Ganetespib (STA-9090)

For research use only.

Catalog No.S1159

34 publications

Ganetespib (STA-9090) Chemical Structure

CAS No. 888216-25-9

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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Selleck's Ganetespib (STA-9090) has been cited by 34 publications

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Choose Selective HSP (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 NHroXFFCeG:ydH;zbZMhSXO|YYm= NHzHdGE{OC96MD:xOVAwOjVyIH7N NVzONFFPOjRxNEivO|IhcA>? MkDBbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NYr2[VVvOjV6OEK1OVA>
MV411 NXXZbZRKSXCxcITvd4l{KEG|c3H5 NE\GW3Q{OC96MD:xOVAwOjVyIH7N MlWzNlQwPDhxN{KgbC=> M3f4XIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NIm1bZkzPTh6MkW1NC=>
MGC-803 M{[4dmNmdGxiVnnhZoltcXS7IFHzd4F6 M2P0WFAvOS1zMECwJI5O MYK3NkBp MV\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUCyOVU6ODhyNR?=
SGC-7901 M4TzOWNmdGxiVnnhZoltcXS7IFHzd4F6 MV2wMlEuOTByMDDuUS=> MlPqO|IhcA>? MXLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3T6RlI2PTlyOEC1
MKN-28 NHew[pFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4LBWVAvOS1zMECwJI5O MnLsO|IhcA>? MV7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NGmzSmEzPTV7MEiwOS=>
MGC-803 NXHIbYpkTnWwY4Tpc44hSXO|YYm= MYWwMlEuOTByMDDuUS=> MV:yOEBp M33S[Ylv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? NVTVZ|d[OjV3OUC4NFU>
HCT-116 NE\xd3FHfW6ldHnvckBCe3OjeR?= MoPBOVBvVQ>? MlnnNlQhcA>? NEjwZWlFVVOR NIfYSJlqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MVeyOVIyODd7NB?=
HT-29 NFLsXVRHfW6ldHnvckBCe3OjeR?= Ml;ROVBvVQ>? NIPLT5gzPCCq NULoPHkyTE2VTx?= NVHQUHBIcW6mdXPl[EBIOC:JMTDhdpJme3R? M4fMPFI2OjFyN{m0
SCC25 MmG3R5l1d3irY3n0fUBCe3OjeR?= NXzie4tNOTBxNUCgcm0> NHPDdZAzPCCq NVfjRZMx\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NVHDdXE1OjV{MEW0N|A>
FUDA NIX0cmhEgXSxeHnjbZR6KEG|c3H5 M4DzbFExNzVyIH7N Mn;0NlQhcA>? M2XQUIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M3TDSFI2OjB3NEOw
Detroit562 NIHSdFlEgXSxeHnjbZR6KEG|c3H5 MYGxNE82OCCwTR?= M3PlbFI1KGh? M1z4NIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MYKyOVIxPTR|MB?=
CAL27 MofhR5l1d3irY3n0fUBCe3OjeR?= NYfoVWo6OTBxNUCgcm0> MXyyOEBp NGXUXmFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NEDDTZczPTJyNUSzNC=>
DSH1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2KybmlEPTB;NjDuUS=> NWPEWoNpOjR5OES4N|k>
SW-1710 M{O2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTZibl2= NV;DfJp3OjR5OES4N|k>
T24 M2nIcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfHbodKSzVyPUegcm0> NIf2bHczPDd6NEizPS=>
RT112 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLNTWM2OD17IH7N NYrQdW1GOjR5OES4N|k>
639-V M1;DVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYO4[npFUUN3ME2xNEBvVQ>? NGDLVoQzPDd6NEizPS=>
SCaBER NWLjZ5U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoW4TWM2OD1zMDDuUS=> MXOyOFc5PDh|OR?=
BFTC MmW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37zS2lEPTB;MUegcm0> MUeyOFc5PDh|OR?=
J82 M{fHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXe3Uld7UUN3ME2xPEBvVQ>? M4nSeVI1Pzh2OEO5
HT-1376 NVfXdHA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH3U3czUUN3ME2yNUBvVQ>? MVWyOFc5PDh|OR?=
647-V MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn6e2l[UUN3ME2yO{BvVQ>? MUOyOFc5PDh|OR?=
UM-UC3 M3LaN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnsUpBKSzVyPUOzJI5O MUmyOFc5PDh|OR?=
LB831-BLC NX61e5RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELwN2JKSzVyPUO0JI5O NFzpVI4zPDd6NEizPS=>
KU-19-19 M1u5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPBTWM2OD1|NjDuUS=> MUCyOFc5PDh|OR?=
35612 NXTmTI05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXhZnBWUUN3ME2zPEBvVQ>? NGnLNZQzPDd6NEizPS=>
5637 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfxV4tIUUN3ME20OEBvVQ>? NUXRXGh[OjR5OES4N|k>
HT-1197 NEn5d2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjrTHpKSzVyPUWzJI5O M33UeVI1Pzh2OEO5
MGH-U3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjDV4FKSzVyPUWzJI5O NXPvZVZXOjR5OES4N|k>
TCCSUP MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF2MjDuUS=> NVrkc4ZKOjR5OES4N|k>
RT4 NYjr[lQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF5M{Ogcm0> NHXDPWszPDd6NEizPS=>
SW780 M1XYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DtXWlEPTB;M{S1NUBvVQ>? Mmq0NlQ4QDR6M{m=
RKO NYXWZZA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLkSYhKSzVyPUSgcm0> NHHwOIIzPDZ6Mke0Oy=>
LS-411 N NXzHWVN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OxeGlEPTB;NTDuUS=> NVH5[XlSOjR4OEK3OFc>
SW620 M4S0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXjOpVzUUN3ME24JI5O NWrvUJI2OjR4OEK3OFc>
HCT-15 NIPPXZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3y0V2lEPTB;ODDuUS=> M365PFI1Pjh{N{S3
HuTu-80 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\uUoRqUUN3ME2xN{BvVQ>? MkTLNlQ3QDJ5NEe=
HCT 116 M{nGemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrkOWdKSzVyPUG0JI5O NV3KWWg4OjR4OEK3OFc>
COLO-205 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXITWM2OD1zNDDuUS=> NIq1fIkzPDZ6Mke0Oy=>
NCI-H747 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS1Opg1UUN3ME2xO{BvVQ>? NXjy[|JlOjR4OEK3OFc>
COLO-678 M{SzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LVcmlEPTB;MkGgcm0> MnmxNlQ3QDJ5NEe=
LoVo MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon4TWM2OD1{MjDuUS=> MoPVNlQ3QDJ5NEe=
LS-1034 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrvO2JwUUN3ME2zNUBvVQ>? MX[yOFY5Ojd2Nx?=
SNU-C2B M4XKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XZVGlEPTB;NEWgcm0> NH;1bYQzPDZ6Mke0Oy=>
LS-123 NIPYWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf2TFVTUUN3ME23N{BvVQ>? NYPEd41ROjR4OEK3OFc>
SK-CO-1 M1TEO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRThzIH7N MlPrNlQ3QDJ5NEe=
HCC2998 M{LEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17vW2lEPTB;MUK4JI5O NHLtcXMzPDZ6Mke0Oy=>
MDA-MB-231 NIC0d4VHfW6ldHnvckBCe3OjeR?= MX[xNFAhdk1? NEfjXZU{OCCvaX6= MlG5bY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? M2[3VFI1OjR6Mk[1
MDA-MB-435 NVvmUFdHTnWwY4Tpc44hSXO|YYm= MW[xNFAhdk1? NFHUNYo{OCCvaX6= M4HBV4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NUHOTldIOjR{NEiyOlU>
BT-20  M1jtTmZ2dmO2aX;uJGF{e2G7 NFnlT2syODBxMkWwJI5O NYewR5R{OjRiaB?= M4rXeJJme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? NFuwN2kzPDF5M{W0NS=>
MDA-MB-231 MWjGeY5kfGmxbjDBd5NigQ>? MnK0NVAxKG6P NWTtWFV{OjRiaB?= Mo\TbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> Ml:zNlQyPzN3NEG=
H82 NGrpcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjxTWM2OD1|MD6yO{BvVQ>? MkP4NlQyPjZ3MEW=
GLC4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXGRopKSzVyPUKwMlQ4KG6P NYCwOotIOjRzNk[1NFU>
H69 M3HVcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTEeYNOUUN3ME24N{4{PiCwTR?= Ml\iNlQyPjZ3MEW=
H128 NW\4OmRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnIcVNKSzVyPU[5MlU2KG6P NWfXOoxyOjRzNk[1NFU>
H146 M3LJU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnXXnJjUUN3ME2yPE42OSCwTR?= NUX5SVhxOjRzNk[1NFU>
H187 M1HD[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTJ2Lkm5JI5O Mk\ONlQyPjZ3MEW=
H526 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJzLk[0JI5O MnnPNlQyPjZ3MEW=
N592 MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLxVnBIUUN3ME2xOE4yOiCwTR?= NGDCZlMzPDF4NkWwOS=>
H620 NY[zNXFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjoWHE{UUN3ME2zNk43PyCwTR?= M2jXNlI1OTZ4NUC1
H792 NWr4OGdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j6SWlEPTB;NEWuNFchdk1? M{TVcVI1OTZ4NUC1
H1173 NITXOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTF{Lk[yJI5O MmXmNlQyPjZ3MEW=
AC3 NVzSfFIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTHOJB{UUN3ME2yOU46KG6P MWSyOFE3PjVyNR?=
H82 MUXGeY5kfGmxbjDBd5NigQ>? M{PsZVMxKG6P MlP6O|IhcA>? Ml:zbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MXWyOFE3PjVyNR?=
GLC4 MWPGeY5kfGmxbjDBd5NigQ>? MnjjN|Ahdk1? NUDGblJkPzJiaB?= NWGyZW5ucW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M2LuW|I1OTZ4NUC1
H146  Ml\uSpVv[3Srb36gRZN{[Xl? Mly3N|Ahdk1? MXK3NkBp M{HIT4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MUeyOFE3PjVyNR?=
OVCAR-5 MmnhR4VtdCCYaXHibYxqfHliQYPzZZk> NFjIdpExNTFyMECgcm0> NXLHWXJZPzJiaB?= MlzMbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MlHSNlM6ODBzM{[=
OVCAR-8 M{OwSWNmdGxiVnnhZoltcXS7IFHzd4F6 NEm3[3UxNTFyMECgcm0> MVu3NkBp NEfNN4xqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1rGNFI{QTByMUO2
A1847 NHzBTpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlL5NE0yODByIH7N MYG3NkBp MnexbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MUCyN|kxODF|Nh?=
SKOV-3 NEHVellE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYjIeG1NOC1zMECwJI5O MnPjO|IhcA>? MVjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M{fLR|I{QTByMUO2
OVCAR-5 NFu1e2pCeG:ydH;zbZMhSXO|YYm= MUixNE0yODBibl2= NIHHSZYzPC92OD:3NkBp NHnqZohqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M1nyNVI{QTByMUO2
OVCAR-8 MkXlRZBweHSxc3nzJGF{e2G7 MYCxNE0yODBibl2= NETyTGYzPC92OD:3NkBp M3\zc4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= Mnn2NlM6ODBzM{[=
A1847 MonGRZBweHSxc3nzJGF{e2G7 M1K4[FExNTFyMDDuUS=> NYWwbZlbOjRxNEivO|IhcA>? M4WxVolv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= NXnhZVB1OjN7MECxN|Y>
H2228 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYL1dHR[OC1zMECwJI5O MX:3NkBp M{\vRWlEPTB;MUOgcm0> NXjxOlJ4OjN3M{OyOlU>
H3122 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NInHPXYxNTFyMECgcm0> MX23NkBp MYPJR|UxRTFyIH7N M1zvflI{PTN|Mk[1
K008 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEn5WplKSzVyPU[wJI5O NYnkc3M4OjN2MUi1NlM>
K028 MWjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXTFVpVFUUN3ME24OEBvVQ>? M3znPVI{PDF6NUKz
K029 MnzRR4VtdCCYaXHibYxqfHliQYPzZZk> MkfsTWM2OD12NjDuUS=> MXGyN|QyQDV{Mx?=
M23 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUnJR|UxRTN5LkWgcm0> NFW1eHczOzRzOEWyNy=>
K033 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{PDbWlEPTB;N{WuOUBvVQ>? M1G2bVI{PDF6NUKz
K008 MYrGeY5kfGmxbjDBd5NigQ>? NYDKdINkOjVyIH7N M1K4XlI1KGh? M{\RWolv\HWlZYOgS|Ih[XK{ZYP0 MWeyN|QyQDV{Mx?=
K028 MV;GeY5kfGmxbjDBd5NigQ>? NIjYd|EzPTBibl2= MmPNNlQhcA>? NGjCS|VqdmS3Y3XzJGczKGG{cnXzeC=> NG\3[5QzOzRzOEWyNy=>
K029 M4jsdmZ2dmO2aX;uJGF{e2G7 NEGyRWszPTBibl2= MXKyOEBp NHnYXGxqdmS3Y3XzJGcyKGG{cnXzeC=> NXfjOog6OjN2MUi1NlM>
M23 MoTWSpVv[3Srb36gRZN{[Xl? M{[zc|I2OCCwTR?= MnXRNlQhcA>? Mlr2bY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= MXyyN|QyQDV{Mx?=
K033 NUnaenplTnWwY4Tpc44hSXO|YYm= NV34NldlOjVyIH7N M2G0RVI1KGh? Moq0bY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NVe4VGRuOjN2MUi1NlM>
K008 NF;xeZRCeG:ydH;zbZMhSXO|YYm= NWn0WVBMOTByIH7N NH3DNVM4OiCq M{HL[JNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MnT5NlM1OTh3MkO=
K028 NIniU5RCeG:ydH;zbZMhSXO|YYm= M{XzelExOCCwTR?= NYf6TG56PzJiaB?= M3XEb5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M4rhXVI{PDF6NUKz
K029 NF;2XHhCeG:ydH;zbZMhSXO|YYm= M2DBOFExOCCwTR?= MVK3NkBp NXPYN2E2e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MmPiNlM1OTh3MkO=
M23 NV34PXF2SXCxcITvd4l{KEG|c3H5 MUGxNFAhdk1? NYXPdYhvPzJiaB?= NFT1SHN{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NIn1SmIzOzRzOEWyNy=>
K033 NIe1TVBCeG:ydH;zbZMhSXO|YYm= NIXmZ28yODBibl2= NXrESZRYPzJiaB?= MlTld4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NYP0WHZ1OjN2MUi1NlM>
RD Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRThibl2= MoPTNlM{ODN5NEG=
Rh41 M2nmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTFyLkSgcm0> M2fQTlI{OzB|N{Sx
Rh18 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;nRmlEPTB;Nj6yJI5O M3m4bVI{OzB|N{Sx
Rh30 NWHYWVhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlviTWM2OD13Lk[gcm0> Ml30NlM{ODN5NEG=
BT-12 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHCeZZ4UUN3ME2xOE4{KG6P NX74N29EOjN|MEO3OFE>
CHLA-266 NWrIWXJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP4TWM2OD1{Nz6xJI5O NWLSNnQ6OjN|MEO3OFE>
TC-71 M4HFZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\IdW5KSzVyPUSuOUBvVQ>? NX3teYJGOjN|MEO3OFE>
CHLA-9 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XJTGlEPTB;ND62JI5O NEDSPWQzOzNyM{e0NS=>
CHLA-10 NVPCdJNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTVwNzDuUS=> MWqyN|MxOzd2MR?=
CHLA-258 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvoTWM2OD14LkSgcm0> NWjENVcxOjN|MEO3OFE>
SJ-GBM2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF{Lkmgcm0> M2fiOlI{OzB|N{Sx
NB-1643 M1HHW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vDdmlEPTB;Nz60JI5O MmK1NlM{ODN5NEG=
NB-EBc1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn0TWM2OD1zNj64JI5O M4XORVI{OzB|N{Sx
CHLA-90 M4LP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ{LkOgcm0> M{nld|I{OzB|N{Sx
CHLA-136 M3;RbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX2XoxKSzVyPUKzMlIhdk1? MlHWNlM{ODN5NEG=
NALM-6 NEjtflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFzLkegcm0> NIXZ[pgzOzNyM{e0NS=>
COG-LL-317 NWj2NoNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTRwNDDuUS=> MWmyN|MxOzd2MR?=
RS4;11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITw[nlKSzVyPUGzMlUhdk1? NGfrPXQzOzNyM{e0NS=>
MOLT-4 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnmOXRKSzVyPUGwMlYhdk1? MWqyN|MxOzd2MR?=
CCRF-CEM (1) M1HXSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PVWmlEPTB;MUKuOUBvVQ>? MXWyN|MxOzd2MR?=
CCRF-CEM (2) Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUP5doliUUN3ME23MlIhdk1? Mn;PNlM{ODN5NEG=
Kasumi-1 Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLESolKSzVyPUWuPEBvVQ>? MYSyN|MxOzd2MR?=
