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
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Cited by 9 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 MWjBdI9xfG:|aYOgRZN{[Xl? NW\OdoVWOzBxOECvNVUxNzJ3MDDuUS=> M2C5bFI1NzR6L{eyJIg> MmP4bY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MYiyOVg5OjV3MB?=
MV411 NVL3ZZM3SXCxcITvd4l{KEG|c3H5 NH7CVWM{OC96MD:xOVAwOjVyIH7N NYXXe3pwOjRxNEivO|IhcA>? NVXGR4xicW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ NGfFZlYzPTh6MkW1NC=>
MGC-803 M3jadmNmdGxiVnnhZoltcXS7IFHzd4F6 MV[wMlEuOTByMDDuUS=> NGDmemI4OiCq NEHG[4xqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1v6bFI2PTlyOEC1
SGC-7901 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWTYVnE1OC5zLUGwNFAhdk1? M1XqV|czKGh? NGjv[lZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Mn;PNlU2QTB6MEW=
MKN-28 MnHBR4VtdCCYaXHibYxqfHliQYPzZZk> MlHWNE4yNTFyMECgcm0> NV7KcI5xPzJiaB?= M4S2N4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mln2NlU2QTB6MEW=
MGC-803 M4S5e2Z2dmO2aX;uJGF{e2G7 MnrLNE4yNTFyMECgcm0> M2XJXVI1KGh? NV7BbpFEcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 M37wdFI2PTlyOEC1
HCT-116 M33Xd2Z2dmO2aX;uJGF{e2G7 M{flVVUxdk1? NH\4OIQzPCCq NUW2b5RwTE2VTx?= MYfpcoR2[2WmIFewM2cyKGG{cnXzeC=> MkfaNlUzOTB5OUS=
HT-29 MVXGeY5kfGmxbjDBd5NigQ>? NFnEeJQ2OG6P M{LNdlI1KGh? Mk\VSG1UVw>? MnuxbY5lfWOnZDDHNE9IOSCjcoLld5Q> Mn;wNlUzOTB5OUS=
SCC25 M{fXWmN6fG:6aXPpeJkhSXO|YYm= Mn3LNVAwPTBibl2= M1TiVlI1KGh? NHnYfYll\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MmT5NlUzODV2M{C=
FUDA MoHwR5l1d3irY3n0fUBCe3OjeR?= MWexNE82OCCwTR?= MmjQNlQhcA>? MoXu[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MXqyOVIxPTR|MB?=
Detroit562 NXfNS5NiS3m2b4jpZ4l1gSCDc4PhfS=> NVvOfVBFOTBxNUCgcm0> M3[3VVI1KGh? NW\DNXFH\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MlfRNlUzODV2M{C=
CAL27 NHHGWWhEgXSxeHnjbZR6KEG|c3H5 MV:xNE82OCCwTR?= NUTCeWxDOjRiaB?= MU\k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MkO3NlUzODV2M{C=
DSH1 NFLmWoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPjfoZKSzVyPU[gcm0> Mnv2NlQ4QDR6M{m=
SW-1710 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\Q[3RKSzVyPU[gcm0> MnnzNlQ4QDR6M{m=
T24 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n0cGlEPTB;NzDuUS=> MmXaNlQ4QDR6M{m=
RT112 M1m4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfaTWM2OD17IH7N MY[yOFc5PDh|OR?=
639-V NVTPTG1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LTU2lEPTB;MUCgcm0> NXq3NGE5OjR5OES4N|k>
SCaBER MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFyIH7N MlzTNlQ4QDR6M{m=
BFTC MlnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF5IH7N MYqyOFc5PDh|OR?=
J82 MkmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m4fmlEPTB;MUigcm0> MofVNlQ4QDR6M{m=
HT-1376 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJzIH7N MXmyOFc5PDh|OR?=
647-V M1vZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ5IH7N MVeyOFc5PDh|OR?=
UM-UC3 M{fpTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTN|IH7N M{W2fVI1Pzh2OEO5
LB831-BLC NEiyXmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTN2IH7N MUCyOFc5PDh|OR?=
KU-19-19 NXnDcpl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWweY57UUN3ME2zOkBvVQ>? M4XEeFI1Pzh2OEO5
35612 M3nP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXFfGxXUUN3ME2zPEBvVQ>? MXyyOFc5PDh|OR?=
5637 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTR2IH7N M1nRUlI1Pzh2OEO5
HT-1197 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGxflR[UUN3ME21N{BvVQ>? NVjYPVhjOjR5OES4N|k>
MGH-U3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XxeGlEPTB;NUOgcm0> MUKyOFc5PDh|OR?=
TCCSUP NWrqVY8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF2MjDuUS=> MX:yOFc5PDh|OR?=
RT4 NXr3eZR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjsXpdKSzVyPUG3N|Mhdk1? MmLsNlQ4QDR6M{m=
SW780 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN2NUGgcm0> NIXKOI0zPDd6NEizPS=>
RKO NYHRVYl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTkTWM2OD12IH7N NGe5eZMzPDZ6Mke0Oy=>
LS-411 N MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37qe2lEPTB;NTDuUS=> MlrUNlQ3QDJ5NEe=
SW620 NX:3fGlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITwT3dKSzVyPUigcm0> M1PZVVI1Pjh{N{S3
HCT-15 NVv2N3BRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OzUWlEPTB;ODDuUS=> NIHmXnczPDZ6Mke0Oy=>
HuTu-80 M3nqOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTF|IH7N Mk\XNlQ3QDJ5NEe=
HCT 116 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLnb5JKSzVyPUG0JI5O MUWyOFY5Ojd2Nx?=
COLO-205 NITQXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF2IH7N NEjpN5czPDZ6Mke0Oy=>
NCI-H747 M1fPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnGzTWM2OD1zNzDuUS=> NUXSNo05OjR4OEK3OFc>
COLO-678 M3O1TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJzIH7N MoLFNlQ3QDJ5NEe=
LoVo MkjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJ{IH7N NX7NWphzOjR4OEK3OFc>
LS-1034 NH\TZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\0eYdKSzVyPUOxJI5O NFnq[VYzPDZ6Mke0Oy=>
SNU-C2B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTHfpVKSzVyPUS1JI5O NEPJTIkzPDZ6Mke0Oy=>
LS-123 M4rwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIniU3ZKSzVyPUezJI5O MXyyOFY5Ojd2Nx?=
SK-CO-1 NXzodWNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRThzIH7N MmHXNlQ3QDJ5NEe=
HCC2998 NGPZdpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj5c3BpUUN3ME2xNlghdk1? NHu0OnQzPDZ6Mke0Oy=>
MDA-MB-231 NIHFXXVHfW6ldHnvckBCe3OjeR?= M4HOXlExOCCwTR?= MUizNEBucW5? MYrpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NIjSVGszPDJ2OEK2OS=>
MDA-MB-435 MX;GeY5kfGmxbjDBd5NigQ>? NVrkR5JROTByIH7N MVGzNEBucW5? NVLKfI9rcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MWeyOFI1QDJ4NR?=
BT-20  NUnIPZh[TnWwY4Tpc44hSXO|YYm= Mn\YNVAxNzJ3MDDuUS=> NXrYSG5QOjRiaB?= MlrrdoV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH MVyyOFE4OzV2MR?=
MDA-MB-231 MWnGeY5kfGmxbjDBd5NigQ>? NF3sSJMyODBibl2= Mn24NlQhcA>? NHnJcnJqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh M1HBflI1OTd|NUSx
H82 M17Qe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNyLkK3JI5O MViyOFE3PjVyNR?=
GLC4 M2Hhcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jxSmlEPTB;MkCuOFchdk1? MX[yOFE3PjVyNR?=
H69 M4jFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHSx[lBKSzVyPUizMlM3KG6P Ml\MNlQyPjZ3MEW=
H128 NHnuem9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOwTWM2OD14OT61OUBvVQ>? Mly2NlQyPjZ3MEW=
H146 MmrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\tWHlwUUN3ME2yPE42OSCwTR?= M3\iTFI1OTZ4NUC1
H187 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfHN2RKSzVyPUK0Mlk6KG6P NWHpc|IxOjRzNk[1NFU>
H526 NIDmbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\TU2lEPTB;MkGuOlQhdk1? M17nclI1OTZ4NUC1
N592 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnlRpVWUUN3ME2xOE4yOiCwTR?= NX;PZpdqOjRzNk[1NFU>
H620 NFrCXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3TTWM2OD1|Mj62O{BvVQ>? MXuyOFE3PjVyNR?=
H792 NGjLdGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jWeWlEPTB;NEWuNFchdk1? NGjSWYszPDF4NkWwOS=>
H1173 MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\MTWM2OD1zMj62NkBvVQ>? NF;IRYUzPDF4NkWwOS=>
AC3 MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTJ3Lkmgcm0> MYqyOFE3PjVyNR?=
H82 M2[0OmZ2dmO2aX;uJGF{e2G7 NHPJTGk{OCCwTR?= MUG3NkBp MYrpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= M2DhNVI1OTZ4NUC1
GLC4 NVLQT2huTnWwY4Tpc44hSXO|YYm= Mkn2N|Ahdk1? MXW3NkBp MnTvbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NWK5d29ZOjRzNk[1NFU>
H146  NIPRRYdHfW6ldHnvckBCe3OjeR?= Mkn5N|Ahdk1? M1H2[VczKGh? M1e2NIlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NWXnOWc5OjRzNk[1NFU>
OVCAR-5 NIjFZ4JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4q0SVAuOTByMDDuUS=> NIPlWnk4OiCq Mkf0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NGHJS2QzOzlyMEGzOi=>
OVCAR-8 NWHKbJRLS2WubDDWbYFjcWyrdImgRZN{[Xl? M{f1eFAuOTByMDDuUS=> NVTQT3VNPzJiaB?= NVLtO2E1cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVSyN|kxODF|Nh?=
A1847 MnPTR4VtdCCYaXHibYxqfHliQYPzZZk> NVfpSlFROC1zMECwJI5O NV;ze4lUPzJiaB?= NWLQN5RncW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M121bFI{QTByMUO2
SKOV-3 Mkf2R4VtdCCYaXHibYxqfHliQYPzZZk> NV63c5Q1OC1zMECwJI5O MnPaO|IhcA>? MkPBbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NYK3RmhLOjN7MECxN|Y>
OVCAR-5 MWnBdI9xfG:|aYOgRZN{[Xl? MnuxNVAuOTByIH7N NF65[nYzPC92OD:3NkBp M{\0U4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MlfDNlM6ODBzM{[=
OVCAR-8 M1XUNmFxd3C2b4Ppd{BCe3OjeR?= NHHiXZkyOC1zMECgcm0> MXiyOE81QC95MjDo NUPzd2pwcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NVrEXZJsOjN7MECxN|Y>
A1847 M{HmOWFxd3C2b4Ppd{BCe3OjeR?= MYmxNE0yODBibl2= MmjZNlQwPDhxN{KgbC=> NIrROIlqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M1WwbVI{QTByMUO2
H2228 NFTsPYRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUSwMVExODBibl2= MnqxO|IhcA>? MXfJR|UxRTF|IH7N NGP5OW0zOzV|M{K2OS=>
H3122 NYXI[mY1S2WubDDWbYFjcWyrdImgRZN{[Xl? NXzzSFV[OC1zMECwJI5O MnLRO|IhcA>? NXHTc2tXUUN3ME2xNEBvVQ>? M2LsOlI{PTN|Mk[1
K008 M3TIWGNmdGxiVnnhZoltcXS7IFHzd4F6 M{TYdWlEPTB;NkCgcm0> NXSwNFcxOjN2MUi1NlM>
K028 NUXUO2pGS2WubDDWbYFjcWyrdImgRZN{[Xl? M4XPdWlEPTB;OESgcm0> NF7S[nEzOzRzOEWyNy=>
K029 NHTEPY9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXHCNIZQUUN3ME20OkBvVQ>? NH60dZczOzRzOEWyNy=>
M23 MoTSR4VtdCCYaXHibYxqfHliQYPzZZk> M4W1W2lEPTB;M{euOUBvVQ>? NViy[GhyOjN2MUi1NlM>
K033 M4fIZWNmdGxiVnnhZoltcXS7IFHzd4F6 NF7ZV4RKSzVyPUe1MlUhdk1? NFfCWIEzOzRzOEWyNy=>
K008 NV\5TWN4TnWwY4Tpc44hSXO|YYm= M1:zT|I2OCCwTR?= Mo\XNlQhcA>? MUTpcoR2[2W|IFeyJIFzemW|dB?= MWOyN|QyQDV{Mx?=
K028 MVLGeY5kfGmxbjDBd5NigQ>? M4LNTVI2OCCwTR?= NIjZblIzPCCq MlXjbY5lfWOnczDHNkBienKnc4S= Mn3ZNlM1OTh3MkO=
K029 MmTRSpVv[3Srb36gRZN{[Xl? MmqxNlUxKG6P MmrwNlQhcA>? NEPHUGhqdmS3Y3XzJGcyKGG{cnXzeC=> MmXmNlM1OTh3MkO=
M23 NX;s[pJGTnWwY4Tpc44hSXO|YYm= NUfKclNJOjVyIH7N MWGyOEBp MX;pcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= M4XhfFI{PDF6NUKz
K033 M1jaOGZ2dmO2aX;uJGF{e2G7 M4XDOVI2OCCwTR?= NF7uXZMzPCCq NWnnNZZzcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u MnjPNlM1OTh3MkO=
K008 NVfsZXhuSXCxcITvd4l{KEG|c3H5 M4PVZVExOCCwTR?= NITNXmU4OiCq NGSzS|N{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| M1HlWlI{PDF6NUKz
K028 MUnBdI9xfG:|aYOgRZN{[Xl? MmLHNVAxKG6P M2LpSVczKGh? MoS2d4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MVeyN|QyQDV{Mx?=
K029 MomyRZBweHSxc3nzJGF{e2G7 MkD6NVAxKG6P MVK3NkBp NUTYTGs3e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NFfH[5IzOzRzOEWyNy=>
M23 NWn5eFZuSXCxcITvd4l{KEG|c3H5 MV6xNFAhdk1? Mmm4O|IhcA>? M{\rWZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NIGxPIkzOzRzOEWyNy=>
K033 MULBdI9xfG:|aYOgRZN{[Xl? NFzXemEyODBibl2= MYS3NkBp NUTOeVVFe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= Ml7HNlM1OTh3MkO=
RD NX7OOZpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HGfGlEPTB;ODDuUS=> NWHCTpQ2OjN|MEO3OFE>
Rh41 NXK4THJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFyLkSgcm0> NH:0dokzOzNyM{e0NS=>
Rh18 NYXBVoFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13GeWlEPTB;Nj6yJI5O MWqyN|MxOzd2MR?=
Rh30 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzTNpVjUUN3ME21MlYhdk1? M1W3V|I{OzB|N{Sx
BT-12 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF2LkOgcm0> NWTQfZNCOjN|MEO3OFE>
CHLA-266 Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJ5LkGgcm0> M1fO[FI{OzB|N{Sx
TC-71 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTRwNTDuUS=> MX6yN|MxOzd2MR?=
CHLA-9 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVewfGhlUUN3ME20MlYhdk1? NGH5OG8zOzNyM{e0NS=>
CHLA-10 NVfy[G5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTVwNzDuUS=> M3z6OVI{OzB|N{Sx
CHLA-258 MlrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\YTWM2OD14LkSgcm0> NHfZdZIzOzNyM{e0NS=>
SJ-GBM2 NVfNUJZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\EOWlEPTB;MUKuPUBvVQ>? M1PsTVI{OzB|N{Sx
NB-1643 NV\qeGtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjSUolKSzVyPUeuOEBvVQ>? M3z1Z|I{OzB|N{Sx
NB-EBc1 MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYThVpNmUUN3ME2xOk45KG6P NYjrVnFFOjN|MEO3OFE>
CHLA-90 M1TjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH0TWM2OD1{Mj6zJI5O MWmyN|MxOzd2MR?=
CHLA-136 Mnf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nZVWlEPTB;MkOuNkBvVQ>? MUiyN|MxOzd2MR?=
NALM-6 Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTFzLkegcm0> MYiyN|MxOzd2MR?=
COG-LL-317 NFTOcldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTRwNDDuUS=> MViyN|MxOzd2MR?=
RS4;11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTF|LkWgcm0> NILVV3QzOzNyM{e0NS=>
MOLT-4 MnnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\sTWM2OD1zMD62JI5O MU[yN|MxOzd2MR?=
CCRF-CEM (1) NVzycmt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnPSWpKSzVyPUGyMlUhdk1? MVeyN|MxOzd2MR?=
CCRF-CEM (2) MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTdwMjDuUS=> M4fVSFI{OzB|N{Sx
Kasumi-1 M{Psdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonqTWM2OD13Lkigcm0> MlrONlM{ODN5NEG=
Karpas-299 NF\IWpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTlwNjDuUS=> MXuyN|MxOzd2MR?=
Ramos-RA1 NUO4VIdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTdwNDDuUS=> M1Xn[|I{OzB|N{Sx
LNCaP NF3RUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnzVVRKSzVyPUigcm0> NW\nTmRlOjNzNUKwNFQ>
VCaP MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjWZnFKSzVyPUegcm0> NFXMOnkzOzF3MkCwOC=>
H1355 NFLiNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXjWWdKSzVyPUWgcm0> MVGyN|AyOjJ2OB?=
H157 M4rxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LzfGlEPTB;NzDuUS=> Ml\rNlMxOTJ{NEi=
H460 NHP2UItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzuc4NGUUN3ME24JI5O NIGxfHMzOzBzMkK0PC=>
IA-LM NU\wS2R6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\iR4tKSzVyPUGwJI5O M2TEelI{ODF{MkS4
HOP-62 NWfI[FZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHjU5VKSzVyPUGxJI5O NInENWIzOzBzMkK0PC=>
H23 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7TXWtrUUN3ME2xNUBvVQ>? MmfTNlMxOTJ{NEi=
H2030 M3S3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG0Z2pKSzVyPUGyJI5O MmfhNlMxOTJ{NEi=
H441 NYLsbnVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnQU25NUUN3ME2xOEBvVQ>? MUmyN|AyOjJ2OB?=
H2212 NWnlXpZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrGTWM2OD1zNzDuUS=> M3vMWFI{ODF{MkS4
SK-LU-1 MmXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF6IH7N MoXsNlMxOTJ{NEi=
H2009 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF7IH7N NXvsTVVjOjNyMUKyOFg>
H1792 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf3OWRKSzVyPUKwJI5O MVmyN|AyOjJ2OB?=
COR-L23 Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITx[YhKSzVyPUKyJI5O M1v1[FI{ODF{MkS4
H727 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjzdoNKSzVyPUK4JI5O NVTqZ2NiOjNyMUKyOFg>
H1734 M4joPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLHTWM2OD1{ODDuUS=> NELOfoQzOzBzMkK0PC=>
H358 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPxTWM2OD1{OTDuUS=> M4m0eVI{ODF{MkS4
A549 NXrncllMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn3TWM2OD12MzDuUS=> M3jxdlI{ODF{MkS4
H2122 NV;0VVBQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonLTWM2OD13MzDuUS=> MmLrNlMxOTJ{NEi=
Calu-1 M1;mc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[2TWM2OD13ODDuUS=> M4DXPVI{ODF{MkS4
Calu-6 M3Hybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoGyTWM2OD14NDDuUS=> NEftelYzOzBzMkK0PC=>
NCI-H1975 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7BSYc1QCCq NU[2ZZlQUUN3ME2xOkBvVQ>? M1yyOlIzOTR2Nk[1
NCI-H1975 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\CO|IhcA>? Mk\MTWM2OD16IH7N MWSyNlE1PDZ4NR?=

... 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

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1

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) Products4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID