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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In DMSO USD 302 In stock
USD 270 In stock
USD 370 In stock
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3 Customer Reviews

  • Loss of viability (Z score) resulting from HSP90 inhibition (HSP90i; ganetespib, 5 nM) in FANCA null GM6914 cells transduced with retroviruses encoding FANCA wild-type (squares; WT) or empty vector control (circles; null) in the presence (black symbols) of MMC (31.6 nM) or DMSO control (gray symbols). Data from three independent experiments are presented as mean ± SEM.

    Cell, 2017, 168(5):856-866. Ganetespib (STA-9090) purchased from Selleck.

    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

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 NHflWmVCeG:ydH;zbZMhSXO|YYm= NHXDTII{OC96MD:xOVAwOjVyIH7N Mn\iNlQwPDhxN{KgbC=> NFfmfYpqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MmO4NlU5QDJ3NUC=
MV411 MlrkRZBweHSxc3nzJGF{e2G7 NUjQc3FTOzBxOECvNVUxNzJ3MDDuUS=> NHmySZAzPC92OD:3NkBp M4G5e4lv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NYnLZYd4OjV6OEK1OVA>
MGC-803 MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkXLNE4yNTFyMECgcm0> NVLMOXp4PzJiaB?= NWDifoVFcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3fiN|I2PTlyOEC1
SGC-7901 NUjuPGN3S2WubDDWbYFjcWyrdImgRZN{[Xl? M12wT|AvOS1zMECwJI5O MUi3NkBp MmDBbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXeyOVU6ODhyNR?=
MKN-28 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{mweVAvOS1zMECwJI5O MWe3NkBp MlOybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NXjIdWhQOjV3OUC4NFU>
MGC-803 MoPYSpVv[3Srb36gRZN{[Xl? M1LCV|AvOS1zMECwJI5O NXr2NpBZOjRiaB?= NEnrXG1qdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? NV;qXm5qOjV3OUC4NFU>
HCT-116 MVXGeY5kfGmxbjDBd5NigQ>? NICzToY2OG6P NVXP[49bOjRiaB?= MVHEUXNQ Mly0bY5lfWOnZDDHNE9IOSCjcoLld5Q> MnvyNlUzOTB5OUS=
HT-29 MX3GeY5kfGmxbjDBd5NigQ>? NF3DcoQ2OG6P M4TMO|I1KGh? MYPEUXNQ MnSwbY5lfWOnZDDHNE9IOSCjcoLld5Q> MViyOVIyODd7NB?=
SCC25 M37oNmN6fG:6aXPpeJkhSXO|YYm= NYTONVA2OTBxNUCgcm0> NX:5R|BiOjRiaB?= M{XzboRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NVHEZ4ZsOjV{MEW0N|A>
FUDA M1G4fGN6fG:6aXPpeJkhSXO|YYm= NVGz[Zl3OTBxNUCgcm0> MX2yOEBp MoXt[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MlHTNlUzODV2M{C=
Detroit562 M{nnfGN6fG:6aXPpeJkhSXO|YYm= MkXLNVAwPTBibl2= NF\rXFUzPCCq M1PW[YRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MYCyOVIxPTR|MB?=
CAL27 NIrFeHVEgXSxeHnjbZR6KEG|c3H5 NUHubpJzOTBxNUCgcm0> MoGyNlQhcA>? M2C0OIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MXOyOVIxPTR|MB?=
DSH1 M{HaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknOTWM2OD14IH7N NEnPTHAzPDd6NEizPS=>
SW-1710 NUfI[4poT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojQTWM2OD14IH7N MViyOFc5PDh|OR?=
T24 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzUbVdmUUN3ME23JI5O MV:yOFc5PDh|OR?=
RT112 MljyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTOPGVuUUN3ME25JI5O MVuyOFc5PDh|OR?=
639-V MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\QdlNkUUN3ME2xNEBvVQ>? MViyOFc5PDh|OR?=
SCaBER M17Gfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFyIH7N NVyzdXgzOjR5OES4N|k>
BFTC MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DSc2lEPTB;MUegcm0> MXWyOFc5PDh|OR?=
J82 NV;GZ4IyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTF6IH7N MXeyOFc5PDh|OR?=
HT-1376 NGXyeYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:zXGdKSzVyPUKxJI5O NX;V[XdsOjR5OES4N|k>
647-V MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJ5IH7N NV\uWnlqOjR5OES4N|k>
UM-UC3 M1\ZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTN|IH7N MWmyOFc5PDh|OR?=
LB831-BLC NXPBOm5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HvZWlEPTB;M{Sgcm0> MYOyOFc5PDh|OR?=
KU-19-19 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPtco5KSzVyPUO2JI5O MWmyOFc5PDh|OR?=
35612 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe5c3pRUUN3ME2zPEBvVQ>? MlWyNlQ4QDR6M{m=
5637 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzJcmpKSzVyPUS0JI5O M1PNT|I1Pzh2OEO5
HT-1197 NXLWO2Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj6N2h1UUN3ME21N{BvVQ>? MmnjNlQ4QDR6M{m=
MGH-U3 NYPaeIxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrPZY53UUN3ME21N{BvVQ>? NEHQO2QzPDd6NEizPS=>
TCCSUP M4TEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnYVZFKSzVyPUG0NkBvVQ>? NXTYcnNQOjR5OES4N|k>
RT4 NXz5OIdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TYdmlEPTB;MUezN{BvVQ>? NFWwNGEzPDd6NEizPS=>
SW780 M3Pa[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;kTGlEPTB;M{S1NUBvVQ>? NFy4eHczPDd6NEizPS=>
RKO MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjienZKSzVyPUSgcm0> MXuyOFY5Ojd2Nx?=
LS-411 N Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTVibl2= MYmyOFY5Ojd2Nx?=
SW620 NEXCZ2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\3NpJKSzVyPUigcm0> M4LQNFI1Pjh{N{S3
HCT-15 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\oTWM2OD16IH7N NGO3NXEzPDZ6Mke0Oy=>
HuTu-80 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF|IH7N NVzrVohbOjR4OEK3OFc>
HCT 116 MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XWRWlEPTB;MUSgcm0> NY\6VYw3OjR4OEK3OFc>
COLO-205 NIKyXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvwNIxLUUN3ME2xOEBvVQ>? NYTRfHRVOjR4OEK3OFc>
NCI-H747 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPaeZV6UUN3ME2xO{BvVQ>? MoPJNlQ3QDJ5NEe=
COLO-678 NEWxZnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\XcVRGUUN3ME2yNUBvVQ>? MV6yOFY5Ojd2Nx?=
LoVo NH3IfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;HXpdsUUN3ME2yNkBvVQ>? M{mwPFI1Pjh{N{S3
LS-1034 NEnOOYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vEV2lEPTB;M{Ggcm0> MWiyOFY5Ojd2Nx?=
SNU-C2B NYi4XphbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17HZWlEPTB;NEWgcm0> MWmyOFY5Ojd2Nx?=
LS-123 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTd|IH7N NXHDZ2pZOjR4OEK3OFc>
SK-CO-1 NEfocmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HnemlEPTB;OEGgcm0> MViyOFY5Ojd2Nx?=
HCC2998 M2jmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTF{ODDuUS=> M1TkXVI1Pjh{N{S3
MDA-MB-231 M{O3XGZ2dmO2aX;uJGF{e2G7 M2LhdVExOCCwTR?= NYHUTnJVOzBibXnu NVT6cHhGcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NV;5Ro9vOjR{NEiyOlU>
MDA-MB-435 M4\Be2Z2dmO2aX;uJGF{e2G7 M17iUVExOCCwTR?= M3zYcFMxKG2rbh?= Mmj4bY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NVXwSVV4OjR{NEiyOlU>
BT-20  MYrGeY5kfGmxbjDBd5NigQ>? MUWxNFAwOjVyIH7N MlT3NlQhcA>? NEKxUG9z\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? NV\FOnE1OjRzN{O1OFE>
MDA-MB-231 M1nXXWZ2dmO2aX;uJGF{e2G7 M2r2eVExOCCwTR?= M3LkcFI1KGh? NVfOdHNHcW6qaXLpeJMhfGinIH3p[5JifG:{eTDhcoQhcW64YYPpeoUh[2GyYXPpeJnDqA>? NF3PVlMzPDF5M{W0NS=>
H82 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nkbmlEPTB;M{CuNlchdk1? MUeyOFE3PjVyNR?=
GLC4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJyLkS3JI5O M{XIPFI1OTZ4NUC1
H69 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v6RmlEPTB;OEOuN|Yhdk1? NYDPSJJvOjRzNk[1NFU>
H128 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP3[|BJUUN3ME22PU42PSCwTR?= MVuyOFE3PjVyNR?=
H146 NE[zcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzTWM2OD1{OD61NUBvVQ>? Mn3INlQyPjZ3MEW=
H187 NELOdmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJ2Lkm5JI5O MWGyOFE3PjVyNR?=
H526 NGTqdJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nZ[GlEPTB;MkGuOlQhdk1? M4TT[FI1OTZ4NUC1
N592 M4DpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPQTHo3UUN3ME2xOE4yOiCwTR?= MnXINlQyPjZ3MEW=
H620 NUfMRVQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Xvb2lEPTB;M{KuOlchdk1? MlLLNlQyPjZ3MEW=
H792 MlKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTR3LkC3JI5O M{D2cVI1OTZ4NUC1
H1173 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuwSJBKSzVyPUGyMlYzKG6P NV36V|VGOjRzNk[1NFU>
AC3 NYi4RWJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIWzOG5KSzVyPUK1Mlkhdk1? NF7OepczPDF4NkWwOS=>
H82 M2PJRmZ2dmO2aX;uJGF{e2G7 MUWzNEBvVQ>? M37QelczKGh? MkXZbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NFPIbHczPDF4NkWwOS=>
GLC4 NGXxPXNHfW6ldHnvckBCe3OjeR?= Mn7hN|Ahdk1? MmP1O|IhcA>? NGnnPFhqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NVH1PWN1OjRzNk[1NFU>
H146  Mn\ESpVv[3Srb36gRZN{[Xl? NYm1dFluOzBibl2= NIjN[5g4OiCq NIfD[XJqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MX[yOFE3PjVyNR?=
OVCAR-5 NYfYRXVuS2WubDDWbYFjcWyrdImgRZN{[Xl? NHvJeIsxNTFyMECgcm0> M4jmeFczKGh? MYrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4H4VlI{QTByMUO2
OVCAR-8 NYX3RoJsS2WubDDWbYFjcWyrdImgRZN{[Xl? M2Pub|AuOTByMDDuUS=> Mnu1O|IhcA>? NWn5dnJ2cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3jlT|I{QTByMUO2
A1847 M4rUOWNmdGxiVnnhZoltcXS7IFHzd4F6 MlvuNE0yODByIH7N NXzFRWVtPzJiaB?= NX7IT5FtcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MlO5NlM6ODBzM{[=
SKOV-3 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYSwMVExODBibl2= Mn:3O|IhcA>? NHzmR5pqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MV2yN|kxODF|Nh?=
OVCAR-5 Ml;URZBweHSxc3nzJGF{e2G7 M{W0PFExNTFyMDDuUS=> NVnDVWt7OjRxNEivO|IhcA>? NFq0SINqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M{XEOlI{QTByMUO2
OVCAR-8 Ml3IRZBweHSxc3nzJGF{e2G7 M1vHZlExNTFyMDDuUS=> NHTFTGIzPC92OD:3NkBp M371U4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= M3faT|I{QTByMUO2
A1847 M3z6fmFxd3C2b4Ppd{BCe3OjeR?= NGHXfmEyOC1zMECgcm0> NX;CdWkxOjRxNEivO|IhcA>? M{nheolv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= M{LiUFI{QTByMUO2
H2228 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVWwMVExODBibl2= MVS3NkBp MVLJR|UxRTF|IH7N NF6zSJUzOzV|M{K2OS=>
H3122 MoPsR4VtdCCYaXHibYxqfHliQYPzZZk> NWK4UVdJOC1zMECwJI5O MlXRO|IhcA>? Mkj5TWM2OD1zMDDuUS=> MXiyN|U{OzJ4NR?=
K008 MmCyR4VtdCCYaXHibYxqfHliQYPzZZk> MlnJTWM2OD14MDDuUS=> M1TVcVI{PDF6NUKz
K028 M3PUdmNmdGxiVnnhZoltcXS7IFHzd4F6 M1nKN2lEPTB;OESgcm0> M4DId|I{PDF6NUKz
K029 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3u5[WlEPTB;NE[gcm0> M{PGcVI{PDF6NUKz
M23 M4HFUmNmdGxiVnnhZoltcXS7IFHzd4F6 MYrJR|UxRTN5LkWgcm0> Mo[4NlM1OTh3MkO=
K033 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXTVSpVwUUN3ME23OU42KG6P MWOyN|QyQDV{Mx?=
K008 M2jVT2Z2dmO2aX;uJGF{e2G7 MnLlNlUxKG6P NInNU2gzPCCq Ml:2bY5lfWOnczDHNkBienKnc4S= MWOyN|QyQDV{Mx?=
K028 NHXBO5JHfW6ldHnvckBCe3OjeR?= M{OzR|I2OCCwTR?= NVuxd2pQOjRiaB?= MmOwbY5lfWOnczDHNkBienKnc4S= M4TNblI{PDF6NUKz
K029 NHWwUZNHfW6ldHnvckBCe3OjeR?= NXHJdYs3OjVyIH7N NWjrN|lCOjRiaB?= NFHMZ4hqdmS3Y3XzJGcyKGG{cnXzeC=> NIPYRZAzOzRzOEWyNy=>
M23 NIP0ZYRHfW6ldHnvckBCe3OjeR?= M1\i[FI2OCCwTR?= NUHEfIlrOjRiaB?= M{L3bYlv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 NGDwflMzOzRzOEWyNy=>
K033 NEHYNmxHfW6ldHnvckBCe3OjeR?= M174b|I2OCCwTR?= MYWyOEBp NXPmZXlFcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u MViyN|QyQDV{Mx?=
K008 NVvxO5FoSXCxcITvd4l{KEG|c3H5 NYfrcnpKOTByIH7N M4fSS|czKGh? NHrDcFZ{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M1fGTlI{PDF6NUKz
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K029 NWrGOIhGSXCxcITvd4l{KEG|c3H5 MYixNFAhdk1? MmroO|IhcA>? NFm3UHZ{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MX[yN|QyQDV{Mx?=
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... 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:[1]
+ 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:[4]
+ 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 Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
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
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 )

  • C1
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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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Completed Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 9, 2014 Phase 1
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 Terminated Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 Phase 1|Phase 2
NCT02272478 Recruiting Acute Myeloid Leukaemia|Myelodysplastic Syndrome Cardiff University|Cancer Research UK October 2014 Phase 3

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

Related HSP (e.g. HSP90) Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID