Ganetespib (STA-9090)

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.

Price Stock Quantity  
USD 302 In stock
USD 270 In stock
USD 370 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Ganetespib (STA-9090) Chemical Structure

Ganetespib (STA-9090) Chemical Structure
Molecular Weight: 364.4

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

Related Compound Libraries

Ganetespib (STA-9090) is available in the following compound libraries:

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

  • Selective HSP90 Inhibitor

    NVP-BEP800 HSP90β-selective, IC50=58 nM.

  • Most Potent HSP90 Inhibitor

    KW-2478 HSP90, IC50=3.8 nM.

  • HSP90 Inhibitor in Clinical Trial

    17-AAG (Tanespimycin) Phase III for Gastrointestinal Stromal Tumors.

  • Newest HSP90 Inhibitor

    XL888 ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

Product Information

  • Compare HSP (e.g. HSP90) Inhibitors
    Compare HSP (e.g. HSP90) Products
  • Research Area

Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HL60M4XwfWFxd3C2b4Ppd{BCe3OjeR?=NYDqR4tCOzBxOECvNVUxNzJ3MDDuUS=>NF7sbFgzPC92OD:3NkBpMnL5bY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nzMVyyOVg5OjV3MB?=
MV411MlLkRZBweHSxc3nzJGF{e2G7Mlr5N|AwQDBxMUWwM|I2OCCwTR?=NYnNeph7OjRxNEivO|IhcA>?NGnKclRqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM>M333eFI2QDh{NUWw
MGC-803MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=>MoH1NE4yNTFyMECgcm0>NYDYOZM5PzJiaB?=MlnTbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?M3ThPVI2PTlyOEC1
SGC-7901NHi0NVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>?MYCwMlEuOTByMDDuUS=>NXTFWXZoPzJiaB?=NVjZUottcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=M1XURVI2PTlyOEC1
MKN-28MlHaR4VtdCCYaXHibYxqfHliQYPzZZk>MnfDNE4yNTFyMECgcm0>MofCO|IhcA>?Ml\zbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?MUWyOVU6ODhyNR?=
MGC-803M1;yemZ2dmO2aX;uJGF{e2G7NYX6So9VOC5zLUGwNFAhdk1?MoHNNlQhcA>?MWLpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q>MknZNlU2QTB6MEW=
HCT-116NVzy[GxqTnWwY4Tpc44hSXO|YYm=M2HHOlUxdk1?NYjsWIJZOjRiaB?=MmLGSG1UVw>?NF7LUVNqdmS3Y3XkJGcxN0dzIHHydoV{fA>?NWXQNIE{OjV{MUC3PVQ>
HT-29NWr5WJVRTnWwY4Tpc44hSXO|YYm=M{DVWlUxdk1?Mn3jNlQhcA>?MnTBSG1UVw>?NEPkdHVqdmS3Y3XkJGcxN0dzIHHydoV{fA>?MkTONlUzOTB5OUS=
SCC25MUjDfZRwgGmlaYT5JGF{e2G7MmnoNVAwPTBibl2=NHXuOpAzPCCqM1LCbYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=>NVPIRoFKOjV{MEW0N|A>
FUDANEfyN4lEgXSxeHnjbZR6KEG|c3H5NU\1[2EzOTBxNUCgcm0>NYDzSHJoOjRiaB?=MXjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=MVGyOVIxPTR|MB?=
Detroit562MX7DfZRwgGmlaYT5JGF{e2G7NUnEUmt1OTBxNUCgcm0>NIfEXmwzPCCqMWPk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=MX2yOVIxPTR|MB?=
CAL27M{jJVWN6fG:6aXPpeJkhSXO|YYm=M{LzdFExNzVyIH7NMYiyOEBpNW\GVY5M\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6NFX0enEzPTJyNUSzNC=>
DSH1M1HMemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYDJR|UxRTZibl2=NWO1ZXp7OjR5OES4N|k>
SW-1710MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUnEZ|RLUUN3ME22JI5ONXrjfXlLOjR5OES4N|k>
T24NVi2dFdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXr0RlhbUUN3ME23JI5ONFLMR3czPDd6NEizPS=>
RT112M{TRW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7Ml7yTWM2OD17IH7NNGTPbYwzPDd6NEizPS=>
639-VNGnSVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF7oR|VKSzVyPUGwJI5OMYmyOFc5PDh|OR?=
SCaBERMVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnvTTWM2OD1zMDDuUS=>MUmyOFc5PDh|OR?=
BFTCNVHCZnBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUXJR|UxRTF5IH7NNYXGSnJwOjR5OES4N|k>
J82Mm[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NEfMSpRKSzVyPUG4JI5ONIfhWHAzPDd6NEizPS=>
HT-1376MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYHBWosxUUN3ME2yNUBvVQ>?Mli1NlQ4QDR6M{m=
647-VNED1V3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXG5PIJQUUN3ME2yO{BvVQ>?NFX4Sm0zPDd6NEizPS=>
UM-UC3M4X5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1fVPGlEPTB;M{Ogcm0>NX\a[lc2OjR5OES4N|k>
LB831-BLCNYDEcmp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1voUmlEPTB;M{Sgcm0>M3XyfVI1Pzh2OEO5
KU-19-19MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MknwTWM2OD1|NjDuUS=>NYTqeINuOjR5OES4N|k>
35612NVPQemIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{[3OWlEPTB;M{igcm0>MUeyOFc5PDh|OR?=
5637NX:1Z5NNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFf4VYhKSzVyPUS0JI5ONHTtdokzPDd6NEizPS=>
HT-1197NITlPZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnXtTWM2OD13MzDuUS=>MYSyOFc5PDh|OR?=
MGH-U3NILqTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFrKfG1KSzVyPUWzJI5OM4nUe|I1Pzh2OEO5
TCCSUPNGTKXlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MU\JR|UxRTF2MjDuUS=>MY[yOFc5PDh|OR?=
RT4M{LWeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXW1TIppUUN3ME2xO|M{KG6PMVeyOFc5PDh|OR?=
SW780M4fmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUTJR|UxRTN2NUGgcm0>MlXyNlQ4QDR6M{m=
RKOM4DSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MV;JR|UxRTRibl2=NWfuUWRVOjR4OEK3OFc>
LS-411 NNHvVZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF;UXWZKSzVyPUWgcm0>M4G1clI1Pjh{N{S3
SW620MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXPJR|UxRThibl2=M3;BclI1Pjh{N{S3
HCT-15MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWr4NVdQUUN3ME24JI5ONVLLeoFEOjR4OEK3OFc>
HuTu-80Mk\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MneyTWM2OD1zMzDuUS=>MoXSNlQ3QDJ5NEe=
HCT 116MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVrJR|UxRTF2IH7NNWL5ZnRvOjR4OEK3OFc>
COLO-205MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mo\hTWM2OD1zNDDuUS=>M1;OU|I1Pjh{N{S3
NCI-H747NVTiTYR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3i2dWlEPTB;MUegcm0>NYHUTW5EOjR4OEK3OFc>
COLO-678M13ZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHjHc2dKSzVyPUKxJI5ONXHmXXVoOjR4OEK3OFc>
LoVoNF3vdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkP0TWM2OD1{MjDuUS=>MVyyOFY5Ojd2Nx?=
LS-1034MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnfBTWM2OD1|MTDuUS=>NVHPRYZrOjR4OEK3OFc>
SNU-C2BM2LmU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MorPTWM2OD12NTDuUS=>NF;M[nIzPDZ6Mke0Oy=>
LS-123M3vjOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MV3JR|UxRTd|IH7NNYXjdJpwOjR4OEK3OFc>
SK-CO-1NE\4OYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFHYW|JKSzVyPUixJI5OMYeyOFY5Ojd2Nx?=
HCC2998MkW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmTITWM2OD1zMkigcm0>NIjPcGgzPDZ6Mke0Oy=>
MDA-MB-231M330SGZ2dmO2aX;uJGF{e2G7Mo\5NVAxKG6PNGjDU2Y{OCCvaX6=NGXnfIJqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?=NVLEdZZGOjR{NEiyOlU>
MDA-MB-435NXK4N4NETnWwY4Tpc44hSXO|YYm=M1;QWlExOCCwTR?=NVTlVnl[OzBibXnuNHPUc4VqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?=MmjCNlQzPDh{NkW=
BT-20 MUnGeY5kfGmxbjDBd5NigQ>?NFfocHoyODBxMkWwJI5OMV2yOEBpNVLxNZNEemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGIMmrlNlQyPzN3NEG=
MDA-MB-231NFfm[ndHfW6ldHnvckBCe3OjeR?=MnzxNVAxKG6PMXiyOEBpMkLlbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=>MYqyOFE4OzV2MR?=
H82NF\MPJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{DmcmlEPTB;M{CuNlchdk1?MVqyOFE3PjVyNR?=
GLC4NVex[oVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4GxdWlEPTB;MkCuOFchdk1?NF;sbnMzPDF4NkWwOS=>
H69NIL5NlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NG\UWIZKSzVyPUizMlM3KG6PMmj5NlQyPjZ3MEW=
H128MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Ml;MTWM2OD14OT61OUBvVQ>?M2fJ[lI1OTZ4NUC1
H146M1f5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlnHTWM2OD1{OD61NUBvVQ>?MYKyOFE3PjVyNR?=
H187MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MY\JR|UxRTJ2Lkm5JI5ONFvqb|YzPDF4NkWwOS=>
H526MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlzRTWM2OD1{MT62OEBvVQ>?NV3mXodzOjRzNk[1NFU>
N592NHXXd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2DVd2lEPTB;MUSuNVIhdk1?M3frNlI1OTZ4NUC1
H620NGf4cnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnH3TWM2OD1|Mj62O{BvVQ>?NIHuUHgzPDF4NkWwOS=>
H792MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVz5fWpiUUN3ME20OU4xPyCwTR?=MV6yOFE3PjVyNR?=
H1173Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGTGWVdKSzVyPUGyMlYzKG6PMkjUNlQyPjZ3MEW=
AC3NYLjSmVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2fke2lEPTB;MkWuPUBvVQ>?MYOyOFE3PjVyNR?=
H82MUjGeY5kfGmxbjDBd5NigQ>?NYjqVpFuOzBibl2=NGDYdVA4OiCqM3SycYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=>MWeyOFE3PjVyNR?=
GLC4MV;GeY5kfGmxbjDBd5NigQ>?MVWzNEBvVQ>?MkThO|IhcA>?MV\pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S=M3H4Z|I1OTZ4NUC1
H146 NW\HXpk4TnWwY4Tpc44hSXO|YYm=M{TVRVMxKG6PNIjjT4Q4OiCqMnfvbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0MkXSNlQyPjZ3MEW=
OVCAR-5NHX0[VNE\WyuIG\pZYJqdGm2eTDBd5NigQ>?M2XZZlAuOTByMDDuUS=>MlHLO|IhcA>?M2fJTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?MY[yN|kxODF|Nh?=
OVCAR-8MmPSR4VtdCCYaXHibYxqfHliQYPzZZk>NUKwOFNCOC1zMECwJI5OMlnrO|IhcA>?NVrBc2VwcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=NGXMOlMzOzlyMEGzOi=>
A1847M3rVVWNmdGxiVnnhZoltcXS7IFHzd4F6NH;wTpoxNTFyMECgcm0>NHHLUVA4OiCqM2HIRYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?M3vQZlI{QTByMUO2
SKOV-3NHXXOoJE\WyuIG\pZYJqdGm2eTDBd5NigQ>?MknPNE0yODByIH7NMXe3NkBpM4PUfIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?MmP6NlM6ODBzM{[=
OVCAR-5NI\WTpFCeG:ydH;zbZMhSXO|YYm=MUCxNE0yODBibl2=NI\4VGozPC92OD:3NkBpMnKybY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?=NV65[Zd[OjN7MECxN|Y>
OVCAR-8MkDKRZBweHSxc3nzJGF{e2G7NV7Uc2lYOTBvMUCwJI5OM1q2WFI1NzR6L{eyJIg>MYrpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7MWiyN|kxODF|Nh?=
A1847MX7BdI9xfG:|aYOgRZN{[Xl?NHPBVVUyOC1zMECgcm0>M3P3PVI1NzR6L{eyJIg>NGjDdnNqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5MW[yN|kxODF|Nh?=
H2228M1XUfWNmdGxiVnnhZoltcXS7IFHzd4F6NX7QT5dxOC1zMECwJI5ONHj3UmE4OiCqMkjBTWM2OD1zMzDuUS=>NXf6SIluOjN3M{OyOlU>
H3122MkDJR4VtdCCYaXHibYxqfHliQYPzZZk>NXjifoE{OC1zMECwJI5OMkLNO|IhcA>?Ml3yTWM2OD1zMDDuUS=>NXPicZQ4OjN3M{OyOlU>
K008MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=>M2jCW2lEPTB;NkCgcm0>M{H5VlI{PDF6NUKz
K028MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=>NWi5dWdjUUN3ME24OEBvVQ>?M3O4dFI{PDF6NUKz
K029M1vwbmNmdGxiVnnhZoltcXS7IFHzd4F6MY\JR|UxRTR4IH7NNE\nUJYzOzRzOEWyNy=>
M23MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=>M1PmfGlEPTB;M{euOUBvVQ>?M1uzSVI{PDF6NUKz
K033M2\LVGNmdGxiVnnhZoltcXS7IFHzd4F6MkLYTWM2OD15NT61JI5OMlThNlM1OTh3MkO=
K008NGL5U3VHfW6ldHnvckBCe3OjeR?=MXKyOVAhdk1?NHftcoczPCCqM1LLXYlv\HWlZYOgS|Ih[XK{ZYP0MYqyN|QyQDV{Mx?=
K028NV25b5RKTnWwY4Tpc44hSXO|YYm=NFH1PXozPTBibl2=MkLRNlQhcA>?M3vjNYlv\HWlZYOgS|Ih[XK{ZYP0NXXROolmOjN2MUi1NlM>
K029NIj4c2pHfW6ldHnvckBCe3OjeR?=NX\CTI96OjVyIH7NMoruNlQhcA>?NVi2Z3lTcW6mdXPld{BIOSCjcoLld5Q>NFfMUGszOzRzOEWyNy=>
M23MoP4SpVv[3Srb36gRZN{[Xl?NYTVWXFkOjVyIH7NNYi1O5l3OjRiaB?=M2P6Rolv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0NHS0WmkzOzRzOEWyNy=>
K033M4TyfWZ2dmO2aX;uJGF{e2G7MmKwNlUxKG6PNFv2UpQzPCCqM{HxPIlv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?=M{T5TlI{PDF6NUKz
K008M1HqW2Fxd3C2b4Ppd{BCe3OjeR?=NILabpUyODBibl2=M2[0TVczKGh?NITpWmh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|NWnsXWdUOjN2MUi1NlM>
K028NXrGV4JJSXCxcITvd4l{KEG|c3H5Moq2NVAxKG6PNGfWTJQ4OiCqMVTzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{NFq0Oo8zOzRzOEWyNy=>
K029M3eyT2Fxd3C2b4Ppd{BCe3OjeR?=NYjGeZZ3OTByIH7NMX23NkBpNInQbYV{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m|NHfWR3UzOzRzOEWyNy=>
M23MXfBdI9xfG:|aYOgRZN{[Xl?M4\2[VExOCCwTR?=M1\xV|czKGh?M1rXZ5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN?NV;qbYE1OjN2MUi1NlM>
K033MknxRZBweHSxc3nzJGF{e2G7NYnmRlltOTByIH7NMX:3NkBpMWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{M3zQflI{PDF6NUKz
RDNYewXZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWrlfoxnUUN3ME24JI5OMlfTNlM{ODN5NEG=
Rh41MlrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{izUmlEPTB;MUCuOEBvVQ>?MYKyN|MxOzd2MR?=
Rh18NHz6[GVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVTyV3VYUUN3ME22MlIhdk1?M1m0N|I{OzB|N{Sx
Rh30M3XzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlTsTWM2OD13Lk[gcm0>MnvMNlM{ODN5NEG=
BT-12MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHHaR|JKSzVyPUG0MlMhdk1?NVvTVFNJOjN|MEO3OFE>
CHLA-266M{TIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NELPVllKSzVyPUK3MlEhdk1?MVSyN|MxOzd2MR?=
TC-71NWXY[2pET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWrJR|UxRTRwNTDuUS=>MoDONlM{ODN5NEG=
CHLA-9NXeyTnh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkfBTWM2OD12Lk[gcm0>NGf5fYQzOzNyM{e0NS=>
CHLA-10MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXfJR|UxRTVwNzDuUS=>NVnLZ25ROjN|MEO3OFE>
CHLA-258MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIexenBKSzVyPU[uOEBvVQ>?NHnzcpczOzNyM{e0NS=>
SJ-GBM2MnvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkHCTWM2OD1zMj65JI5ONU\lXGNxOjN|MEO3OFE>
NB-1643MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFzqV|lKSzVyPUeuOEBvVQ>?MXeyN|MxOzd2MR?=
NB-EBc1NYK2PGpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWLvUmZGUUN3ME2xOk45KG6PNXfN[4JGOjN|MEO3OFE>
CHLA-90Mn;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4q3PWlEPTB;MkKuN{BvVQ>?M3;3ZVI{OzB|N{Sx
CHLA-136MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVjJR|UxRTJ|LkKgcm0>MnvZNlM{ODN5NEG=
NALM-6NW\lXZZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NEn0N2RKSzVyPUGxMlchdk1?MlHwNlM{ODN5NEG=
COG-LL-317NWH5[IlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUPJR|UxRTRwNDDuUS=>Mn7QNlM{ODN5NEG=
RS4;11M2\wS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUHJR|UxRTF|LkWgcm0>NF3PRo0zOzNyM{e0NS=>
MOLT-4MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mo\LTWM2OD1zMD62JI5OMnHINlM{ODN5NEG=
CCRF-CEM (1)NWmyOFlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{D1U2lEPTB;MUKuOUBvVQ>?NIWwW44zOzNyM{e0NS=>
CCRF-CEM (2)M4\IWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYHwW4lbUUN3ME23MlIhdk1?M2XlNFI{OzB|N{Sx
Kasumi-1Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkDuTWM2OD13Lkigcm0>NGnqZ3QzOzNyM{e0NS=>
Karpas-299Ml7wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3vQNmlEPTB;OT62JI5OMm\oNlM{ODN5NEG=
Ramos-RA1M2DEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF:0cItKSzVyPUeuOEBvVQ>?NEX2VFkzOzNyM{e0NS=>
LNCaPMn73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYnuWoMxUUN3ME24JI5OMWqyN|E2OjByNB?=
VCaPMYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUTJR|UxRTdibl2=NF;EeFkzOzF3MkCwOC=>
H1355NUPFO3dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHzwNGdKSzVyPUWgcm0>M{nzc|I{ODF{MkS4
H157Mn\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3HiO2lEPTB;NzDuUS=>MX6yN|AyOjJ2OB?=
H460MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlGyTWM2OD16IH7NM{LNclI{ODF{MkS4
IA-LMMVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlPITWM2OD1zMDDuUS=>MXKyN|AyOjJ2OB?=
HOP-62MkDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIqxeZNKSzVyPUGxJI5OM{jtWlI{ODF{MkS4
H23M16xW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnnJTWM2OD1zMTDuUS=>M4HLd|I{ODF{MkS4
H2030NIDNSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlLrTWM2OD1zMjDuUS=>Mn7aNlMxOTJ{NEi=
H441MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUXPS2FJUUN3ME2xOEBvVQ>?M3zk[VI{ODF{MkS4
H2212M2TqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnnZTWM2OD1zNzDuUS=>NF[4fZkzOzBzMkK0PC=>
SK-LU-1MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUPJR|UxRTF6IH7NMXeyN|AyOjJ2OB?=
H2009NXnIfmwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmTLTWM2OD1zOTDuUS=>NU\qZ2M1OjNyMUKyOFg>
H1792NYG5fVB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmXTTWM2OD1{MDDuUS=>MV6yN|AyOjJ2OB?=
COR-L23NVvUbW9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnrlTWM2OD1{MjDuUS=>M{D2VlI{ODF{MkS4
H727NGXxTW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3X2VWlEPTB;Mkigcm0>M3Prd|I{ODF{MkS4
H1734MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmS1TWM2OD1{ODDuUS=>NGPDVmEzOzBzMkK0PC=>
H358NW\aRpJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mo[2TWM2OD1{OTDuUS=>MXWyN|AyOjJ2OB?=
A549MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NH7Sd4VKSzVyPUSzJI5OMm\uNlMxOTJ{NEi=
H2122MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{PycmlEPTB;NUOgcm0>M2HneFI{ODF{MkS4
Calu-1M2f4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{f2XmlEPTB;NUigcm0>NF\TfYwzOzBzMkK0PC=>
Calu-6MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEDJ[GdKSzVyPU[0JI5ONGO0OYszOzBzMkK0PC=>
NCI-H1975MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{Hvd|Q5KGh?M3zwRWlEPTB;MU[gcm0>Ml;FNlIyPDR4NkW=
NCI-H1975NXfkSWRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF36[ZY4OiCqMXjJR|UxRThibl2=MUWyNlE1PDZ4NR?=

... Click to View More Cell Line Experimental Data

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]
Features

Protocol(Only for Reference)

Cell Assay: [1]

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.

Animal Study: [4]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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

References

[1] McCleese Jk, et al. Int J Cancer. 2009, 125(12), 2792-2801.

[2] Wang Y, et al. Curr Opin Investig Drugs. 2010 , 11(12), 1466-1476.

view more

Chemical Information

Download Ganetespib (STA-9090) SDF
Molecular Weight (MW) 364.4
Formula

C20H20N4O3

CAS No. 888216-25-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 40 mg/mL (109.76 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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.
Chemical Name 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one

Customer Product Validation (2)


Click to enlarge
Rating
Source Cancer Res 2014 10.1158/0008-5472.CAN-14-1017. Ganetespib (STA-9090) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231, SKM1, PaTu2, A549, HCT-116 cells
Concentrations 0-1.0 uM
Incubation Time 24 h
Results To investigate whether PRKD2 stability is affected after pharmacologic HSP90 inhibition, eight human cancer cell lines representing six different tumor types (breast cancer, pancreatic cancer, lung cancer, colon cancer, acutemyeloid leukemia, and glioblastoma) were incubated for 24 hours with increasing concentrations of two different compounds: PU-H71, an optimized water soluble member of the purine class of HSP90 inhibitors and STA-9090, a resor-cinol-containing triazole molecule with a novel chemical structure, both unrelated to the geldanamycin class of HSP90 inhibitors. Both inhibitors caused dose-dependent degradation of PRKD2 in all tumor cell lines. STA-9090 was associated with increased apoptosis as revealed by augmented PARP and caspase-9 cleavage in all tumor cell lines.

Click to enlarge
Rating
Source Hum Mol Genet, 2015, 10.1093/hmg/ddv136. Ganetespib (STA-9090) purchased from Selleck
Method Western Blot
Cell Lines Pkd1 null MEK cells、Pkd1 mutant PN24 cells
Concentrations 0-200 nM
Incubation Time 0-24 h
Results Treatment with STA9090, a second generation Hsp90 inhibitor that binds to ATP binding domain at the N-terminal of Hsp90, decreased the levels of Brd4 protein in Pkd1 mutant MEK cells and PN24 cells in a dose- and time-dependent manner.

Product Use Citation (4)

Tech Support & FAQs

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.

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

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

* Indicates a Required Field

Related HSP (e.g. HSP90) Products

  • PU-H71

    PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

  • KNK437

    KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

  • 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.

  • 17-AAG (Tanespimycin)

    17-AAG (Tanespimycin) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2.

    Features:Displays very low toxicity toward normal cells.

  • Luminespib (AUY-922, NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.

  • 17-DMAG (Alvespimycin) HCl

    17-DMAG (Alvespimycin) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

    Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.

  • Geldanamycin

    Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

  • 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.

  • Elesclomol (STA-4783)

    Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.

  • Onalespib (AT13387)

    Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

Recently Viewed Items

Tags: buy Ganetespib (STA-9090) | Ganetespib (STA-9090) supplier | purchase Ganetespib (STA-9090) | Ganetespib (STA-9090) cost | Ganetespib (STA-9090) manufacturer | order Ganetespib (STA-9090) | Ganetespib (STA-9090) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us