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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Cited by 12 Publications

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 MX;BdI9xfG:|aYOgRZN{[Xl? Ml\SN|AwQDBxMUWwM|I2OCCwTR?= MnHLNlQwPDhxN{KgbC=> NFTjb3RqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> M3TrU|I2QDh{NUWw
MV411 NYq5[29nSXCxcITvd4l{KEG|c3H5 NVKyUY1COzBxOECvNVUxNzJ3MDDuUS=> M3[5PFI1NzR6L{eyJIg> NGTBSW5qdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MUWyOVg5OjV3MB?=
MGC-803 M4r6c2NmdGxiVnnhZoltcXS7IFHzd4F6 M3rrNlAvOS1zMECwJI5O NVPEXlBoPzJiaB?= NGXiVnZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1fVbVI2PTlyOEC1
SGC-7901 NYjnZpRtS2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\KNE4yNTFyMECgcm0> NY\5NlFvPzJiaB?= MnnhbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmDqNlU2QTB6MEW=
MKN-28 Mlm5R4VtdCCYaXHibYxqfHliQYPzZZk> MYewMlEuOTByMDDuUS=> NFjQdlE4OiCq NYP2[FJ3cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWq1ZmtjOjV3OUC4NFU>
MGC-803 M3fyfWZ2dmO2aX;uJGF{e2G7 NUHqbVAxOC5zLUGwNFAhdk1? NHfyS2gzPCCq Mn\jbY5lfWOnczDHNk9OKGOnbHytZ5lkdGViYYLy[ZN1 NFHPfIUzPTV7MEiwOS=>
HCT-116 MkHUSpVv[3Srb36gRZN{[Xl? MWO1NI5O NV;TZYdmOjRiaB?= NXqzUnBGTE2VTx?= MU\pcoR2[2WmIFewM2cyKGG{cnXzeC=> MX:yOVIyODd7NB?=
HT-29 NF\jWFFHfW6ldHnvckBCe3OjeR?= M3u3WVUxdk1? MX:yOEBp M1vVbWROW09? NXXFNI9NcW6mdXPl[EBIOC:JMTDhdpJme3R? MoTtNlUzOTB5OUS=
SCC25 MVHDfZRwgGmlaYT5JGF{e2G7 NIeyd|kyOC93MDDuUS=> MlvMNlQhcA>? M2fXZ4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NHG0[5czPTJyNUSzNC=>
FUDA NXKwUVFQS3m2b4jpZ4l1gSCDc4PhfS=> Mn\pNVAwPTBibl2= NFnpblEzPCCq MnTl[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NHK0cGMzPTJyNUSzNC=>
Detroit562 MXLDfZRwgGmlaYT5JGF{e2G7 MonZNVAwPTBibl2= NXy2SGhpOjRiaB?= NHXxWVRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MorCNlUzODV2M{C=
CAL27 M2PSeGN6fG:6aXPpeJkhSXO|YYm= NUTHVnJ2OTBxNUCgcm0> MoPDNlQhcA>? NE\kO5Rl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NVzCdVg5OjV{MEW0N|A>
DSH1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXNUXdKSzVyPU[gcm0> MYGyOFc5PDh|OR?=
SW-1710 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;YcGlEPTB;NjDuUS=> M17BdlI1Pzh2OEO5
T24 M3fEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nQTmlEPTB;NzDuUS=> MUeyOFc5PDh|OR?=
RT112 M2jv[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPPeY1KSzVyPUmgcm0> M4[4U|I1Pzh2OEO5
639-V NEiwWFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHlTWM2OD1zMDDuUS=> NUL4TXd6OjR5OES4N|k>
SCaBER M1nRN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFyIH7N M1;L[VI1Pzh2OEO5
BFTC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF5IH7N NIHCe4UzPDd6NEizPS=>
J82 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF6IH7N NH;zPXczPDd6NEizPS=>
HT-1376 NVLsV4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\HTWM2OD1{MTDuUS=> M1jmR|I1Pzh2OEO5
647-V MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rB[GlEPTB;Mkegcm0> M2fXflI1Pzh2OEO5
UM-UC3 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLxe29KSzVyPUOzJI5O Mlv4NlQ4QDR6M{m=
LB831-BLC NYm1ZncyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mon2TWM2OD1|NDDuUS=> NHf6OlgzPDd6NEizPS=>
KU-19-19 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;3Xm1[UUN3ME2zOkBvVQ>? MWeyOFc5PDh|OR?=
35612 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSwZplNUUN3ME2zPEBvVQ>? NXHiVoR1OjR5OES4N|k>
