Ganetespib (STA-9090)

For research use only.

Catalog No.S1159

35 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 35 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 M1OwRWFxd3C2b4Ppd{BCe3OjeR?= MkHTN|AwQDBxMUWwM|I2OCCwTR?= MUCyOE81QC95MjDo M4\PNIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NWnjflZvOjV6OEK1OVA>
MV411 Ml\IRZBweHSxc3nzJGF{e2G7 M{HkSVMxNzhyL{G1NE8zPTBibl2= NITiZ3gzPC92OD:3NkBp MVPpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= MWGyOVg5OjV3MB?=
MGC-803 NHPKd5lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYSwMlEuOTByMDDuUS=> M{T0ZlczKGh? MUXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYmyOVU6ODhyNR?=
SGC-7901 MnvHR4VtdCCYaXHibYxqfHliQYPzZZk> MkHTNE4yNTFyMECgcm0> Mnn4O|IhcA>? NXvrV|RucW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MlmxNlU2QTB6MEW=
MKN-28 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIHVSFkxNjFvMUCwNEBvVQ>? NGP4V4E4OiCq M1H6folvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NF;memgzPTV7MEiwOS=>
MGC-803 NY\3SJoxTnWwY4Tpc44hSXO|YYm= M33hNVAvOS1zMECwJI5O MV:yOEBp M{XoSIlv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? M1\PPVI2PTlyOEC1
HCT-116 NXXveIZrTnWwY4Tpc44hSXO|YYm= NWLnclBPPTCwTR?= MlvVNlQhcA>? NHH4c4hFVVOR MVfpcoR2[2WmIFewM2cyKGG{cnXzeC=> M1TLclI2OjFyN{m0
HT-29 M2DKcWZ2dmO2aX;uJGF{e2G7 NImzXZM2OG6P M{TaO|I1KGh? NVPkRYttTE2VTx?= M3;Jfolv\HWlZXSgS|AwTzFiYYLy[ZN1 NVHqTHQ2OjV{MUC3PVQ>
SCC25 NFWzbmhEgXSxeHnjbZR6KEG|c3H5 NVO2TWVqOTBxNUCgcm0> NV:2cpRVOjRiaB?= MoPF[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NILUdGczPTJyNUSzNC=>
FUDA NEG4d4REgXSxeHnjbZR6KEG|c3H5 NUPKUWVbOTBxNUCgcm0> M3XnZlI1KGh? MVXk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MYeyOVIxPTR|MB?=
Detroit562 MnjoR5l1d3irY3n0fUBCe3OjeR?= M3nsfVExNzVyIH7N NGG1SGkzPCCq M3zT[YRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MXiyOVIxPTR|MB?=
CAL27 MlrMR5l1d3irY3n0fUBCe3OjeR?= NVq5SZdtOTBxNUCgcm0> M2K4W|I1KGh? NEXTeGFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MWGyOVIxPTR|MB?=
DSH1 NYHGZ2g5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTZibl2= Mo\UNlQ4QDR6M{m=
SW-1710 NUPTOI1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jZNmlEPTB;NjDuUS=> Mle2NlQ4QDR6M{m=
T24 NYTW[|hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrLXoo4UUN3ME23JI5O NFzC[GQzPDd6NEizPS=>
RT112 NFfBZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkWyTWM2OD17IH7N MoDYNlQ4QDR6M{m=
639-V NUm1Z4FkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DzOmlEPTB;MUCgcm0> M{LXXVI1Pzh2OEO5
SCaBER MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXlS5pRUUN3ME2xNEBvVQ>? NWWzXmFPOjR5OES4N|k>
BFTC MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vyRmlEPTB;MUegcm0> M3njVVI1Pzh2OEO5
J82 NGfrcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTF6IH7N MnvHNlQ4QDR6M{m=
HT-1376 MnjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfGTWM2OD1{MTDuUS=> NI[0blIzPDd6NEizPS=>
647-V MkLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ5IH7N NHWxXFMzPDd6NEizPS=>
UM-UC3 M4q2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P5bmlEPTB;M{Ogcm0> MorVNlQ4QDR6M{m=
LB831-BLC M4rVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\5TWM2OD1|NDDuUS=> NYLYWpF7OjR5OES4N|k>
KU-19-19 NI\ueHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\qTWM2OD1|NjDuUS=> MX[yOFc5PDh|OR?=
35612 NVHQdo1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTN6IH7N NVHuWVl4OjR5OES4N|k>
5637 MoXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLOWYNKSzVyPUS0JI5O M3vDV|I1Pzh2OEO5
HT-1197 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTI[4dKSzVyPUWzJI5O M2LKSFI1Pzh2OEO5
MGH-U3 NHvKbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P4emlEPTB;NUOgcm0> MnXRNlQ4QDR6M{m=
TCCSUP MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonmTWM2OD1zNEKgcm0> NUTl[JlFOjR5OES4N|k>
RT4 NEW0VnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLOTWM2OD1zN{OzJI5O M1vZWVI1Pzh2OEO5
SW780 NXfRb3dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXuUnlZUUN3ME2zOFUyKG6P MXyyOFc5PDh|OR?=
RKO NF:0dXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL3TWM2OD12IH7N MX2yOFY5Ojd2Nx?=
LS-411 N MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme1TWM2OD13IH7N M32xeFI1Pjh{N{S3
SW620 NFfuR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRThibl2= NGnUPGczPDZ6Mke0Oy=>
HCT-15 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXGXppKSzVyPUigcm0> NVXZR3NuOjR4OEK3OFc>
HuTu-80 Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLhdmlKSzVyPUGzJI5O NXLmT5hIOjR4OEK3OFc>
HCT 116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrGNHhKSzVyPUG0JI5O Ml64NlQ3QDJ5NEe=
COLO-205 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkK3TWM2OD1zNDDuUS=> NG\kXnIzPDZ6Mke0Oy=>
NCI-H747 MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF5IH7N NVjwPFc1OjR4OEK3OFc>
COLO-678 NWPTWFFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPseG9KSzVyPUKxJI5O MX:yOFY5Ojd2Nx?=
LoVo Mo\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJ{IH7N M2S3Z|I1Pjh{N{S3
LS-1034 NYe0eGpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXq1XVBGUUN3ME2zNUBvVQ>? M3vRVVI1Pjh{N{S3
SNU-C2B NUjYdlNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\4TWM2OD12NTDuUS=> MnTmNlQ3QDJ5NEe=
LS-123 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXztR|ZsUUN3ME23N{BvVQ>? MWeyOFY5Ojd2Nx?=
SK-CO-1 NVTybYNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HsTGlEPTB;OEGgcm0> M4jPVlI1Pjh{N{S3
HCC2998 NYPCN2RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;Xb5NKSzVyPUGyPEBvVQ>? MkC5NlQ3QDJ5NEe=
MDA-MB-231 MWPGeY5kfGmxbjDBd5NigQ>? M4\LSFExOCCwTR?= NUPnXXFYOzBibXnu NVq3[ldRcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NUnINIxrOjR{NEiyOlU>
MDA-MB-435 MV7GeY5kfGmxbjDBd5NigQ>? MnexNVAxKG6P M1\n[lMxKG2rbh?= M{\pN4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z M3nsfFI1OjR6Mk[1
BT-20  Mn;XSpVv[3Srb36gRZN{[Xl? NGXCdWkyODBxMkWwJI5O MlvaNlQhcA>? MV;y[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> NXXHcIJTOjRzN{O1OFE>
MDA-MB-231 MkPzSpVv[3Srb36gRZN{[Xl? MYmxNFAhdk1? MlLvNlQhcA>? M33hfYlvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> MojYNlQyPzN3NEG=
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GLC4 M{f6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLCbJBKSzVyPUKwMlQ4KG6P MWeyOFE3PjVyNR?=
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H128 NXXBXppjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLVXW1KSzVyPU[5MlU2KG6P MoL3NlQyPjZ3MEW=
H146 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\2TnpSUUN3ME2yPE42OSCwTR?= NHjRT5AzPDF4NkWwOS=>
H187 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHEeVFKSzVyPUK0Mlk6KG6P NX7zVXp5OjRzNk[1NFU>
H526 M4qweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH1OG9KSzVyPUKxMlY1KG6P NGXKbnEzPDF4NkWwOS=>
N592 NILuZm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HMdmlEPTB;MUSuNVIhdk1? NXfSU|FTOjRzNk[1NFU>
H620 Mn\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXmZ|BbUUN3ME2zNk43PyCwTR?= MXKyOFE3PjVyNR?=
H792 NIq4OoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LmRWlEPTB;NEWuNFchdk1? MYWyOFE3PjVyNR?=
H1173 M2i3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfUTWM2OD1zMj62NkBvVQ>? M1\Ze|I1OTZ4NUC1
