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 MlPhRZBweHSxc3nzJGF{e2G7 M1X0ZlMxNzhyL{G1NE8zPTBibl2= MWOyOE81QC95MjDo NFXlWFRqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MmjpNlU5QDJ3NUC=
MV411 M4jnXmFxd3C2b4Ppd{BCe3OjeR?= NInIZYI{OC96MD:xOVAwOjVyIH7N M3\3ZVI1NzR6L{eyJIg> MXvpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= NGmwUVgzPTh6MkW1NC=>
MGC-803 NXW0bGpMS2WubDDWbYFjcWyrdImgRZN{[Xl? M1mzWlAvOS1zMECwJI5O MknMO|IhcA>? MlzFbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVviZ5czOjV3OUC4NFU>
SGC-7901 NVntS5JKS2WubDDWbYFjcWyrdImgRZN{[Xl? NXzZRmJ{OC5zLUGwNFAhdk1? MUC3NkBp M2DJUYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIL3Uo0zPTV7MEiwOS=>
MKN-28 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXvFVZA1OC5zLUGwNFAhdk1? MnXYO|IhcA>? MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M{nNSVI2PTlyOEC1
MGC-803 MoqxSpVv[3Srb36gRZN{[Xl? NF\pdpExNjFvMUCwNEBvVQ>? NHPtdWozPCCq NVX1Woo4cW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 MUeyOVU6ODhyNR?=
HCT-116 M37sZWZ2dmO2aX;uJGF{e2G7 M1\IZ|Uxdk1? NYric5VQOjRiaB?= NUezc|RpTE2VTx?= Mn7wbY5lfWOnZDDHNE9IOSCjcoLld5Q> M1LpT|I2OjFyN{m0
HT-29 MknkSpVv[3Srb36gRZN{[Xl? M4nnOFUxdk1? M2S3PFI1KGh? NIraW5hFVVOR MmnTbY5lfWOnZDDHNE9IOSCjcoLld5Q> NHv2flEzPTJzMEe5OC=>
SCC25 NYiyWXRtS3m2b4jpZ4l1gSCDc4PhfS=> NFrWZmEyOC93MDDuUS=> MUCyOEBp NVP0bZVq\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MUmyOVIxPTR|MB?=
FUDA MoPtR5l1d3irY3n0fUBCe3OjeR?= NYrxfHZoOTBxNUCgcm0> NFLm[mQzPCCq MWTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M1jIUVI2OjB3NEOw
Detroit562 NYKxVnlPS3m2b4jpZ4l1gSCDc4PhfS=> MkDyNVAwPTBibl2= MWiyOEBp MoDh[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MWeyOVIxPTR|MB?=
CAL27 MnHoR5l1d3irY3n0fUBCe3OjeR?= NF;BR5oyOC93MDDuUS=> MofvNlQhcA>? NEe1Nmll\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M3LmdFI2OjB3NEOw
DSH1 M1PNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXL1cmpxUUN3ME22JI5O NEnWU20zPDd6NEizPS=>
SW-1710 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTZibl2= NYLKSmdGOjR5OES4N|k>
T24 NYnHelVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfpbHRKSzVyPUegcm0> MlHFNlQ4QDR6M{m=
RT112 MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyxTWM2OD17IH7N NXHKNYhqOjR5OES4N|k>
639-V MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfxcHJHUUN3ME2xNEBvVQ>? MoCxNlQ4QDR6M{m=
SCaBER NUHOT2p4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPZbWFKSzVyPUGwJI5O NGnBTmMzPDd6NEizPS=>
BFTC M2j5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nDcGlEPTB;MUegcm0> Mn\xNlQ4QDR6M{m=
J82 M3zCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLHNZhrUUN3ME2xPEBvVQ>? MnrvNlQ4QDR6M{m=
HT-1376 M{jUTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmK4TWM2OD1{MTDuUS=> MlLmNlQ4QDR6M{m=
647-V MmnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ5IH7N M1PONFI1Pzh2OEO5
UM-UC3 M4XUd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKxW5JKSzVyPUOzJI5O NYTNTHRlOjR5OES4N|k>
LB831-BLC M3fmTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLvdGVDUUN3ME2zOEBvVQ>? NFezcm8zPDd6NEizPS=>
KU-19-19 NYHjPJlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\sTGlEPTB;M{[gcm0> NWT3NFloOjR5OES4N|k>
35612 NWPW[lRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGxSoFKSzVyPUO4JI5O Mne3NlQ4QDR6M{m=
5637 M1ex[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfsTWM2OD12NDDuUS=> M1\PZVI1Pzh2OEO5
HT-1197 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTLOHc3UUN3ME21N{BvVQ>? MlzsNlQ4QDR6M{m=
MGH-U3 NHrDNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vZeGlEPTB;NUOgcm0> M1L0elI1Pzh2OEO5
TCCSUP MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\JTopiUUN3ME2xOFIhdk1? NIDxfGEzPDd6NEizPS=>
RT4 NIe4fpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvQfY9KSzVyPUG3N|Mhdk1? MVWyOFc5PDh|OR?=
SW780 M{G0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTN2NUGgcm0> NV3oNWxNOjR5OES4N|k>
RKO Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXPfJRtUUN3ME20JI5O MXSyOFY5Ojd2Nx?=
LS-411 N M1fJc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljiTWM2OD13IH7N NX:5dFZlOjR4OEK3OFc>
SW620 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[zTWM2OD16IH7N NYrVb|B1OjR4OEK3OFc>
HCT-15 M2TuXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRThibl2= NUHkPGx2OjR4OEK3OFc>
HuTu-80 NFP3U45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX1RoFKSzVyPUGzJI5O NX;FNY44OjR4OEK3OFc>
HCT 116 M1vRfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLsdmRKSzVyPUG0JI5O NWrudHl2OjR4OEK3OFc>
COLO-205 NInJRmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX1TWM2OD1zNDDuUS=> M{C3TFI1Pjh{N{S3
NCI-H747 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvvTWM2OD1zNzDuUS=> NIL2U2UzPDZ6Mke0Oy=>
COLO-678 M3uxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;5dVNMUUN3ME2yNUBvVQ>? Mnv0NlQ3QDJ5NEe=
LoVo M4TPUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rnbmlEPTB;MkKgcm0> MWiyOFY5Ojd2Nx?=
LS-1034 M4K2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNzIH7N NUXmdnpxOjR4OEK3OFc>
SNU-C2B MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TuR2lEPTB;NEWgcm0> MmqzNlQ3QDJ5NEe=
LS-123 MnXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf0Z4tGUUN3ME23N{BvVQ>? MkOxNlQ3QDJ5NEe=
SK-CO-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[4TWM2OD16MTDuUS=> NYDWWJVPOjR4OEK3OFc>
HCC2998 NHTyTmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDY[YVTUUN3ME2xNlghdk1? MkK2NlQ3QDJ5NEe=
MDA-MB-231 MlPmSpVv[3Srb36gRZN{[Xl? MWOxNFAhdk1? M{LUNlMxKG2rbh?= M3Tl[olvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MoTDNlQzPDh{NkW=
MDA-MB-435 NFLQe4VHfW6ldHnvckBCe3OjeR?= M1zJO|ExOCCwTR?= MXOzNEBucW5? M1W0NIlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NYTyc|RlOjR{NEiyOlU>
BT-20  NGPJSFhHfW6ldHnvckBCe3OjeR?= MoTiNVAxNzJ3MDDuUS=> NYPxTGpYOjRiaB?= MkXKdoV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH NILnWY4zPDF5M{W0NS=>
MDA-MB-231 M{DaZmZ2dmO2aX;uJGF{e2G7 MmPKNVAxKG6P MWWyOEBp Mly1bY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> NGTsV|IzPDF5M{W0NS=>
H82 NE\GVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPmbHVKSzVyPUOwMlI4KG6P MVGyOFE3PjVyNR?=
GLC4 NF74[WZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ITWM2OD1{MD60O{BvVQ>? NHzsWlgzPDF4NkWwOS=>
H69 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTh|LkO2JI5O MV[yOFE3PjVyNR?=
H128 M2fIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MormTWM2OD14OT61OUBvVQ>? NIHDWXUzPDF4NkWwOS=>
H146 NX7ZOGY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJ6LkWxJI5O M33aUlI1OTZ4NUC1
H187 NEnNNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ2Lkm5JI5O MVyyOFE3PjVyNR?=
H526 NXW2PHZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrzZm9YUUN3ME2yNU43PCCwTR?= NFW4PIEzPDF4NkWwOS=>
N592 NXXsb5BXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWze2cyUUN3ME2xOE4yOiCwTR?= M1e2eFI1OTZ4NUC1
H620 NIrQVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN{Lk[3JI5O MUGyOFE3PjVyNR?=
H792 MlzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLSWHpkUUN3ME20OU4xPyCwTR?= M4DDU|I1OTZ4NUC1
H1173 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET0b4RKSzVyPUGyMlYzKG6P M2f5WVI1OTZ4NUC1
AC3 NEnXRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfTTWM2OD1{NT65JI5O NGDSW3AzPDF4NkWwOS=>
H82 NUPtPFVXTnWwY4Tpc44hSXO|YYm= Mm\YN|Ahdk1? MY[3NkBp NF60eItqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NF7HWHMzPDF4NkWwOS=>
GLC4 NXXzdW17TnWwY4Tpc44hSXO|YYm= MV:zNEBvVQ>? M4XvRVczKGh? MnrxbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NGDWNJYzPDF4NkWwOS=>
H146  NWnGfWN[TnWwY4Tpc44hSXO|YYm= MYmzNEBvVQ>? NWLNVYJlPzJiaB?= MXjpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NFruem8zPDF4NkWwOS=>
OVCAR-5 MlK4R4VtdCCYaXHibYxqfHliQYPzZZk> NVK4SIQ4OC1zMECwJI5O NHXJb2Q4OiCq MmPQbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MnLDNlM6ODBzM{[=
OVCAR-8 MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NV\sbJp5OC1zMECwJI5O MkLJO|IhcA>? MWHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M{K1VFI{QTByMUO2
A1847 MlziR4VtdCCYaXHibYxqfHliQYPzZZk> M{PUfFAuOTByMDDuUS=> M1m2R|czKGh? NUT1eYt[cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NV3vSI1zOjN7MECxN|Y>
SKOV-3 NIHUNIJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVewMVExODBibl2= M33PcVczKGh? NGX6O|RqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MXeyN|kxODF|Nh?=
OVCAR-5 NX3M[I9OSXCxcITvd4l{KEG|c3H5 MYOxNE0yODBibl2= NYT5VFE1OjRxNEivO|IhcA>? MkG4bY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NW\GXmhrOjN7MECxN|Y>
OVCAR-8 NULhbWlJSXCxcITvd4l{KEG|c3H5 NF7NRoYyOC1zMECgcm0> MWeyOE81QC95MjDo M{fLcIlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MXOyN|kxODF|Nh?=
A1847 MlnxRZBweHSxc3nzJGF{e2G7 M1naclExNTFyMDDuUS=> M{PVOlI1NzR6L{eyJIg> MnGwbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= M1HGcFI{QTByMUO2
H2228 NYjyfVBDS2WubDDWbYFjcWyrdImgRZN{[Xl? MUWwMVExODBibl2= M3zt[|czKGh? NHzrO5JKSzVyPUGzJI5O MmLMNlM2OzN{NkW=
H3122 Mm\NR4VtdCCYaXHibYxqfHliQYPzZZk> NVPqem9DOC1zMECwJI5O MUi3NkBp MVjJR|UxRTFyIH7N MWSyN|U{OzJ4NR?=
K008 M1rzPGNmdGxiVnnhZoltcXS7IFHzd4F6 NFi1RZNKSzVyPU[wJI5O M3HuPVI{PDF6NUKz
K028 MmCzR4VtdCCYaXHibYxqfHliQYPzZZk> M3\lNWlEPTB;OESgcm0> M1q4dVI{PDF6NUKz
K029 NHvoVW5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4i4[WlEPTB;NE[gcm0> NGLoR5EzOzRzOEWyNy=>
M23 NUSxdGlbS2WubDDWbYFjcWyrdImgRZN{[Xl? NVXzW2tzUUN3ME2zO{42KG6P MoG0NlM1OTh3MkO=
K033 M2TiZWNmdGxiVnnhZoltcXS7IFHzd4F6 NGjZfW1KSzVyPUe1MlUhdk1? MW[yN|QyQDV{Mx?=
K008 M{\mN2Z2dmO2aX;uJGF{e2G7 NWXjflFNOjVyIH7N MViyOEBp M1TuUolv\HWlZYOgS|Ih[XK{ZYP0 M3zwTFI{PDF6NUKz
K028 Mn\LSpVv[3Srb36gRZN{[Xl? MVyyOVAhdk1? NUPaXHduOjRiaB?= MoDnbY5lfWOnczDHNkBienKnc4S= MlnDNlM1OTh3MkO=
K029 NUDFRlNDTnWwY4Tpc44hSXO|YYm= MYOyOVAhdk1? MUGyOEBp MWPpcoR2[2W|IFexJIFzemW|dB?= MofuNlM1OTh3MkO=
M23 NE[4c5hHfW6ldHnvckBCe3OjeR?= NX;xN254OjVyIH7N MmX6NlQhcA>? NWD1dmV[cW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> NF7xc2wzOzRzOEWyNy=>
K033 MlrSSpVv[3Srb36gRZN{[Xl? MYOyOVAhdk1? MWWyOEBp M2Ppb4lv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= M4HmWVI{PDF6NUKz
K008 MXXBdI9xfG:|aYOgRZN{[Xl? NGG4dowyODBibl2= NYT5emdRPzJiaB?= NYSyeINne2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MXmyN|QyQDV{Mx?=
K028 MkXpRZBweHSxc3nzJGF{e2G7 M2\P[FExOCCwTR?= M4DCfVczKGh? MlXad4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NEi1WGozOzRzOEWyNy=>
K029 NIq1emNCeG:ydH;zbZMhSXO|YYm= NYjxcmZROTByIH7N M4[wNFczKGh? MkLmd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NX;ZZZhVOjN2MUi1NlM>
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SJ-GBM2 M3XjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPyd4xKSzVyPUGyMlkhdk1? M16wUlI{OzB|N{Sx
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CCRF-CEM (2) MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHOOpI2UUN3ME23MlIhdk1? MkL3NlM{ODN5NEG=
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HOP-62 NWXhenpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;3TWM2OD1zMTDuUS=> M4PVO|I{ODF{MkS4
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H1792 NHvme5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJyIH7N MUiyN|AyOjJ2OB?=
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H727 NX\Xb2ZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmWyTWM2OD1{ODDuUS=> NH63UY0zOzBzMkK0PC=>
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H358 NWizOGFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ywU2lEPTB;Mkmgcm0> MYqyN|AyOjJ2OB?=
A549 M1Lafmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDVUWRKSzVyPUSzJI5O NGj2U3ozOzBzMkK0PC=>
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Calu-6 NE\vVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnEPYRKSzVyPU[0JI5O NGrpbHkzOzBzMkK0PC=>
NCI-H1975 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjUOlNVPDhiaB?= NEL0cGdKSzVyPUG2JI5O Mn30NlIyPDR4NkW=
NCI-H1975 Mlu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF63S4g4OiCq NGH6bGRKSzVyPUigcm0> M1TjZlIzOTR2Nk[1

... 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 to the product individually and in order:
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
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).

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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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID