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.

Size Price Stock Quantity  
In DMSO USD 302 In stock
USD 270 In stock
USD 370 In stock

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  • Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.

    Cancer Res 2014 10.1158/0008-5472.CAN-14-1017. Ganetespib (STA-9090) purchased from Selleck.

    Western blot analysis of the expression of Brd4 and Hsp90 from whole-cell lysates of Pkd1 null MEK cells and Pkd1 mutant PN24 cells treated with STA9090 at indicated concentrations for 24 h (B), and in Pkd1 null MEK cells and Pkd1 mutant PN24 cells treated with STA9090 (200 nM) at indicated time points (C).

    Hum Mol Genet, 2015, 10.1093/hmg/ddv136. Ganetespib (STA-9090) purchased from Selleck.

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NFH6RnZCeG:ydH;zbZMhSXO|YYm= MkO5N|AwQDBxMUWwM|I2OCCwTR?= M13kU|I1NzR6L{eyJIg> MYfpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= MUKyOVg5OjV3MB?=
MV411 MUnBdI9xfG:|aYOgRZN{[Xl? M4TNNVMxNzhyL{G1NE8zPTBibl2= Mm\hNlQwPDhxN{KgbC=> MXPpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= Mo\6NlU5QDJ3NUC=
MGC-803 NEPrVVdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVjPeFNUOC5zLUGwNFAhdk1? MVO3NkBp NV6wWZNWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M33ZZ|I2PTlyOEC1
SGC-7901 MoTuR4VtdCCYaXHibYxqfHliQYPzZZk> NWPDeYx{OC5zLUGwNFAhdk1? MmXhO|IhcA>? NWjGfVFQcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NI\EfpMzPTV7MEiwOS=>
MKN-28 M4HXemNmdGxiVnnhZoltcXS7IFHzd4F6 M{nZXVAvOS1zMECwJI5O M1PQXlczKGh? NV;GO5NlcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MojZNlU2QTB6MEW=
MGC-803 MWfGeY5kfGmxbjDBd5NigQ>? NGfwPWkxNjFvMUCwNEBvVQ>? M1fGfFI1KGh? NVnWUZpKcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NGflcmMzPTV7MEiwOS=>
HCT-116 M2HVemZ2dmO2aX;uJGF{e2G7 MWK1NI5O MWeyOEBp NG[yZ2hFVVOR MVHpcoR2[2WmIFewM2cyKGG{cnXzeC=> NUnCO5p7OjV{MUC3PVQ>
HT-29 NEfpbGlHfW6ldHnvckBCe3OjeR?= M3fLTlUxdk1? MkfTNlQhcA>? NH\FU5FFVVOR MX;pcoR2[2WmIFewM2cyKGG{cnXzeC=> MlXaNlUzOTB5OUS=
SCC25 NHzZb4lEgXSxeHnjbZR6KEG|c3H5 MVexNE82OCCwTR?= M1TR[VI1KGh? MXPk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MX:yOVIxPTR|MB?=
FUDA MoXYR5l1d3irY3n0fUBCe3OjeR?= NEf0XFkyOC93MDDuUS=> NFj2PHozPCCq Mmn2[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MV:yOVIxPTR|MB?=
Detroit562 MUXDfZRwgGmlaYT5JGF{e2G7 NGHwRZEyOC93MDDuUS=> MnrxNlQhcA>? NFixZ2Fl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M{HUblI2OjB3NEOw
CAL27 NWDoOIc4S3m2b4jpZ4l1gSCDc4PhfS=> M1jrOVExNzVyIH7N Ml3MNlQhcA>? M4PJ[IRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M2r3UFI2OjB3NEOw
DSH1 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD0WINNUUN3ME22JI5O NFPzTpozPDd6NEizPS=>
SW-1710 NYqwVHFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq4OnFKSzVyPU[gcm0> MmS1NlQ4QDR6M{m=
T24 M4[wWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrwV|VKSzVyPUegcm0> NFnIOmgzPDd6NEizPS=>
RT112 NFHrbG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;1dHd4UUN3ME25JI5O MkHHNlQ4QDR6M{m=
639-V M4HreWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3ZOFBKSzVyPUGwJI5O M2C2U|I1Pzh2OEO5
SCaBER M17YN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFyIH7N M4jxelI1Pzh2OEO5
BFTC M4\yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF5IH7N NUf2O2JKOjR5OES4N|k>
J82 M3fvXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1voe2lEPTB;MUigcm0> NXrHOHlsOjR5OES4N|k>
HT-1376 NE\3c|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJzIH7N NIfkW5IzPDd6NEizPS=>
647-V NEmwV3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjv[HJKSzVyPUK3JI5O MYqyOFc5PDh|OR?=
UM-UC3 MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ObodKSzVyPUOzJI5O NWfBc3RsOjR5OES4N|k>
LB831-BLC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX0TWM2OD1|NDDuUS=> NGfZPWozPDd6NEizPS=>
KU-19-19 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjuR25xUUN3ME2zOkBvVQ>? NG\KbIczPDd6NEizPS=>
35612 NHjIWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDLRoVpUUN3ME2zPEBvVQ>? MVSyOFc5PDh|OR?=
5637 MmTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nS[2lEPTB;NESgcm0> NHL0XnAzPDd6NEizPS=>
HT-1197 NXLiSIxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4npN2lEPTB;NUOgcm0> MkCzNlQ4QDR6M{m=
MGH-U3 M3WydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\iTWM2OD13MzDuUS=> M1ziXlI1Pzh2OEO5
TCCSUP NV64WYViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF2MjDuUS=> MXGyOFc5PDh|OR?=
RT4 M2rKXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HpPGlEPTB;MUezN{BvVQ>? NGqzcGEzPDd6NEizPS=>
SW780 NXT0TFB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P4SmlEPTB;M{S1NUBvVQ>? NWnkdWNpOjR5OES4N|k>
RKO MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPFTWM2OD12IH7N NIrCfXYzPDZ6Mke0Oy=>
LS-411 N M{LsNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjFTWM2OD13IH7N MYSyOFY5Ojd2Nx?=
SW620 M3;IRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK4bZNkUUN3ME24JI5O NUfjPIEyOjR4OEK3OFc>
HCT-15 NWL3SGF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDCfIdKSzVyPUigcm0> Mn62NlQ3QDJ5NEe=
HuTu-80 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmP0TWM2OD1zMzDuUS=> M1\YNVI1Pjh{N{S3
HCT 116 MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHQemZ4UUN3ME2xOEBvVQ>? NGe3R3IzPDZ6Mke0Oy=>
COLO-205 NWr2TnQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTF2IH7N NFvlXZczPDZ6Mke0Oy=>
NCI-H747 NWjENWZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf0ZZRKSzVyPUG3JI5O Mlq5NlQ3QDJ5NEe=
COLO-678 M2r5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjwVY5rUUN3ME2yNUBvVQ>? MUWyOFY5Ojd2Nx?=
LoVo M{D2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC0TWM2OD1{MjDuUS=> NFL5PFMzPDZ6Mke0Oy=>
LS-1034 NILiU|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnCR2lKSzVyPUOxJI5O M3rjRVI1Pjh{N{S3
SNU-C2B NEnpfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXjWYtKSzVyPUS1JI5O NHrEOo4zPDZ6Mke0Oy=>
LS-123 M1:xWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHPXFFKSzVyPUezJI5O NXvndpdEOjR4OEK3OFc>
SK-CO-1 NGXpV5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzjUFRKSzVyPUixJI5O MVyyOFY5Ojd2Nx?=
HCC2998 MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF{ODDuUS=> M1T5NlI1Pjh{N{S3
MDA-MB-231 M2rESmZ2dmO2aX;uJGF{e2G7 MmXFNVAxKG6P Mn\PN|AhdWmw Mm[2bY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NWniSXdVOjR{NEiyOlU>
MDA-MB-435 M2CwNmZ2dmO2aX;uJGF{e2G7 NGLDUY8yODBibl2= MnfEN|AhdWmw MXzpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? Mm\PNlQzPDh{NkW=
BT-20  M3zkRWZ2dmO2aX;uJGF{e2G7 NXG3NYV3OTByL{K1NEBvVQ>? M2DmTFI1KGh? MUjy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> NHX0b|QzPDF5M{W0NS=>
MDA-MB-231 Mmm4SpVv[3Srb36gRZN{[Xl? M3v1ZVExOCCwTR?= MWCyOEBp M2nNTolvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> NWTFZXFuOjRzN{O1OFE>
H82 NF3PSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C5e2lEPTB;M{CuNlchdk1? MWCyOFE3PjVyNR?=
GLC4 NUXMe3VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DzcGlEPTB;MkCuOFchdk1? MnLCNlQyPjZ3MEW=
H69 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILmcHJKSzVyPUizMlM3KG6P Mn3lNlQyPjZ3MEW=
H128 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfoZ3lKSzVyPU[5MlU2KG6P NIHuTXEzPDF4NkWwOS=>
H146 NXiwPZV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPWRYZjUUN3ME2yPE42OSCwTR?= MljRNlQyPjZ3MEW=
H187 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrwTpFqUUN3ME2yOE46QSCwTR?= NXfNT3JVOjRzNk[1NFU>
H526 NFjrNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInacWhKSzVyPUKxMlY1KG6P NWTNVoRvOjRzNk[1NFU>
N592 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLWfYlsUUN3ME2xOE4yOiCwTR?= NEjIWpIzPDF4NkWwOS=>
H620 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[0cZhKSzVyPUOyMlY4KG6P M2S3TVI1OTZ4NUC1
H792 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojiTWM2OD12NT6wO{BvVQ>? Mk\nNlQyPjZ3MEW=
H1173 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moi4TWM2OD1zMj62NkBvVQ>? Mo\HNlQyPjZ3MEW=
AC3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ3Lkmgcm0> MXiyOFE3PjVyNR?=
H82 M4HyN2Z2dmO2aX;uJGF{e2G7 M136flMxKG6P MV63NkBp MoewbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MWSyOFE3PjVyNR?=
GLC4 MULGeY5kfGmxbjDBd5NigQ>? NYPubWtuOzBibl2= M2Hj[VczKGh? NEDufWhqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M{XUVFI1OTZ4NUC1
H146  NGnIXY1HfW6ldHnvckBCe3OjeR?= MUizNEBvVQ>? M4i1W|czKGh? MoPnbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MV:yOFE3PjVyNR?=
OVCAR-5 MlrrR4VtdCCYaXHibYxqfHliQYPzZZk> NGHERVUxNTFyMECgcm0> Mn;QO|IhcA>? NGK4W5ZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1jLNVI{QTByMUO2
OVCAR-8 NHPKRoxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYWwMVExODBibl2= M{G0elczKGh? NXn5b|I6cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4XVVVI{QTByMUO2
A1847 M1u5XGNmdGxiVnnhZoltcXS7IFHzd4F6 MU[wMVExODBibl2= M1;wb|czKGh? MnTvbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M{i1b|I{QTByMUO2
SKOV-3 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlTaNE0yODByIH7N NHO2PG44OiCq M4XNOYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M3jFPFI{QTByMUO2
OVCAR-5 NYLsOIN2SXCxcITvd4l{KEG|c3H5 MlPyNVAuOTByIH7N NIrJNXIzPC92OD:3NkBp NYXrSm5icW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NWHYZ|dqOjN7MECxN|Y>
OVCAR-8 MYDBdI9xfG:|aYOgRZN{[Xl? NUfyc41COTBvMUCwJI5O M2r5b|I1NzR6L{eyJIg> NVrvPZVQcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MnjGNlM6ODBzM{[=
A1847 M1O1dGFxd3C2b4Ppd{BCe3OjeR?= NUHa[INnOTBvMUCwJI5O MW[yOE81QC95MjDo MVjpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 NHK1WFEzOzlyMEGzOi=>
H2228 NUi5T|N6S2WubDDWbYFjcWyrdImgRZN{[Xl? MoDFNE0yODByIH7N MXm3NkBp MULJR|UxRTF|IH7N MUmyN|U{OzJ4NR?=
H3122 M4fMWGNmdGxiVnnhZoltcXS7IFHzd4F6 Ml6yNE0yODByIH7N MYq3NkBp MY\JR|UxRTFyIH7N MUiyN|U{OzJ4NR?=
K008 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmXHTWM2OD14MDDuUS=> MnWwNlM1OTh3MkO=
K028 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnPRTWM2OD16NDDuUS=> MV2yN|QyQDV{Mx?=
K029 NYLKe2d5S2WubDDWbYFjcWyrdImgRZN{[Xl? NFTWTZdKSzVyPUS2JI5O NHezO4wzOzRzOEWyNy=>
M23 NX;kN41jS2WubDDWbYFjcWyrdImgRZN{[Xl? NWqyNYxWUUN3ME2zO{42KG6P MnnUNlM1OTh3MkO=
K033 Mk\FR4VtdCCYaXHibYxqfHliQYPzZZk> MUnJR|UxRTd3LkWgcm0> M{S1[VI{PDF6NUKz
K008 MmL2SpVv[3Srb36gRZN{[Xl? NVPCN4ZOOjVyIH7N NH;Jd4IzPCCq M4nkOolv\HWlZYOgS|Ih[XK{ZYP0 MnPkNlM1OTh3MkO=
K028 MkX5SpVv[3Srb36gRZN{[Xl? NYrxTldbOjVyIH7N NGHMcYUzPCCq M4\veYlv\HWlZYOgS|Ih[XK{ZYP0 MVyyN|QyQDV{Mx?=
K029 NIr2SZFHfW6ldHnvckBCe3OjeR?= M4HnTFI2OCCwTR?= MoHkNlQhcA>? Mkn4bY5lfWOnczDHNUBienKnc4S= NUHTPZl4OjN2MUi1NlM>
M23 NFu2RW5HfW6ldHnvckBCe3OjeR?= NIqxTVgzPTBibl2= Ml60NlQhcA>? Mn;obY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= MUKyN|QyQDV{Mx?=
K033 M33TdmZ2dmO2aX;uJGF{e2G7 NEDxUI8zPTBibl2= M4K5VVI1KGh? MnnybY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NXu4WnVjOjN2MUi1NlM>
K008 NF\FfJVCeG:ydH;zbZMhSXO|YYm= NFXuXXcyODBibl2= MWO3NkBp Mlvyd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NU\6TJliOjN2MUi1NlM>
K028 MYXBdI9xfG:|aYOgRZN{[Xl? MUSxNFAhdk1? NVvi[oJkPzJiaB?= NX:wT2xNe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= M1\oSVI{PDF6NUKz
K029 NWrHToRMSXCxcITvd4l{KEG|c3H5 NXS3WVYxOTByIH7N M3zqXFczKGh? MUPzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M2HIS|I{PDF6NUKz
M23 MY\BdI9xfG:|aYOgRZN{[Xl? NE\jbWMyODBibl2= MkG5O|IhcA>? NGrPUVV{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MlmwNlM1OTh3MkO=
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SJ-GBM2 M{O2VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXETWM2OD1zMj65JI5O M3zB[lI{OzB|N{Sx
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COG-LL-317 NGDVW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ZTWM2OD12LkSgcm0> Ml\3NlM{ODN5NEG=
RS4;11 NYHsOZU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF|LkWgcm0> MV2yN|MxOzd2MR?=
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H1355 M1TyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTVibl2= NEfuUnYzOzBzMkK0PC=>
H157 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTdibl2= MmjBNlMxOTJ{NEi=
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H1792 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHjeGhKSzVyPUKwJI5O M{DNRlI{ODF{MkS4
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H727 M3jiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJ6IH7N NWj1WI9OOjNyMUKyOFg>
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H358 NXrucJZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXBSHpKSzVyPUK5JI5O MnHlNlMxOTJ{NEi=
A549 NX3oNFJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnpTWM2OD12MzDuUS=> MVqyN|AyOjJ2OB?=
H2122 NIDGV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTV|IH7N NHfXUI0zOzBzMkK0PC=>
Calu-1 NEm2T5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTV6IH7N NVLJZWRpOjNyMUKyOFg>
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NCI-H1975 NITYc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ENoE1QCCq Mki3TWM2OD1zNjDuUS=> MlSwNlIyPDR4NkW=
NCI-H1975 M4\BWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe1Zot5PzJiaB?= M4Dq[2lEPTB;ODDuUS=> MV:yNlE1PDZ4NR?=

... 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]

Protocol

Cell Research
+ Expand
  • 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
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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 (g) = Concentration (mol/L) × Volume (L) × 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

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 --
NCT02389751 Active, not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. April 2015 Phase 1
NCT02334319 Terminated Stage I Hypopharyngeal Squamous Cell Carcinoma|Stage I Laryngeal Squamous Cell Carcinoma|Stage I Oral Cavity Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma|Stage II Hypopharyngeal Squamous Cell Carcinoma|Stage II Laryngeal Squamous Cell Carcinoma|Stage II Oral Cavity Squamous Cell Carcinoma|Stage II Oropharyngeal Squamous Cell Carcinoma|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma Emory University|Synta Pharmaceuticals Corp. December 2014 Phase 1
NCT02261805 Recruiting Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 Phase 1|Phase 2
NCT02272478 Not yet recruiting Acute Myeloid Leukaemia|Myelodysplastic Syndrome Cardiff University|Cancer Research UK October 2014 Phase 3
NCT02192541 Completed Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 2014 Phase 1

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