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 8 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 M4LHWmFxd3C2b4Ppd{BCe3OjeR?= NH\iOVY{OC96MD:xOVAwOjVyIH7N MlL4NlQwPDhxN{KgbC=> MnPMbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz Ml7QNlU5QDJ3NUC=
MV411 M2nzO2Fxd3C2b4Ppd{BCe3OjeR?= NIfBdnM{OC96MD:xOVAwOjVyIH7N NUH4fXhYOjRxNEivO|IhcA>? M17UOIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NGDGZ5MzPTh6MkW1NC=>
MGC-803 NUX2cFRbS2WubDDWbYFjcWyrdImgRZN{[Xl? MlLLNE4yNTFyMECgcm0> MnrkO|IhcA>? NHXubYJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MXuyOVU6ODhyNR?=
SGC-7901 MlmwR4VtdCCYaXHibYxqfHliQYPzZZk> NUC1d2VSOC5zLUGwNFAhdk1? Mn7aO|IhcA>? NHy5VZJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3rkeVI2PTlyOEC1
MKN-28 NGHQWGNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3vLOlAvOS1zMECwJI5O MXW3NkBp MYnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MoLJNlU2QTB6MEW=
MGC-803 MULGeY5kfGmxbjDBd5NigQ>? MUKwMlEuOTByMDDuUS=> MorJNlQhcA>? M2LkT4lv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? M1HvelI2PTlyOEC1
HCT-116 MnPFSpVv[3Srb36gRZN{[Xl? Mne0OVBvVQ>? MYeyOEBp MUDEUXNQ NHHIV2hqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NEjaNYozPTJzMEe5OC=>
HT-29 M1TyUGZ2dmO2aX;uJGF{e2G7 NWjhcoo4PTCwTR?= NH34TVIzPCCq M1f4RWROW09? NGqyNnlqdmS3Y3XkJGcxN0dzIHHydoV{fA>? Mm[0NlUzOTB5OUS=
SCC25 MlTTR5l1d3irY3n0fUBCe3OjeR?= M3rYR|ExNzVyIH7N MV6yOEBp NWDYcZZt\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NY\U[WlQOjV{MEW0N|A>
FUDA MXTDfZRwgGmlaYT5JGF{e2G7 NUjEfIl6OTBxNUCgcm0> MoXVNlQhcA>? NGfpdJRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NXvRUJVUOjV{MEW0N|A>
Detroit562 NX;GcYhVS3m2b4jpZ4l1gSCDc4PhfS=> MWOxNE82OCCwTR?= NH\EPXgzPCCq M2fR[4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MYqyOVIxPTR|MB?=
CAL27 M1[5emN6fG:6aXPpeJkhSXO|YYm= MnHYNVAwPTBibl2= NGjMfGIzPCCq M37hU4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NGC0dJQzPTJyNUSzNC=>
DSH1 M3HrPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;TTWM2OD14IH7N M{fodVI1Pzh2OEO5
SW-1710 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHtXlFKSzVyPU[gcm0> NX;hPYRvOjR5OES4N|k>
T24 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj1emdKSzVyPUegcm0> MmnzNlQ4QDR6M{m=
RT112 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjNVoFiUUN3ME25JI5O MUeyOFc5PDh|OR?=
639-V MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrDeo5{UUN3ME2xNEBvVQ>? M3XTfFI1Pzh2OEO5
SCaBER NXPDO|VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFyIH7N NF3NeW0zPDd6NEizPS=>
BFTC MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XFUGlEPTB;MUegcm0> MVOyOFc5PDh|OR?=
J82 M{[xNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\OW2JRUUN3ME2xPEBvVQ>? MV6yOFc5PDh|OR?=
HT-1376 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITTXItKSzVyPUKxJI5O MV6yOFc5PDh|OR?=
647-V MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jOOmlEPTB;Mkegcm0> M1HvfVI1Pzh2OEO5
UM-UC3 M2Xsfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn5TWM2OD1|MzDuUS=> NYPDbVJSOjR5OES4N|k>
LB831-BLC M3Kx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH24W3JKSzVyPUO0JI5O NI\FcYkzPDd6NEizPS=>
KU-19-19 MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTN4IH7N MYmyOFc5PDh|OR?=
35612 MoXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XtVmlEPTB;M{igcm0> NH;hRokzPDd6NEizPS=>
5637 NWrUWHZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPxc|NKSzVyPUS0JI5O NW\qSFByOjR5OES4N|k>
HT-1197 NHm3O3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XJcmlEPTB;NUOgcm0> NUDGW25OOjR5OES4N|k>
MGH-U3 NGjQdo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnvTWM2OD13MzDuUS=> Mnr5NlQ4QDR6M{m=
TCCSUP NFTEUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV74WGFbUUN3ME2xOFIhdk1? NEm2flkzPDd6NEizPS=>
RT4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP3OFJjUUN3ME2xO|M{KG6P MkPQNlQ4QDR6M{m=
SW780 M3jvV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTxTWM2OD1|NEWxJI5O M13YNlI1Pzh2OEO5
RKO NHnCOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzvTWM2OD12IH7N MojxNlQ3QDJ5NEe=
LS-411 N NHzSZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXQUYpKSzVyPUWgcm0> MXOyOFY5Ojd2Nx?=
SW620 Ml:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnpcml2UUN3ME24JI5O NWHCe4sxOjR4OEK3OFc>
HCT-15 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRThibl2= M4H4WVI1Pjh{N{S3
HuTu-80 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO5TWM2OD1zMzDuUS=> NInxVJEzPDZ6Mke0Oy=>
HCT 116 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF2IH7N NVnzcplIOjR4OEK3OFc>
COLO-205 MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fmRmlEPTB;MUSgcm0> NIfFeFIzPDZ6Mke0Oy=>
NCI-H747 NEHxbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF5IH7N MmnQNlQ3QDJ5NEe=
COLO-678 M2jh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPQTWM2OD1{MTDuUS=> MUCyOFY5Ojd2Nx?=
LoVo NF2y[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\M[GlEPTB;MkKgcm0> MXOyOFY5Ojd2Nx?=
LS-1034 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfaRVZrUUN3ME2zNUBvVQ>? MW[yOFY5Ojd2Nx?=
SNU-C2B NH3s[GhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC3O4lKSzVyPUS1JI5O NX[3NoY1OjR4OEK3OFc>
LS-123 M3Pmemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTd|IH7N MVKyOFY5Ojd2Nx?=
SK-CO-1 Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRThzIH7N MknqNlQ3QDJ5NEe=
HCC2998 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTMSGpKSzVyPUGyPEBvVQ>? NWfFRphoOjR4OEK3OFc>
MDA-MB-231 M{XZXGZ2dmO2aX;uJGF{e2G7 NEDXeWMyODBibl2= NF73VGs{OCCvaX6= NXHvbWVbcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MoD2NlQzPDh{NkW=
MDA-MB-435 M3nQS2Z2dmO2aX;uJGF{e2G7 MYqxNFAhdk1? M3v1OlMxKG2rbh?= NVzOZo15cW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MkD2NlQzPDh{NkW=
BT-20  NI\Gd5VHfW6ldHnvckBCe3OjeR?= NIrkeWUyODBxMkWwJI5O MUCyOEBp NYrJeY9bemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI NGLE[2szPDF5M{W0NS=>
MDA-MB-231 MWLGeY5kfGmxbjDBd5NigQ>? MYWxNFAhdk1? M13PeVI1KGh? NWXUWmJmcW6qaXLpeJMhfGinIH3p[5JifG:{eTDhcoQhcW64YYPpeoUh[2GyYXPpeJnDqA>? NX;kcmZWOjRzN{O1OFE>
H82 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn5XXZyUUN3ME2zNE4zPyCwTR?= NU\ybYEyOjRzNk[1NFU>
GLC4 NYHWPHBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vuOGlEPTB;MkCuOFchdk1? NIKzcW8zPDF4NkWwOS=>
H69 NF33ZZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTRTWM2OD16Mz6zOkBvVQ>? NUPYSYlDOjRzNk[1NFU>
H128 MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjITWhKSzVyPU[5MlU2KG6P MkWzNlQyPjZ3MEW=
H146 NXLTfYdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DaZmlEPTB;MkiuOVEhdk1? MU[yOFE3PjVyNR?=
H187 MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkmzTWM2OD1{ND65PUBvVQ>? MUmyOFE3PjVyNR?=
H526 NUTDUVJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj3ZmdKSzVyPUKxMlY1KG6P MWiyOFE3PjVyNR?=
N592 NVflc|B1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\GTWM2OD1zND6xNkBvVQ>? NVHZZVN{OjRzNk[1NFU>
H620 M1vLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPs[ZRFUUN3ME2zNk43PyCwTR?= MVmyOFE3PjVyNR?=
H792 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTR3LkC3JI5O MXeyOFE3PjVyNR?=
H1173 NYDTeWVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvUTWM2OD1zMj62NkBvVQ>? M132ZVI1OTZ4NUC1
AC3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ3Lkmgcm0> Ml;kNlQyPjZ3MEW=
H82 NVnwSWZoTnWwY4Tpc44hSXO|YYm= M2PuNFMxKG6P NW\4cnNrPzJiaB?= NY\RPY9NcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 MV2yOFE3PjVyNR?=
GLC4 MYrGeY5kfGmxbjDBd5NigQ>? M4e0[VMxKG6P NVj4d2JwPzJiaB?= NUDBd5VWcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M2DOPFI1OTZ4NUC1
H146  M1fSTWZ2dmO2aX;uJGF{e2G7 NVWwVJBKOzBibl2= NFq3bYc4OiCq MoLTbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NF\IVHIzPDF4NkWwOS=>
OVCAR-5 NHfycHhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M33BcVAuOTByMDDuUS=> MWe3NkBp MnHabY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M{jX[VI{QTByMUO2
OVCAR-8 NYPZU5o4S2WubDDWbYFjcWyrdImgRZN{[Xl? NXnFellbOC1zMECwJI5O NIfv[5A4OiCq M1jYOolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWPofGR4OjN7MECxN|Y>
A1847 NW\wO21oS2WubDDWbYFjcWyrdImgRZN{[Xl? MUCwMVExODBibl2= MkHPO|IhcA>? NYP3S|NYcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1ezPVI{QTByMUO2
SKOV-3 MojCR4VtdCCYaXHibYxqfHliQYPzZZk> M3zKTlAuOTByMDDuUS=> MW[3NkBp NH7adnNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MnnjNlM6ODBzM{[=
OVCAR-5 NVr0WHM5SXCxcITvd4l{KEG|c3H5 M3rsXlExNTFyMDDuUS=> M{nYeVI1NzR6L{eyJIg> NYXnXHRKcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NWXGVHQzOjN7MECxN|Y>
OVCAR-8 MXHBdI9xfG:|aYOgRZN{[Xl? MWSxNE0yODBibl2= NIHJ[ZEzPC92OD:3NkBp NIjHNWtqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NIHWd3czOzlyMEGzOi=>
A1847 NWHkXZJUSXCxcITvd4l{KEG|c3H5 M2\yWVExNTFyMDDuUS=> NY[xd|VnOjRxNEivO|IhcA>? NEPHcXNqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M1;iflI{QTByMUO2
H2228 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3rKR|AuOTByMDDuUS=> NHXxXZU4OiCq M1vWW2lEPTB;MUOgcm0> NWHEfGVSOjN3M{OyOlU>
H3122 Mk\SR4VtdCCYaXHibYxqfHliQYPzZZk> MXqwMVExODBibl2= NIOxdVY4OiCq NYGzSoxVUUN3ME2xNEBvVQ>? MYCyN|U{OzJ4NR?=
K008 MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGrBTmpKSzVyPU[wJI5O MkPINlM1OTh3MkO=
K028 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVHWT243UUN3ME24OEBvVQ>? NUW1WG14OjN2MUi1NlM>
K029 M1jz[mNmdGxiVnnhZoltcXS7IFHzd4F6 NVrvZ5lsUUN3ME20OkBvVQ>? NFfuVGUzOzRzOEWyNy=>
M23 M{DMd2NmdGxiVnnhZoltcXS7IFHzd4F6 NULYTpJ3UUN3ME2zO{42KG6P Mn7sNlM1OTh3MkO=
K033 NF\Gfm9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnLmTWM2OD15NT61JI5O NGTt[JozOzRzOEWyNy=>
K008 NF\lVXlHfW6ldHnvckBCe3OjeR?= M2jIflI2OCCwTR?= MVeyOEBp MkDabY5lfWOnczDHNkBienKnc4S= M{fJZVI{PDF6NUKz
K028 M{\z[2Z2dmO2aX;uJGF{e2G7 M4fhfFI2OCCwTR?= MkjJNlQhcA>? MXvpcoR2[2W|IFeyJIFzemW|dB?= MkTpNlM1OTh3MkO=
K029 MVjGeY5kfGmxbjDBd5NigQ>? NWK4ZmxSOjVyIH7N MkS2NlQhcA>? M{nVV4lv\HWlZYOgS|Eh[XK{ZYP0 NFrGRWwzOzRzOEWyNy=>
M23 MnXBSpVv[3Srb36gRZN{[Xl? M{LGNlI2OCCwTR?= NXjaRZdZOjRiaB?= M2\5[Ilv\HWlZYOgS|Eh[W6mIFeyM20h[XK{ZYP0 MXqyN|QyQDV{Mx?=
K033 M4X6VWZ2dmO2aX;uJGF{e2G7 MVmyOVAhdk1? MW[yOEBp M2HqWYlv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= NX\N[VVkOjN2MUi1NlM>
K008 Mn7aRZBweHSxc3nzJGF{e2G7 M2nUUFExOCCwTR?= NVfFWVh5PzJiaB?= NVfxPZp6e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= Ml7qNlM1OTh3MkO=
K028 NXHnSpJGSXCxcITvd4l{KEG|c3H5 MlzHNVAxKG6P M3nEZlczKGh? NV\JOopje2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= Ml63NlM1OTh3MkO=
K029 MWHBdI9xfG:|aYOgRZN{[Xl? MkfjNVAxKG6P MYi3NkBp NVPJbXJJe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MlLqNlM1OTh3MkO=
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... Click to View More Cell Line Experimental Data

In vivo Administration of Ganetespib leads to significant tumor shrinkage in several tumor xenograft models in mice and appears to be less toxic. Furthermore Ganetespib demonstrated better tumor penetration compared with tanespimycin.[2] Ganetespib inhibits in vivo tumor growth in both malignant mast cell and OSA xenograft models. Ganetespib significantly inhibits tumor growth when dosed with two repeating cycles of 25 mg/kg/day for 3 days, with a %T/C value of 18. Ganetespib is well-tolerated, with the vehicle and Ganetespib groups having average bodyweight changes relative to the start of the study of +0.3% and -8.1% on day 17, respectively.[4]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: OSA cells
  • Concentrations: 0.001-1μM
  • Incubation Time: 5 days
  • Method: A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Female severe combined immune-deficient (SCID) mice
  • Formulation: In DMSO and diluted 1:10 with 20% Cremophor RH 40
  • Dosages: 25 mg/kg/day for 3 days
  • Administration: Tail vein injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (109.76 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(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

Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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