5637 MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC3TXVKSzVyPUS0JI5O NFjtNXQzPDd6NEizPS=>
HT-1197 NVqxeIE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e1eGlEPTB;NUOgcm0> Mn;nNlQ4QDR6M{m=
MGH-U3 NFrpWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljQTWM2OD13MzDuUS=> MoX5NlQ4QDR6M{m=
TCCSUP MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DTemlEPTB;MUSyJI5O MlG5NlQ4QDR6M{m=
RT4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEGzXZFKSzVyPUG3N|Mhdk1? MXeyOFc5PDh|OR?=
SW780 M1fObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmCyTWM2OD1|NEWxJI5O MWWyOFc5PDh|OR?=
RKO NYPSfo9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTRibl2= Mn\jNlQ3QDJ5NEe=
LS-411 N NWDjOXc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DJV2lEPTB;NTDuUS=> M2LJ[|I1Pjh{N{S3
SW620 M4Hn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rrN2lEPTB;ODDuUS=> MUiyOFY5Ojd2Nx?=
HCT-15 NHTVb41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfOTWM2OD16IH7N NVrlVFVbOjR4OEK3OFc>
HuTu-80 NXr2XnJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\wc2lEPTB;MUOgcm0> MoDINlQ3QDJ5NEe=
HCT 116 NHPtSWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojTTWM2OD1zNDDuUS=> NF7r[nUzPDZ6Mke0Oy=>
COLO-205 M1\BN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XXSWlEPTB;MUSgcm0> MWWyOFY5Ojd2Nx?=
NCI-H747 NYXWXXB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPqN4g6UUN3ME2xO{BvVQ>? MonmNlQ3QDJ5NEe=
COLO-678 NFHRVFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnL1TWM2OD1{MTDuUS=> M4DTUVI1Pjh{N{S3
LoVo NITmS3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD4TWM2OD1{MjDuUS=> NF;3WZYzPDZ6Mke0Oy=>
LS-1034 NHv0ZZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlqxTWM2OD1|MTDuUS=> M4ntN|I1Pjh{N{S3
SNU-C2B NGXNUIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnznTWM2OD12NTDuUS=> NGTPPVUzPDZ6Mke0Oy=>
LS-123 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13reWlEPTB;N{Ogcm0> NGK4bIMzPDZ6Mke0Oy=>
SK-CO-1 NFfxW|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHFTWM2OD16MTDuUS=> NU\YPVR5OjR4OEK3OFc>
HCC2998 M3fNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF{ODDuUS=> M4\EVFI1Pjh{N{S3
MDA-MB-231 MWPGeY5kfGmxbjDBd5NigQ>? NWfwdZRsOTByIH7N MWqzNEBucW5? MoPTbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NHiwVHUzPDJ2OEK2OS=>
MDA-MB-435 MYnGeY5kfGmxbjDBd5NigQ>? NVjIWGhNOTByIH7N M4nIdVMxKG2rbh?= M4iwcolvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MVyyOFI1QDJ4NR?=
BT-20  Mn;ZSpVv[3Srb36gRZN{[Xl? MknRNVAxNzJ3MDDuUS=> NUnR[FVZOjRiaB?= M3T5T5Jme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? NGj3b4kzPDF5M{W0NS=>
MDA-MB-231 Mme4SpVv[3Srb36gRZN{[Xl? MnzkNVAxKG6P NHi5OWkzPCCq MoLubY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> Mk\xNlQyPzN3NEG=
H82 M1zIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLOdGpqUUN3ME2zNE4zPyCwTR?= MX2yOFE3PjVyNR?=
GLC4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7rTWM2OD1{MD60O{BvVQ>? Mof1NlQyPjZ3MEW=
H69 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{S1eWlEPTB;OEOuN|Yhdk1? M1fvTlI1OTZ4NUC1
H128 M1W5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LCOGlEPTB;NkmuOVUhdk1? MnPoNlQyPjZ3MEW=
H146 M1vyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJ6LkWxJI5O NGXUUFgzPDF4NkWwOS=>
H187 NHLlPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nxVmlEPTB;MkSuPVkhdk1? NWXaOnp1OjRzNk[1NFU>
H526 M3vyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NISwbJVKSzVyPUKxMlY1KG6P MV[yOFE3PjVyNR?=
N592 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO4RVR3UUN3ME2xOE4yOiCwTR?= NYfPS|lxOjRzNk[1NFU>
H620 M1PXSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni3TWM2OD1|Mj62O{BvVQ>? M{P6N|I1OTZ4NUC1
H792 NHjCOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILCbGFKSzVyPUS1MlA4KG6P MYCyOFE3PjVyNR?=
H1173 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XiZWlEPTB;MUKuOlIhdk1? MXeyOFE3PjVyNR?=
AC3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37RdWlEPTB;MkWuPUBvVQ>? MkPvNlQyPjZ3MEW=
H82 MmXTSpVv[3Srb36gRZN{[Xl? NICzPXY{OCCwTR?= Ml\WO|IhcA>? NVu1Wm1ncW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NXLrZ29pOjRzNk[1NFU>
GLC4 MUTGeY5kfGmxbjDBd5NigQ>? NXn5RopYOzBibl2= NFiwWpY4OiCq NHfNVXVqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MonTNlQyPjZ3MEW=
H146  NUfPb3Z7TnWwY4Tpc44hSXO|YYm= NHPVT5Y{OCCwTR?= M4DSblczKGh? NYj5e5N3cW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NIDBPIozPDF4NkWwOS=>
OVCAR-5 MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4jzbFAuOTByMDDuUS=> NWKz[|kxPzJiaB?= NFXwSFJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MX[yN|kxODF|Nh?=
OVCAR-8 NFnQOmRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXSwMVExODBibl2= NFXjVWw4OiCq MYrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3rQO|I{QTByMUO2
A1847 MmO1R4VtdCCYaXHibYxqfHliQYPzZZk> MV[wMVExODBibl2= NIDmTHY4OiCq NI\OTINqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NXu2WYNbOjN7MECxN|Y>
SKOV-3 NWryR3k2S2WubDDWbYFjcWyrdImgRZN{[Xl? Mke3NE0yODByIH7N M{Xib|czKGh? MkXKbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3PtU|I{QTByMUO2
OVCAR-5 M4XWTmFxd3C2b4Ppd{BCe3OjeR?= MkniNVAuOTByIH7N M2DkZ|I1NzR6L{eyJIg> M1LUfolv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MUiyN|kxODF|Nh?=
OVCAR-8 M3vUNGFxd3C2b4Ppd{BCe3OjeR?= NVLEb25iOTBvMUCwJI5O NWe1PJh3OjRxNEivO|IhcA>? Mn7XbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MmjMNlM6ODBzM{[=
A1847 MVzBdI9xfG:|aYOgRZN{[Xl? NWfKTlR{OTBvMUCwJI5O NXT2dY12OjRxNEivO|IhcA>? MWjpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MmrQNlM6ODBzM{[=
H2228 NF3CR4VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NETHUFAxNTFyMECgcm0> Mom2O|IhcA>? NILhb3lKSzVyPUGzJI5O NED4Tm4zOzV|M{K2OS=>
H3122 NGr2PJBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGnF[ZMxNTFyMECgcm0> MVS3NkBp MnrNTWM2OD1zMDDuUS=> MnzBNlM2OzN{NkW=
K008 MljxR4VtdCCYaXHibYxqfHliQYPzZZk> NEe0U3BKSzVyPU[wJI5O NWjaeXR1OjN2MUi1NlM>
K028 M2jKUmNmdGxiVnnhZoltcXS7IFHzd4F6 MXPJR|UxRTh2IH7N M333R|I{PDF6NUKz
K029 NXvWbYZRS2WubDDWbYFjcWyrdImgRZN{[Xl? NUDwfWhJUUN3ME20OkBvVQ>? MlPBNlM1OTh3MkO=
M23 NVnYWY9US2WubDDWbYFjcWyrdImgRZN{[Xl? MlHRTWM2OD1|Nz61JI5O NETGe2EzOzRzOEWyNy=>
K033 M3\uOGNmdGxiVnnhZoltcXS7IFHzd4F6 MUjJR|UxRTd3LkWgcm0> MnXnNlM1OTh3MkO=
K008 M3HHb2Z2dmO2aX;uJGF{e2G7 M331fVI2OCCwTR?= M3zJ[FI1KGh? NVvoeotXcW6mdXPld{BIOiCjcoLld5Q> Mlm5NlM1OTh3MkO=
K028 M2\m[2Z2dmO2aX;uJGF{e2G7 MnTGNlUxKG6P MoXKNlQhcA>? NE\FNJdqdmS3Y3XzJGczKGG{cnXzeC=> NFH2e|YzOzRzOEWyNy=>
K029 MYXGeY5kfGmxbjDBd5NigQ>? NYX0TIZFOjVyIH7N M3HZTVI1KGh? MmXLbY5lfWOnczDHNUBienKnc4S= NUC5NId7OjN2MUi1NlM>
M23 MXHGeY5kfGmxbjDBd5NigQ>? MY[yOVAhdk1? NGnQNGYzPCCq NX;EUYxucW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> MXGyN|QyQDV{Mx?=
K033 NXHTZ2xwTnWwY4Tpc44hSXO|YYm= M3;NPFI2OCCwTR?= M3XBXFI1KGh? NHjafpZqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36= MlvuNlM1OTh3MkO=
K008 NH\SU|lCeG:ydH;zbZMhSXO|YYm= MoXNNVAxKG6P NIDHRYE4OiCq M2j5OpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MWmyN|QyQDV{Mx?=
K028 NV7oNo5kSXCxcITvd4l{KEG|c3H5 NFXvb|IyODBibl2= NWTtUHh4PzJiaB?= M4\Oc5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NVLYfXBsOjN2MUi1NlM>
K029 NVnrNWp[SXCxcITvd4l{KEG|c3H5 M3LL[VExOCCwTR?= NWLjU2hyPzJiaB?= NH;kWmF{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M2TablI{PDF6NUKz
M23 MlmzRZBweHSxc3nzJGF{e2G7 NEfxZmoyODBibl2= NXnJTW1rPzJiaB?= M3PV[pNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MX[yN|QyQDV{Mx?=
K033 M4TPWGFxd3C2b4Ppd{BCe3OjeR?= NELMOpcyODBibl2= M2K2OVczKGh? MY\zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M1:wRlI{PDF6NUKz
RD MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDDb3czUUN3ME24JI5O M2fUTlI{OzB|N{Sx
Rh41 NXX0dJpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPjTWM2OD1zMD60JI5O NYXkfXI6OjN|MEO3OFE>
Rh18 NEG2PHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXEe2RKSzVyPU[uNkBvVQ>? M3fWc|I{OzB|N{Sx
Rh30 M4rwPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTVwNjDuUS=> Mnu1NlM{ODN5NEG=
BT-12 NYnuNG5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\2[Y1SUUN3ME2xOE4{KG6P NULUVGdsOjN|MEO3OFE>
CHLA-266 NYXLTVZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[2TWM2OD1{Nz6xJI5O MorNNlM{ODN5NEG=
TC-71 NYPXUVZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTRwNTDuUS=> NGLJdJQzOzNyM{e0NS=>
CHLA-9 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHiwRmZKSzVyPUSuOkBvVQ>? MV2yN|MxOzd2MR?=
CHLA-10 NXPyeppxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDuTWM2OD13Lkegcm0> MVGyN|MxOzd2MR?=
CHLA-258 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnZW2V6UUN3ME22MlQhdk1? MYmyN|MxOzd2MR?=
SJ-GBM2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvNTWM2OD1zMj65JI5O Ml3DNlM{ODN5NEG=
NB-1643 NV\JVGppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nkVWlEPTB;Nz60JI5O M1jGV|I{OzB|N{Sx
NB-EBc1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID2TIdKSzVyPUG2Mlghdk1? NVvXSnRbOjN|MEO3OFE>
CHLA-90 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ{LkOgcm0> NV7zNlU2OjN|MEO3OFE>
CHLA-136 M1jFeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnyTWM2OD1{Mz6yJI5O NVHkd|F7OjN|MEO3OFE>
NALM-6 MkC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HLRmlEPTB;MUGuO{BvVQ>? NUK2Sm5QOjN|MEO3OFE>
COG-LL-317 M3P0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0TWM2OD12LkSgcm0> MnPNNlM{ODN5NEG=
RS4;11 NUnlcGc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLkT2V1UUN3ME2xN{42KG6P M1\0OVI{OzB|N{Sx
MOLT-4 NWXn[WhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\IUmlEPTB;MUCuOkBvVQ>? M2jtSFI{OzB|N{Sx
CCRF-CEM (1) M1f0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;FSFhKSzVyPUGyMlUhdk1? MWGyN|MxOzd2MR?=
CCRF-CEM (2) M33xZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL0TWM2OD15LkKgcm0> NETLR3EzOzNyM{e0NS=>
Kasumi-1 NGn5[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfZ[ZR7UUN3ME21Mlghdk1? M3\UcVI{OzB|N{Sx
Karpas-299 M2rTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTlwNjDuUS=> Mn20NlM{ODN5NEG=
Ramos-RA1 NHzCfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH2TWM2OD15LkSgcm0> M3PZRVI{OzB|N{Sx
LNCaP NVXsSJFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHPW|ZKSzVyPUigcm0> NV3mWpJYOjNzNUKwNFQ>
VCaP NUnkeWxST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rRW2lEPTB;NzDuUS=> MmnhNlMyPTJyMES=
H1355 NGLhcWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXUWWxSUUN3ME21JI5O NHG1O2wzOzBzMkK0PC=>
H157 M1XOfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3WyNGlEPTB;NzDuUS=> MYiyN|AyOjJ2OB?=
H460 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkn6TWM2OD16IH7N NFrKTpQzOzBzMkK0PC=>
IA-LM NE\wWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFyIH7N M4nLUlI{ODF{MkS4
HOP-62 NVrHXIxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFzIH7N MV[yN|AyOjJ2OB?=
H23 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nLOGlEPTB;MUGgcm0> MnT2NlMxOTJ{NEi=
H2030 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF{IH7N M{TPWVI{ODF{MkS4
H441 M{Phc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jzZ2lEPTB;MUSgcm0> MVOyN|AyOjJ2OB?=
H2212 MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\CTmlEPTB;MUegcm0> NHH0SnozOzBzMkK0PC=>
SK-LU-1 NXXKcHNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\DTWM2OD1zODDuUS=> M{PpeFI{ODF{MkS4
H2009 Mmm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF7IH7N MnS4NlMxOTJ{NEi=
H1792 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqxTWM2OD1{MDDuUS=> NWLHN29XOjNyMUKyOFg>
COR-L23 NF7IeHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ{IH7N NYfFbohoOjNyMUKyOFg>
H727 M17oU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELvS|NKSzVyPUK4JI5O Mkf5NlMxOTJ{NEi=
H1734 M1rkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXFb3hKSzVyPUK4JI5O NH:5ZpgzOzBzMkK0PC=>
H358 M4XOS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPQe41rUUN3ME2yPUBvVQ>? M1noRlI{ODF{MkS4
A549 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Pyb2lEPTB;NEOgcm0> NHX2cWkzOzBzMkK0PC=>
H2122 NUmwZox6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\pfWlEPTB;NUOgcm0> MXmyN|AyOjJ2OB?=
Calu-1 NV3KR2hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vQb2lEPTB;NUigcm0> MkPoNlMxOTJ{NEi=
Calu-6 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvvRXhmUUN3ME22OEBvVQ>? M3H5ZlI{ODF{MkS4
NCI-H1975 NX;rXlRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnQUWFFPDhiaB?= NFPDR5JKSzVyPUG2JI5O MWOyNlE1PDZ4NR?=
NCI-H1975 Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe3e5BOPzJiaB?= NXjyfZl6UUN3ME24JI5O MVuyNlE1PDZ4NR?=

... 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]
+ 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(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

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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/

selleck catalog

HSP (e.g. HSP90) Signaling Pathway Map

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.

Related HSP (e.g. HSP90) Products

  • PU-H71 New

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

  • KNK437 New

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

  • VER155008 New

    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.

  • Tanespimycin (17-AAG)

    Tanespimycin (17-AAG) 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.

  • Alvespimycin (17-DMAG) HCl

    Alvespimycin (17-DMAG) 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)

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  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID