Ganetespib (STA-9090)

For research use only. Not for use in humans.

Catalog No.S1159

23 publications

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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Selleck's Ganetespib (STA-9090) has been cited by 23 publications

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 MlTiRZBweHSxc3nzJGF{e2G7 NYT0Zpc6OzBxOECvNVUxNzJ3MDDuUS=> M2nQXFI1NzR6L{eyJIg> NVu1PHRocW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MoXSNlU5QDJ3NUC=
MV411 NHS4U5RCeG:ydH;zbZMhSXO|YYm= NHfBNJk{OC96MD:xOVAwOjVyIH7N MkjKNlQwPDhxN{KgbC=> NIK1NIZqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NHy5SW4zPTh6MkW1NC=>
MGC-803 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnSzNE4yNTFyMECgcm0> MmjaO|IhcA>? NXXyXIpIcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWGyOVU6ODhyNR?=
SGC-7901 M{HaXmNmdGxiVnnhZoltcXS7IFHzd4F6 NXrUPFRwOC5zLUGwNFAhdk1? NELOT|Q4OiCq M1fLZ4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MUeyOVU6ODhyNR?=
MKN-28 MkLIR4VtdCCYaXHibYxqfHliQYPzZZk> NXXUZZBEOC5zLUGwNFAhdk1? M{LNNlczKGh? Mn3wbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NIHlUZczPTV7MEiwOS=>
MGC-803 NVG2S3RjTnWwY4Tpc44hSXO|YYm= NHPzcmwxNjFvMUCwNEBvVQ>? NGrQUFQzPCCq NXXIWIZDcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NXPRXYJWOjV3OUC4NFU>
HCT-116 MnTJSpVv[3Srb36gRZN{[Xl? NVW2PXF6PTCwTR?= NUnsU|hXOjRiaB?= NVXl[ZV1TE2VTx?= MkOxbY5lfWOnZDDHNE9IOSCjcoLld5Q> MknxNlUzOTB5OUS=
HT-29 MVvGeY5kfGmxbjDBd5NigQ>? M2XjdFUxdk1? MWCyOEBp NYT1U2hqTE2VTx?= NWfubVNJcW6mdXPl[EBIOC:JMTDhdpJme3R? MoXENlUzOTB5OUS=
SCC25 MWLDfZRwgGmlaYT5JGF{e2G7 M{fqUFExNzVyIH7N MXeyOEBp M{D0U4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NX3RWWt6OjV{MEW0N|A>
FUDA NWrId3RwS3m2b4jpZ4l1gSCDc4PhfS=> NGDybWEyOC93MDDuUS=> MlnJNlQhcA>? M1zrRYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NVnJOGhrOjV{MEW0N|A>
Detroit562 MV\DfZRwgGmlaYT5JGF{e2G7 NYTQbZpOOTBxNUCgcm0> NEHLSmMzPCCq NIrq[Yxl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MlHFNlUzODV2M{C=
CAL27 MkHqR5l1d3irY3n0fUBCe3OjeR?= M4jHSFExNzVyIH7N NF2wO20zPCCq NVyw[Jg5\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NH3nTmYzPTJyNUSzNC=>
DSH1 NEWydHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPlTWM2OD14IH7N MojlNlQ4QDR6M{m=
SW-1710 NFr4PJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfrTWM2OD14IH7N MlfrNlQ4QDR6M{m=
T24 M1rVVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nkfGlEPTB;NzDuUS=> MXiyOFc5PDh|OR?=
RT112 Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WxT2lEPTB;OTDuUS=> M3zhflI1Pzh2OEO5
639-V MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfmTWM2OD1zMDDuUS=> NH3kcZEzPDd6NEizPS=>
SCaBER NEjIZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXKTWM2OD1zMDDuUS=> NUjDNYpwOjR5OES4N|k>
BFTC NE\EN|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTF5IH7N M1jxNVI1Pzh2OEO5
J82 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPSUm14UUN3ME2xPEBvVQ>? NE\tNW4zPDd6NEizPS=>
HT-1376 M4Pj[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fVfWlEPTB;MkGgcm0> NHHHRmIzPDd6NEizPS=>
647-V MmG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XENGlEPTB;Mkegcm0> Mlj2NlQ4QDR6M{m=
UM-UC3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPh[GhsUUN3ME2zN{BvVQ>? NY\hPYZUOjR5OES4N|k>
LB831-BLC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\JTWlEPTB;M{Sgcm0> NHLOOnEzPDd6NEizPS=>
KU-19-19 NEDUTZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTN4IH7N MX6yOFc5PDh|OR?=
35612 NVTUdWZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnlSWZYUUN3ME2zPEBvVQ>? NUiyU5N3OjR5OES4N|k>
5637 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR2IH7N M1jsNFI1Pzh2OEO5
HT-1197 NHjvbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTV|IH7N MkOzNlQ4QDR6M{m=
MGH-U3 M3rI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHqXpN3UUN3ME21N{BvVQ>? M{O3UVI1Pzh2OEO5
TCCSUP NHPpfYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonTTWM2OD1zNEKgcm0> NHz1bJMzPDd6NEizPS=>
RT4 NXfCdpZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4excmlEPTB;MUezN{BvVQ>? MlvsNlQ4QDR6M{m=
SW780 NH7FcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGzco1jUUN3ME2zOFUyKG6P Mo\lNlQ4QDR6M{m=
RKO MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS3eJpKSzVyPUSgcm0> M4rzV|I1Pjh{N{S3
LS-411 N NYTYToRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn4fIhwUUN3ME21JI5O NYexVINWOjR4OEK3OFc>
SW620 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXQfXF7UUN3ME24JI5O NFPzOW8zPDZ6Mke0Oy=>
HCT-15 NXvxb4xYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRThibl2= M3jLS|I1Pjh{N{S3
HuTu-80 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULuUnhKUUN3ME2xN{BvVQ>? M2LKT|I1Pjh{N{S3
HCT 116 MoTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLFb21QUUN3ME2xOEBvVQ>? MlPINlQ3QDJ5NEe=
COLO-205 M3nxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILxenZKSzVyPUG0JI5O MV[yOFY5Ojd2Nx?=
NCI-H747 Ml\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rhVmlEPTB;MUegcm0> NF\oWXozPDZ6Mke0Oy=>
COLO-678 M{HXRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPVToVZUUN3ME2yNUBvVQ>? Ml73NlQ3QDJ5NEe=
LoVo MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHHTWM2OD1{MjDuUS=> M1X4[|I1Pjh{N{S3
LS-1034 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNzIH7N MVuyOFY5Ojd2Nx?=
SNU-C2B M4LPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTR3IH7N MlfvNlQ3QDJ5NEe=
LS-123 NX\3cpBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\5bWlEPTB;N{Ogcm0> NFL4ZlQzPDZ6Mke0Oy=>
SK-CO-1 NGXpXVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DXUmlEPTB;OEGgcm0> M2DXZVI1Pjh{N{S3
HCC2998 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF{ODDuUS=> MV:yOFY5Ojd2Nx?=
MDA-MB-231 M33jdGZ2dmO2aX;uJGF{e2G7 MkPCNVAxKG6P Ml7tN|AhdWmw Mk[wbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MkXFNlQzPDh{NkW=
MDA-MB-435 MmDWSpVv[3Srb36gRZN{[Xl? M{DOeFExOCCwTR?= M{LxT|MxKG2rbh?= NW\HO2lycW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NWXaeFYyOjR{NEiyOlU>
BT-20  NXXKe3V7TnWwY4Tpc44hSXO|YYm= Mni4NVAxNzJ3MDDuUS=> MmDkNlQhcA>? NVG5UoRJemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI NXv2cmpIOjRzN{O1OFE>
MDA-MB-231 NFryNVdHfW6ldHnvckBCe3OjeR?= NGDvSmgyODBibl2= M373SlI1KGh? M1TMdolvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> MW[yOFE4OzV2MR?=
H82 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfMfWpQUUN3ME2zNE4zPyCwTR?= NXfMepJqOjRzNk[1NFU>
GLC4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTYTWM2OD1{MD60O{BvVQ>? NFrPbXAzPDF4NkWwOS=>
H69 NV\aTW13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLqWVFKSzVyPUizMlM3KG6P NWWxWlc6OjRzNk[1NFU>
H128 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknXTWM2OD14OT61OUBvVQ>? MX2yOFE3PjVyNR?=
H146 NXHjflhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJ6LkWxJI5O M4jvTlI1OTZ4NUC1
H187 MorQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\VTWM2OD1{ND65PUBvVQ>? MYKyOFE3PjVyNR?=
H526 MnXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJzLk[0JI5O MXGyOFE3PjVyNR?=
N592 M3XFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S4R2lEPTB;MUSuNVIhdk1? NXfSNopHOjRzNk[1NFU>
H620 M4T5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;OUmlEPTB;M{KuOlchdk1? NXzE[WlmOjRzNk[1NFU>
H792 NEG5b3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTR3LkC3JI5O Mmq1NlQyPjZ3MEW=
H1173 NVHhO3o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHIOmRKSzVyPUGyMlYzKG6P M4TYXFI1OTZ4NUC1
AC3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPITYFQUUN3ME2yOU46KG6P MYiyOFE3PjVyNR?=
H82 MV\GeY5kfGmxbjDBd5NigQ>? MnrnN|Ahdk1? MlK2O|IhcA>? NGP4dYtqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MYeyOFE3PjVyNR?=
GLC4 MlHXSpVv[3Srb36gRZN{[Xl? NF3PUXI{OCCwTR?= MkjWO|IhcA>? M4i4[4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MXyyOFE3PjVyNR?=
H146  MUTGeY5kfGmxbjDBd5NigQ>? Mk\oN|Ahdk1? MWq3NkBp MYfpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NI\z[nMzPDF4NkWwOS=>
OVCAR-5 NXraXoc4S2WubDDWbYFjcWyrdImgRZN{[Xl? NV\ZdYg5OC1zMECwJI5O M1:2[|czKGh? MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYnqVWJzOjN7MECxN|Y>
OVCAR-8 NV\3dGFtS2WubDDWbYFjcWyrdImgRZN{[Xl? MoX4NE0yODByIH7N MWK3NkBp MYTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MVeyN|kxODF|Nh?=
A1847 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFvsOpYxNTFyMECgcm0> NWX2XZZQPzJiaB?= NFnuN|JqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGOzNIczOzlyMEGzOi=>
SKOV-3 NYXjWpZFS2WubDDWbYFjcWyrdImgRZN{[Xl? MnLxNE0yODByIH7N NYq2XG5NPzJiaB?= NGLxNIpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUmyOWNwOjN7MECxN|Y>
OVCAR-5 MYTBdI9xfG:|aYOgRZN{[Xl? M1nqb|ExNTFyMDDuUS=> M37WcFI1NzR6L{eyJIg> M2K3dYlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MoPCNlM6ODBzM{[=
OVCAR-8 Ml3oRZBweHSxc3nzJGF{e2G7 NG\4bFYyOC1zMECgcm0> M{\YUVI1NzR6L{eyJIg> M2DubIlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MljGNlM6ODBzM{[=
A1847 MkG4RZBweHSxc3nzJGF{e2G7 NGW4NJAyOC1zMECgcm0> NHj2eJEzPC92OD:3NkBp NHKxSFZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NXfoWmNWOjN7MECxN|Y>
H2228 MlPsR4VtdCCYaXHibYxqfHliQYPzZZk> NWL2c|U5OC1zMECwJI5O MVy3NkBp NWX2UHZFUUN3ME2xN{BvVQ>? M4TJOlI{PTN|Mk[1
H3122 NIfCeGlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYraWmRpOC1zMECwJI5O NXzLSm5{PzJiaB?= Mn76TWM2OD1zMDDuUS=> M2H6XlI{PTN|Mk[1
K008 MoXSR4VtdCCYaXHibYxqfHliQYPzZZk> NVfOfGFqUUN3ME22NEBvVQ>? MnvCNlM1OTh3MkO=
K028 M{TDOGNmdGxiVnnhZoltcXS7IFHzd4F6 MWnJR|UxRTh2IH7N MXmyN|QyQDV{Mx?=
K029 NFvTTFhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4DmRWlEPTB;NE[gcm0> Ml3jNlM1OTh3MkO=
M23 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFi4eHlKSzVyPUO3MlUhdk1? MX[yN|QyQDV{Mx?=
K033 Mlf0R4VtdCCYaXHibYxqfHliQYPzZZk> NEHiTWVKSzVyPUe1MlUhdk1? M4jlZ|I{PDF6NUKz
K008 Mle1SpVv[3Srb36gRZN{[Xl? M17QOVI2OCCwTR?= NEm1b|QzPCCq MofCbY5lfWOnczDHNkBienKnc4S= M2jFUlI{PDF6NUKz
K028 MmLpSpVv[3Srb36gRZN{[Xl? MnroNlUxKG6P MkXoNlQhcA>? NH\RRYtqdmS3Y3XzJGczKGG{cnXzeC=> MWCyN|QyQDV{Mx?=
K029 MYDGeY5kfGmxbjDBd5NigQ>? NEO3b2czPTBibl2= M172PVI1KGh? M2L3[Ilv\HWlZYOgS|Eh[XK{ZYP0 NVfwZ|c5OjN2MUi1NlM>
M23 NEXROXJHfW6ldHnvckBCe3OjeR?= NE\mWHMzPTBibl2= NXjRUmJOOjRiaB?= MX7pcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= M33UbFI{PDF6NUKz
K033 NVnLOJZKTnWwY4Tpc44hSXO|YYm= NFO5[GYzPTBibl2= MX:yOEBp NU[xNXJOcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u Mm\UNlM1OTh3MkO=
K008 MljwRZBweHSxc3nzJGF{e2G7 MVuxNFAhdk1? MlztO|IhcA>? NXvXVHJte2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NFX0TowzOzRzOEWyNy=>
K028 MnTMRZBweHSxc3nzJGF{e2G7 MUCxNFAhdk1? MYi3NkBp Mn7Ed4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MkW0NlM1OTh3MkO=
K029 M4TzcGFxd3C2b4Ppd{BCe3OjeR?= NXnLdYlUOTByIH7N MlvxO|IhcA>? M2HmT5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MnH4NlM1OTh3MkO=
M23 M1PMXWFxd3C2b4Ppd{BCe3OjeR?= NHK3VYcyODBibl2= MVy3NkBp NUfhXHFQe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NHHIUnczOzRzOEWyNy=>
K033 NE\NdJJCeG:ydH;zbZMhSXO|YYm= NEnGbHMyODBibl2= M4\lTlczKGh? MknSd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MVmyN|QyQDV{Mx?=
RD NFrZboJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;ndpFKSzVyPUigcm0> NXrzeVN6OjN|MEO3OFE>
Rh41 MlWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVSwW25KUUN3ME2xNE41KG6P NUHhW|RIOjN|MEO3OFE>
Rh18 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTZwMjDuUS=> MknmNlM{ODN5NEG=
Rh30 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnWyTWM2OD13Lk[gcm0> MV6yN|MxOzd2MR?=
BT-12 Mmf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPpTWM2OD1zND6zJI5O MoTiNlM{ODN5NEG=
CHLA-266 M1HRXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHHc3dHUUN3ME2yO{4yKG6P M3PXelI{OzB|N{Sx
TC-71 NHHlfIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTRwNTDuUS=> NUjJ[Xg3OjN|MEO3OFE>
CHLA-9 NU\TbJZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HIO2lEPTB;ND62JI5O NEHDVoYzOzNyM{e0NS=>
CHLA-10 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDiOmJ4UUN3ME21Mlchdk1? NGK0V5kzOzNyM{e0NS=>
CHLA-258 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDNeodVUUN3ME22MlQhdk1? MXGyN|MxOzd2MR?=
SJ-GBM2 M3G2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4roV2lEPTB;MUKuPUBvVQ>? MW[yN|MxOzd2MR?=
NB-1643 NHfHNmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTdwNDDuUS=> NYH1WlY2OjN|MEO3OFE>
NB-EBc1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnaS4ptUUN3ME2xOk45KG6P MV[yN|MxOzd2MR?=
CHLA-90 NEPpZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ{LkOgcm0> Ml65NlM{ODN5NEG=
CHLA-136 NUX2Nms1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ|LkKgcm0> MUeyN|MxOzd2MR?=
NALM-6 MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3UNZlZUUN3ME2xNU44KG6P M4e0clI{OzB|N{Sx
COG-LL-317 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWTWM2OD12LkSgcm0> M{\0S|I{OzB|N{Sx
RS4;11 NVvTfWJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF|LkWgcm0> M4HVOVI{OzB|N{Sx
MOLT-4 M2LwNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfwVG14UUN3ME2xNE43KG6P MVKyN|MxOzd2MR?=
CCRF-CEM (1) MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfETWM2OD1zMj61JI5O MY[yN|MxOzd2MR?=
CCRF-CEM (2) MlvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PFZmlEPTB;Nz6yJI5O MnW2NlM{ODN5NEG=
Kasumi-1 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTVwODDuUS=> NXqzO3NPOjN|MEO3OFE>
Karpas-299 NF3mUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH6[WR1UUN3ME25MlYhdk1? NELsWHkzOzNyM{e0NS=>
Ramos-RA1 M4X1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\CTWM2OD15LkSgcm0> NXLWc3NUOjN|MEO3OFE>
LNCaP MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRThibl2= NFGyOlIzOzF3MkCwOC=>
VCaP NHziTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTdibl2= NHru[lAzOzF3MkCwOC=>
H1355 NYHmR3pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7JbFRKSzVyPUWgcm0> MUiyN|AyOjJ2OB?=
H157 NIS1PG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jGR2lEPTB;NzDuUS=> M1q5VVI{ODF{MkS4
H460 NGfZWGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPwSI1jUUN3ME24JI5O MVmyN|AyOjJ2OB?=
IA-LM M2HRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XUNWlEPTB;MUCgcm0> Ml\JNlMxOTJ{NEi=
HOP-62 MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXDPG8{UUN3ME2xNUBvVQ>? MWSyN|AyOjJ2OB?=
H23 NH21eJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDGenBKSzVyPUGxJI5O MWmyN|AyOjJ2OB?=
H2030 NUe2c|ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDKTWM2OD1zMjDuUS=> MWSyN|AyOjJ2OB?=
H441 NG\pXIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D1fWlEPTB;MUSgcm0> NYjP[ZR7OjNyMUKyOFg>
H2212 Mo\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjqSoRKSzVyPUG3JI5O M1myc|I{ODF{MkS4
SK-LU-1 NYW5dphtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXWwfpZzUUN3ME2xPEBvVQ>? MWmyN|AyOjJ2OB?=
H2009 NHrRV2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmewTWM2OD1zOTDuUS=> MlfxNlMxOTJ{NEi=
H1792 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkn6TWM2OD1{MDDuUS=> M3[4UFI{ODF{MkS4
COR-L23 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7IepZDUUN3ME2yNkBvVQ>? NWX2[opGOjNyMUKyOFg>
H727 NInoe5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJ6IH7N NX;4e494OjNyMUKyOFg>
H1734 NWDJW5hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W0WmlEPTB;Mkigcm0> NVTke41TOjNyMUKyOFg>
H358 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe0SnhKSzVyPUK5JI5O NILVTI4zOzBzMkK0PC=>
A549 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jJcGlEPTB;NEOgcm0> MYiyN|AyOjJ2OB?=
H2122 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjETWM2OD13MzDuUS=> MonJNlMxOTJ{NEi=
Calu-1 MmPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TYd2lEPTB;NUigcm0> MWOyN|AyOjJ2OB?=
Calu-6 NEPXd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTZ2IH7N M2rLSFI{ODF{MkS4
NCI-H1975 NFHjdoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L3eFQ5KGh? MWXJR|UxRTF4IH7N M{PFblIzOTR2Nk[1
NCI-H1975 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnEVHE4OiCq NX7HPXNuUUN3ME24JI5O M2\QblIzOTR2Nk[1

... 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
  • 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
Smiles CC(C)C1=C(O)C=C(O)C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)[N](C)C=C4

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

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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)
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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.

  • * 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/

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