKSzVyPUizMlM3KG6P NVTR[4F5OjRzNk[1NFU>
H128 NVTqS3ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEKydYRKSzVyPU[5MlU2KG6P NH\QVpkzPDF4NkWwOS=>
H146 NHLTSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDrd3lKSzVyPUK4MlUyKG6P NFnVVpEzPDF4NkWwOS=>
H187 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrHfpRKSzVyPUK0Mlk6KG6P MVmyOFE3PjVyNR?=
H526 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH0SpFKSzVyPUKxMlY1KG6P M{C1U|I1OTZ4NUC1
N592 NGfwcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLTTWM2OD1zND6xNkBvVQ>? NXjFb4NkOjRzNk[1NFU>
H620 M3XPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jrPWlEPTB;M{KuOlchdk1? NYjaWG9KOjRzNk[1NFU>
H792 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDTTWM2OD12NT6wO{BvVQ>? MlTPNlQyPjZ3MEW=
H1173 NUXzVHhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnYV5FuUUN3ME2xNk43OiCwTR?= NF7VXXkzPDF4NkWwOS=>
AC3 MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjWTWM2OD1{NT65JI5O M1Pq[lI1OTZ4NUC1
H82 NW\FNYlqTnWwY4Tpc44hSXO|YYm= M3:0Z|MxKG6P MWS3NkBp M17nSYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M4j5b|I1OTZ4NUC1
GLC4 NEnNRnpHfW6ldHnvckBCe3OjeR?= NVzudY5jOzBibl2= MnHpO|IhcA>? MUPpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= M1uxZlI1OTZ4NUC1
H146  Mom3SpVv[3Srb36gRZN{[Xl? MVqzNEBvVQ>? NFTq[pU4OiCq MX7pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= M13pO|I1OTZ4NUC1
OVCAR-5 MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXGwMVExODBibl2= NHLOdWo4OiCq MnrMbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MoXXNlM6ODBzM{[=
OVCAR-8 NGK1VZdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV3FTVlQOC1zMECwJI5O MXu3NkBp Mn21bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MoTYNlM6ODBzM{[=
A1847 NYnLTHVsS2WubDDWbYFjcWyrdImgRZN{[Xl? NYDDeolJOC1zMECwJI5O M4\xNVczKGh? MVrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkHaNlM6ODBzM{[=
SKOV-3 NFzieG5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHTHUW0xNTFyMECgcm0> MUC3NkBp NED0TGdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NH7wTnUzOzlyMEGzOi=>
OVCAR-5 MVnBdI9xfG:|aYOgRZN{[Xl? MmGwNVAuOTByIH7N NEm2W|gzPC92OD:3NkBp NYCwV5MxcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> Mn7nNlM6ODBzM{[=
OVCAR-8 M3zLU2Fxd3C2b4Ppd{BCe3OjeR?= NF\YbVAyOC1zMECgcm0> M176SVI1NzR6L{eyJIg> NVzn[GM{cW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MkjZNlM6ODBzM{[=
A1847 NXXzfXM4SXCxcITvd4l{KEG|c3H5 NWHoZmdrOTBvMUCwJI5O MYWyOE81QC95MjDo NVixOYZicW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M330VFI{QTByMUO2
H2228 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGrXdIUxNTFyMECgcm0> MmXvO|IhcA>? NYSweXd6UUN3ME2xN{BvVQ>? M{LGNlI{PTN|Mk[1
H3122 NIXK[llE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFLRUHcxNTFyMECgcm0> M4DxfVczKGh? MlL1TWM2OD1zMDDuUS=> NES2SGEzOzV|M{K2OS=>
K008 M2DPRmNmdGxiVnnhZoltcXS7IFHzd4F6 Ml7ITWM2OD14MDDuUS=> NUPyfJJSOjN2MUi1NlM>
K028 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4D2VGlEPTB;OESgcm0> NIricFUzOzRzOEWyNy=>
K029 MoqwR4VtdCCYaXHibYxqfHliQYPzZZk> NX\kfnNSUUN3ME20OkBvVQ>? NXnnSHQ5OjN2MUi1NlM>
M23 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NW\EZpN{UUN3ME2zO{42KG6P NYXLcIp[OjN2MUi1NlM>
K033 NX\oWXNTS2WubDDWbYFjcWyrdImgRZN{[Xl? NEXYeINKSzVyPUe1MlUhdk1? MX[yN|QyQDV{Mx?=
K008 Mn\HSpVv[3Srb36gRZN{[Xl? NFm2UHQzPTBibl2= MVuyOEBp MX7pcoR2[2W|IFeyJIFzemW|dB?= NIrQZoUzOzRzOEWyNy=>
K028 M1G3eWZ2dmO2aX;uJGF{e2G7 MmjLNlUxKG6P M1O4TFI1KGh? MYnpcoR2[2W|IFeyJIFzemW|dB?= M4rWWlI{PDF6NUKz
K029 M1e2VWZ2dmO2aX;uJGF{e2G7 M4\5UFI2OCCwTR?= NUe5WHd6OjRiaB?= MXPpcoR2[2W|IFexJIFzemW|dB?= Ml3sNlM1OTh3MkO=
M23 NXLsUG5KTnWwY4Tpc44hSXO|YYm= Ml75NlUxKG6P NHjNRmUzPCCq NXfDNohScW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> M1HzTVI{PDF6NUKz
K033 M4npNWZ2dmO2aX;uJGF{e2G7 MVOyOVAhdk1? NEPvdXczPCCq MW\pcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? M{nzW|I{PDF6NUKz
K008 NFn2PYZCeG:ydH;zbZMhSXO|YYm= M4DKZVExOCCwTR?= M3fPTFczKGh? Mn25d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MVyyN|QyQDV{Mx?=
K028 M1\lNGFxd3C2b4Ppd{BCe3OjeR?= M3OzVVExOCCwTR?= M1L0UlczKGh? MWDzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MYGyN|QyQDV{Mx?=
K029 NID6fFZCeG:ydH;zbZMhSXO|YYm= Moi3NVAxKG6P NVXYT3l{PzJiaB?= NFPnXnp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M1PUUVI{PDF6NUKz
M23 NEfwXHVCeG:ydH;zbZMhSXO|YYm= M1L4SFExOCCwTR?= NVPoSZdoPzJiaB?= NYiy[FVDe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MXSyN|QyQDV{Mx?=
K033 MojGRZBweHSxc3nzJGF{e2G7 NYPNOVVFOTByIH7N MVK3NkBp MYjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NXPVOYR1OjN2MUi1NlM>
RD MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LKfmlEPTB;ODDuUS=> NETTVXczOzNyM{e0NS=>
Rh41 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnznTWM2OD1zMD60JI5O MX[yN|MxOzd2MR?=
Rh18 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF60U5FKSzVyPU[uNkBvVQ>? M4DYTFI{OzB|N{Sx
Rh30 M3HGO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF32dndKSzVyPUWuOkBvVQ>? NULtO4ljOjN|MEO3OFE>
BT-12 M3e1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrWWnB3UUN3ME2xOE4{KG6P MXeyN|MxOzd2MR?=
CHLA-266 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jLRWlEPTB;MkeuNUBvVQ>? M17NcFI{OzB|N{Sx
TC-71 NGDIeYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHWxUWVKSzVyPUSuOUBvVQ>? NIHw[4YzOzNyM{e0NS=>
CHLA-9 MmHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HoWWlEPTB;ND62JI5O MUGyN|MxOzd2MR?=
CHLA-10 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTVwNzDuUS=> NWHRNmV{OjN|MEO3OFE>
CHLA-258 M{DPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTZwNDDuUS=> NV7zWZloOjN|MEO3OFE>
SJ-GBM2 NVq4UI9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vYbGlEPTB;MUKuPUBvVQ>? NYH3bplyOjN|MEO3OFE>
NB-1643 NYXZOXIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Xo[2lEPTB;Nz60JI5O NXXxcFYyOjN|MEO3OFE>
NB-EBc1 M3P1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF4Lkigcm0> M33TeFI{OzB|N{Sx
CHLA-90 NXraOnd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[yNWlEPTB;MkKuN{BvVQ>? MlnHNlM{ODN5NEG=
CHLA-136 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn5TXIyUUN3ME2yN{4zKG6P M3rlZVI{OzB|N{Sx
NALM-6 Mk\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFzLkegcm0> NVHn[5VsOjN|MEO3OFE>
COG-LL-317 M2X3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLBVm1xUUN3ME20MlQhdk1? NFzZWngzOzNyM{e0NS=>
RS4;11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfWcY9lUUN3ME2xN{42KG6P NGDMfIkzOzNyM{e0NS=>
MOLT-4 NID1OnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLGUGhKSzVyPUGwMlYhdk1? NHOwT4YzOzNyM{e0NS=>
CCRF-CEM (1) M4qwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z4NWlEPTB;MUKuOUBvVQ>? MXyyN|MxOzd2MR?=
CCRF-CEM (2) NF\INWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj4TWM2OD15LkKgcm0> M3;jWVI{OzB|N{Sx
Kasumi-1 NVPlOFlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVyyfpU{UUN3ME21Mlghdk1? MUOyN|MxOzd2MR?=
Karpas-299 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEG4cXRKSzVyPUmuOkBvVQ>? NUe0NHZoOjN|MEO3OFE>
Ramos-RA1 NVfDTY1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTdwNDDuUS=> M4m1XVI{OzB|N{Sx
LNCaP M4PHZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS5b3hFUUN3ME24JI5O NYLJbHVLOjNzNUKwNFQ>
VCaP M1PXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTPd2FTUUN3ME23JI5O M1O1flI{OTV{MEC0
H1355 NXfBO45XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTVibl2= NFWzOngzOzBzMkK0PC=>
H157 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHqcGhKSzVyPUegcm0> MUeyN|AyOjJ2OB?=
H460 NW[wb|RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPMWZJSUUN3ME24JI5O MVKyN|AyOjJ2OB?=
IA-LM MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofYTWM2OD1zMDDuUS=> NGLHSmozOzBzMkK0PC=>
HOP-62 MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHzTWM2OD1zMTDuUS=> Mn7tNlMxOTJ{NEi=
H23 M1zKZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnpTWM2OD1zMTDuUS=> NWTIUZI{OjNyMUKyOFg>
H2030 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf3Tld1UUN3ME2xNkBvVQ>? MU[yN|AyOjJ2OB?=
H441 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDL[I1xUUN3ME2xOEBvVQ>? MkC3NlMxOTJ{NEi=
H2212 MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTGTWM2OD1zNzDuUS=> MlXYNlMxOTJ{NEi=
SK-LU-1 M{WyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF6IH7N M2LTc|I{ODF{MkS4
H2009 NXrxW|RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTDTWM2OD1zOTDuUS=> MUGyN|AyOjJ2OB?=
H1792 NXO0[|R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fUbmlEPTB;MkCgcm0> M3mwblI{ODF{MkS4
COR-L23 NXH4[4JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn1TWM2OD1{MjDuUS=> NH2yU2kzOzBzMkK0PC=>
H727 M3zWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDwcm1KSzVyPUK4JI5O MnHENlMxOTJ{NEi=
H1734 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJ6IH7N MXeyN|AyOjJ2OB?=
H358 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjvVnVKSzVyPUK5JI5O NWrCW5pzOjNyMUKyOFg>
A549 M{XV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3sUHJ6UUN3ME20N{BvVQ>? MWeyN|AyOjJ2OB?=
H2122 Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTx[ph7UUN3ME21N{BvVQ>? M3;Kc|I{ODF{MkS4
Calu-1 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXETWM2OD13ODDuUS=> NVX1Zos2OjNyMUKyOFg>
Calu-6 M2P2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlniTWM2OD14NDDuUS=> NGfXUXIzOzBzMkK0PC=>
NCI-H1975 M2K1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO0PEBp M4S5S2lEPTB;MU[gcm0> M4jDO|IzOTR2Nk[1
NCI-H1975 NXTvWZJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[zSIY4OiCq Ml;wTWM2OD16IH7N M4flWlIzOTR2Nk[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
  • 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

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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)

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Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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