AC3 NXvVdZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nLXWlEPTB;MkWuPUBvVQ>? NGPpZ5AzPDF4NkWwOS=>
H82 NGX3b4FHfW6ldHnvckBCe3OjeR?= MoHnN|Ahdk1? M2TVdVczKGh? MV;pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= M{TqfVI1OTZ4NUC1
GLC4 NES0PJJHfW6ldHnvckBCe3OjeR?= MoftN|Ahdk1? NFTtclU4OiCq NVnyRZRCcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M4fHfVI1OTZ4NUC1
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OVCAR-5 NGrMe2ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUKwMVExODBibl2= MonuO|IhcA>? NHXUdo9qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MX2yN|kxODF|Nh?=
OVCAR-8 NUnqbXN4S2WubDDWbYFjcWyrdImgRZN{[Xl? M{TWVlAuOTByMDDuUS=> M{DSNlczKGh? MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFTuNWQzOzlyMEGzOi=>
A1847 NGPwSXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV[wMVExODBibl2= MVm3NkBp M1GxSYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIfL[44zOzlyMEGzOi=>
SKOV-3 MofHR4VtdCCYaXHibYxqfHliQYPzZZk> NHXDVpkxNTFyMECgcm0> MmLjO|IhcA>? NHTobYFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NIfafmYzOzlyMEGzOi=>
OVCAR-5 MWPBdI9xfG:|aYOgRZN{[Xl? NETBcGYyOC1zMECgcm0> MmH4NlQwPDhxN{KgbC=> NYTQdXhEcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NYGxWVFiOjN7MECxN|Y>
OVCAR-8 M2iyb2Fxd3C2b4Ppd{BCe3OjeR?= NGrLTFMyOC1zMECgcm0> M33qV|I1NzR6L{eyJIg> NVXYOnBrcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M1KzTlI{QTByMUO2
A1847 MY\BdI9xfG:|aYOgRZN{[Xl? MmjyNVAuOTByIH7N NXX6fFU5OjRxNEivO|IhcA>? MWfpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 NXHqdZNEOjN7MECxN|Y>
H2228 NGXIU4NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4K2[lAuOTByMDDuUS=> MXy3NkBp NX\a[odtUUN3ME2xN{BvVQ>? MYqyN|U{OzJ4NR?=
H3122 M2HzemNmdGxiVnnhZoltcXS7IFHzd4F6 NWW2b2w2OC1zMECwJI5O MnjvO|IhcA>? MmjGTWM2OD1zMDDuUS=> NGfFfHgzOzV|M{K2OS=>
K008 Mkn5R4VtdCCYaXHibYxqfHliQYPzZZk> M4nONGlEPTB;NkCgcm0> NX7pWG9jOjN2MUi1NlM>
K028 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlrHTWM2OD16NDDuUS=> MnvENlM1OTh3MkO=
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K033 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXTJR|UxRTd3LkWgcm0> NFPP[WozOzRzOEWyNy=>
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Rh41 NFq4cZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljZTWM2OD1zMD60JI5O M4XWdlI{OzB|N{Sx
Rh18 M1\ob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjFcGd3UUN3ME22MlIhdk1? NWDRbWw6OjN|MEO3OFE>
Rh30 MmrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3NTWM2OD13Lk[gcm0> NEXhRY4zOzNyM{e0NS=>
BT-12 NF3JW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHLcXVKSzVyPUG0MlMhdk1? MUiyN|MxOzd2MR?=
CHLA-266 NIXQ[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mle2TWM2OD1{Nz6xJI5O MnTUNlM{ODN5NEG=
TC-71 MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTRwNTDuUS=> M1HO[FI{OzB|N{Sx
CHLA-9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrpTWM2OD12Lk[gcm0> NYPLT2poOjN|MEO3OFE>
CHLA-10 NH3W[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7WbWJKSzVyPUWuO{BvVQ>? Mn\INlM{ODN5NEG=
CHLA-258 M1nMZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmwTWM2OD14LkSgcm0> NGS0OJUzOzNyM{e0NS=>
SJ-GBM2 NG\ZfohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjKdpRCUUN3ME2xNk46KG6P M1PIOVI{OzB|N{Sx
NB-1643 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\k[2xKSzVyPUeuOEBvVQ>? MlXYNlM{ODN5NEG=
NB-EBc1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF4Lkigcm0> MYmyN|MxOzd2MR?=
CHLA-90 NWT6PJZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJ{LkOgcm0> MYmyN|MxOzd2MR?=
CHLA-136 M2DNVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LhfWlEPTB;MkOuNkBvVQ>? NHjtSXUzOzNyM{e0NS=>
NALM-6 NUjseZZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX20eJlNUUN3ME2xNU44KG6P MViyN|MxOzd2MR?=
COG-LL-317 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTRwNDDuUS=> NIrzem4zOzNyM{e0NS=>
RS4;11 NGL2[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nYdGlEPTB;MUOuOUBvVQ>? MoixNlM{ODN5NEG=
MOLT-4 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFyLk[gcm0> MV[yN|MxOzd2MR?=
CCRF-CEM (1) M2PFZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTF{LkWgcm0> M4PxbVI{OzB|N{Sx
CCRF-CEM (2) MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfudmZKSzVyPUeuNkBvVQ>? NFXZdJAzOzNyM{e0NS=>
Kasumi-1 M4f0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX5TWM2OD13Lkigcm0> MUmyN|MxOzd2MR?=
Karpas-299 NFHI[nVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTlwNjDuUS=> NFLFbm0zOzNyM{e0NS=>
Ramos-RA1 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;vPGlEPTB;Nz60JI5O M37EOVI{OzB|N{Sx
LNCaP NFjNcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPJepREUUN3ME24JI5O NVnCU5FyOjNzNUKwNFQ>
VCaP NEmwbm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoqxTWM2OD15IH7N M{HNdlI{OTV{MEC0
H1355 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDpTWM2OD13IH7N M1HJd|I{ODF{MkS4
H157 M2rGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTzUFVGUUN3ME23JI5O NVS1[|hSOjNyMUKyOFg>
H460 M1nCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nLZmlEPTB;ODDuUS=> NX7j[WFmOjNyMUKyOFg>
IA-LM MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi5XYhKSzVyPUGwJI5O MlyzNlMxOTJ{NEi=
HOP-62 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLZTWM2OD1zMTDuUS=> NF3aVFkzOzBzMkK0PC=>
H23 Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXoOFdCUUN3ME2xNUBvVQ>? MUSyN|AyOjJ2OB?=
H2030 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF{IH7N M1;Fb|I{ODF{MkS4
H441 Mo\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTF2IH7N M3XGUVI{ODF{MkS4
H2212 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjzTWM2OD1zNzDuUS=> NEHBRlMzOzBzMkK0PC=>
SK-LU-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfXOIFKSzVyPUG4JI5O MYSyN|AyOjJ2OB?=
H2009 NH\FfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DmZ2lEPTB;MUmgcm0> MY[yN|AyOjJ2OB?=
H1792 M2rPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDrV45KSzVyPUKwJI5O MXeyN|AyOjJ2OB?=
COR-L23 NEjob5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG1TWM2OD1{MjDuUS=> M4P4UVI{ODF{MkS4
H727 NETCNJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJ6IH7N MWiyN|AyOjJ2OB?=
H1734 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Tkd2lEPTB;Mkigcm0> MknhNlMxOTJ{NEi=
H358 M{P3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXONoFKSzVyPUK5JI5O M4G3T|I{ODF{MkS4
A549 M1v1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTR|IH7N MV[yN|AyOjJ2OB?=
H2122 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fu[mlEPTB;NUOgcm0> MXSyN|AyOjJ2OB?=
Calu-1 NWDtRnFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTV6IH7N NYf0WZVROjNyMUKyOFg>
Calu-6 NHvSXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTZ2IH7N M1vlXVI{ODF{MkS4
NCI-H1975 NULqXplJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi0PEBp NFrH[XlKSzVyPUG2JI5O MYOyNlE1PDZ4NR?=
NCI-H1975 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPhO|IhcA>? M2[xXGlEPTB;ODDuUS=> M3\WTVIzOTR2Nk[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
  • 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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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