Karpas-299 NGnGWm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDFV4RKSzVyPUmuOkBvVQ>? M4S5U|I{OzB|N{Sx
Ramos-RA1 MlzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTdwNDDuUS=> M2jENlI{OzB|N{Sx
LNCaP NXXORmZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi0U3RtUUN3ME24JI5O MWGyN|E2OjByNB?=
VCaP Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXFflZ7UUN3ME23JI5O MWqyN|E2OjByNB?=
H1355 M3TEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPo[5ZNUUN3ME21JI5O NXS1Z2RmOjNyMUKyOFg>
H157 NGiwSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K3OWlEPTB;NzDuUS=> MlzRNlMxOTJ{NEi=
H460 NEHqVGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDMTWM2OD16IH7N M4TNNVI{ODF{MkS4
IA-LM NHOyNVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\hTWM2OD1zMDDuUS=> NVXvW5J7OjNyMUKyOFg>
HOP-62 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fUcWlEPTB;MUGgcm0> NV3xdIdjOjNyMUKyOFg>
H23 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;5R5hOUUN3ME2xNUBvVQ>? M3fyZ|I{ODF{MkS4
H2030 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3rWJE2UUN3ME2xNkBvVQ>? NFr5RVgzOzBzMkK0PC=>
H441 MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHCXodKSzVyPUG0JI5O M4n1[FI{ODF{MkS4
H2212 NHnLVmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF5IH7N NWPU[WVWOjNyMUKyOFg>
SK-LU-1 MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETtfFZKSzVyPUG4JI5O NUDM[oloOjNyMUKyOFg>
H2009 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\mbWFJUUN3ME2xPUBvVQ>? NGTwfHczOzBzMkK0PC=>
H1792 M{HyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHK3XplKSzVyPUKwJI5O NFLtSVgzOzBzMkK0PC=>
COR-L23 NEGwZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3ZTWM2OD1{MjDuUS=> Ml\mNlMxOTJ{NEi=
H727 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:4UmlEPTB;Mkigcm0> NI[3bHczOzBzMkK0PC=>
H1734 M3LsW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ6IH7N MlfUNlMxOTJ{NEi=
H358 M3u4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ7IH7N NXzHcGRPOjNyMUKyOFg>
A549 M4H3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHmT4ZKSzVyPUSzJI5O MmnNNlMxOTJ{NEi=
H2122 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTV|IH7N MXKyN|AyOjJ2OB?=
Calu-1 NXuyOnhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTXbXdlUUN3ME21PEBvVQ>? MojZNlMxOTJ{NEi=
Calu-6 NFrUTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TTT2lEPTB;NkSgcm0> MnzoNlMxOTJ{NEi=
NCI-H1975 M3;WSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1GwRlQ5KGh? NHroR|ZKSzVyPUG2JI5O NX;tRXBoOjJzNES2OlU>
NCI-H1975 NF7F[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XwSFczKGh? M33xVmlEPTB;ODDuUS=> NXrqToh4OjJzNES2OlU>

... 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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female severe combined immune-deficient (SCID) mice
  • 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
Smiles CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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 (mg) = Concentration (mM) × Volume (mL) × 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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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 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.

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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 (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID