Ganetespib (STA-9090)

For research use only.

Catalog No.S1159

31 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 31 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 MnPuRZBweHSxc3nzJGF{e2G7 NWHORZhLOzBxOECvNVUxNzJ3MDDuUS=> NV31T|EzOjRxNEivO|IhcA>? NFjkR2NqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NYe0RlU5OjV6OEK1OVA>
MV411 NH\oZYxCeG:ydH;zbZMhSXO|YYm= NEXqPYE{OC96MD:xOVAwOjVyIH7N NHX5NIkzPC92OD:3NkBp NIDVdJVqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MljJNlU5QDJ3NUC=
MGC-803 MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYewMlEuOTByMDDuUS=> MWm3NkBp NVjWVmNocW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWOyOVU6ODhyNR?=
SGC-7901 M4fMXGNmdGxiVnnhZoltcXS7IFHzd4F6 NIjLOYUxNjFvMUCwNEBvVQ>? Mlf0O|IhcA>? NV7TTFQzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHq5S2gzPTV7MEiwOS=>
MKN-28 MnrnR4VtdCCYaXHibYxqfHliQYPzZZk> NVvYeoZKOC5zLUGwNFAhdk1? MWO3NkBp NILid2JqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlHyNlU2QTB6MEW=
MGC-803 MVvGeY5kfGmxbjDBd5NigQ>? NUOxUYZSOC5zLUGwNFAhdk1? Ml\0NlQhcA>? NX35bIZGcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 MmTWNlU2QTB6MEW=
HCT-116 M3eyfGZ2dmO2aX;uJGF{e2G7 MlHLOVBvVQ>? MYqyOEBp MWTEUXNQ NVzLUpQycW6mdXPl[EBIOC:JMTDhdpJme3R? Mom1NlUzOTB5OUS=
HT-29 NXnES|YzTnWwY4Tpc44hSXO|YYm= M17zZVUxdk1? NHrMXG0zPCCq NGrrRnhFVVOR NEXrTHhqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MWmyOVIyODd7NB?=
SCC25 M3X5XWN6fG:6aXPpeJkhSXO|YYm= MX2xNE82OCCwTR?= NYra[WJWOjRiaB?= Mkn1[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MkH0NlUzODV2M{C=
FUDA NWfqbJhUS3m2b4jpZ4l1gSCDc4PhfS=> NIDXOHYyOC93MDDuUS=> MmrkNlQhcA>? NW\1WnhD\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NGi4cVYzPTJyNUSzNC=>
Detroit562 NVzhVZlMS3m2b4jpZ4l1gSCDc4PhfS=> M4PZ[VExNzVyIH7N NEHzU4QzPCCq MXjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NXLYZ5d1OjV{MEW0N|A>
CAL27 NInjTGVEgXSxeHnjbZR6KEG|c3H5 MnPqNVAwPTBibl2= NYT1XWxDOjRiaB?= MVPk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NVLpTpBKOjV{MEW0N|A>
DSH1 M4rNb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvxVFNKSzVyPU[gcm0> MofQNlQ4QDR6M{m=
SW-1710 NYTBSIlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHidHNKSzVyPU[gcm0> MmP1NlQ4QDR6M{m=
T24 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTdibl2= MmfVNlQ4QDR6M{m=
RT112 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITPfVVKSzVyPUmgcm0> MmDKNlQ4QDR6M{m=
639-V NGHVSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTmTWM2OD1zMDDuUS=> MlvqNlQ4QDR6M{m=
SCaBER MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjySYVsUUN3ME2xNEBvVQ>? MVGyOFc5PDh|OR?=
BFTC NEXUeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHTcZJjUUN3ME2xO{BvVQ>? NWjYVYM5OjR5OES4N|k>
J82 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rxR2lEPTB;MUigcm0> M4jXdFI1Pzh2OEO5
HT-1376 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTufGZMUUN3ME2yNUBvVQ>? M2\D[VI1Pzh2OEO5
647-V NHH6S4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJ5IH7N M1LO[lI1Pzh2OEO5
UM-UC3 NWPyfGl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEG2XmZKSzVyPUOzJI5O M3LocFI1Pzh2OEO5
LB831-BLC NV\zRWVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:1ZnRFUUN3ME2zOEBvVQ>? NILaSnEzPDd6NEizPS=>
KU-19-19 NX33bmpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorETWM2OD1|NjDuUS=> M33y[lI1Pzh2OEO5
35612 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fmZ2lEPTB;M{igcm0> MnXMNlQ4QDR6M{m=
5637 M4XTO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrzbINSUUN3ME20OEBvVQ>? MojNNlQ4QDR6M{m=
HT-1197 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D1dGlEPTB;NUOgcm0> NHXOOIIzPDd6NEizPS=>
MGH-U3 M37ObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7oTpJmUUN3ME21N{BvVQ>? MUeyOFc5PDh|OR?=
TCCSUP NIrOcJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\DOnhWUUN3ME2xOFIhdk1? MVSyOFc5PDh|OR?=
RT4 NH7KTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF5M{Ogcm0> MV:yOFc5PDh|OR?=
SW780 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3tUIlTUUN3ME2zOFUyKG6P NXPKT5FzOjR5OES4N|k>
RKO MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;yOoliUUN3ME20JI5O NYXUOJVIOjR4OEK3OFc>
LS-411 N NYK4Vph5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm1[oE{UUN3ME21JI5O MVqyOFY5Ojd2Nx?=
SW620 NH\lS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT0UIEyUUN3ME24JI5O MV:yOFY5Ojd2Nx?=
HCT-15 M1fLdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRThibl2= NGfCXHQzPDZ6Mke0Oy=>
HuTu-80 NUD2Um0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXieVkxUUN3ME2xN{BvVQ>? NUTPTmZVOjR4OEK3OFc>
HCT 116 NXj5[lNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF2IH7N M4HRRVI1Pjh{N{S3
COLO-205 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;2VJdOUUN3ME2xOEBvVQ>? MnrUNlQ3QDJ5NEe=
NCI-H747 M{Lkb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF5IH7N M3qxUVI1Pjh{N{S3
COLO-678 NVTMTYpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvLc4xKSzVyPUKxJI5O NUOyXXVNOjR4OEK3OFc>
LoVo MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;wOG41UUN3ME2yNkBvVQ>? M17WfFI1Pjh{N{S3
LS-1034 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS1WXZKSzVyPUOxJI5O Mnv0NlQ3QDJ5NEe=
SNU-C2B MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzBdo1zUUN3ME20OUBvVQ>? MnX6NlQ3QDJ5NEe=
LS-123 NV3zPVRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjOTJhKSzVyPUezJI5O MV:yOFY5Ojd2Nx?=
SK-CO-1 MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH1PY82UUN3ME24NUBvVQ>? NGrzUWozPDZ6Mke0Oy=>
HCC2998 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF{ODDuUS=> NV3iU5Q6OjR4OEK3OFc>
MDA-MB-231 MknTSpVv[3Srb36gRZN{[Xl? NVXJWWJTOTByIH7N MmjSN|AhdWmw NYLsXFFUcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MX:yOFI1QDJ4NR?=
MDA-MB-435 M33US2Z2dmO2aX;uJGF{e2G7 NXjqWmQ1OTByIH7N NWfidpZiOzBibXnu NYnkSo57cW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MmTkNlQzPDh{NkW=
BT-20  MV;GeY5kfGmxbjDBd5NigQ>? NXP1b4RCOTByL{K1NEBvVQ>? MnzoNlQhcA>? MXzy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> MYqyOFE4OzV2MR?=
MDA-MB-231 NXHkWIl[TnWwY4Tpc44hSXO|YYm= M2jINVExOCCwTR?= M4rCcVI1KGh? NYHCWlZCcW6qaXLpeJMhfGinIH3p[5JifG:{eTDhcoQhcW64YYPpeoUh[2GyYXPpeJnDqA>? NXLYd5J2OjRzN{O1OFE>
H82 NFHDUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNyLkK3JI5O MoHCNlQyPjZ3MEW=
GLC4 M{T3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJyLkS3JI5O NVS5TlFzOjRzNk[1NFU>
H69 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDJOYtuUUN3ME24N{4{PiCwTR?= MYCyOFE3PjVyNR?=
H128 NYjvOGNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHRR|hNUUN3ME22PU42PSCwTR?= NIXEcWEzPDF4NkWwOS=>
H146 M1v3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrXdncyUUN3ME2yPE42OSCwTR?= Mn;jNlQyPjZ3MEW=
H187 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDvb2RqUUN3ME2yOE46QSCwTR?= MnXINlQyPjZ3MEW=
H526 NWXKVGR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXMTWM2OD1{MT62OEBvVQ>? M1X1WFI1OTZ4NUC1
N592 NWe5VoxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXjTWM2OD1zND6xNkBvVQ>? M3znfVI1OTZ4NUC1
H620 NULHeIl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDRTWM2OD1|Mj62O{BvVQ>? NF[2dWozPDF4NkWwOS=>
H792 NHzU[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3LfYh7UUN3ME20OU4xPyCwTR?= NVTDU5Z5OjRzNk[1NFU>
H1173 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF{Lk[yJI5O MnfoNlQyPjZ3MEW=
AC3 MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn20TWM2OD1{NT65JI5O NGf1NJIzPDF4NkWwOS=>
H82 MorFSpVv[3Srb36gRZN{[Xl? M36ybVMxKG6P NUTnelRbPzJiaB?= NF7vNmVqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M4HKNVI1OTZ4NUC1
GLC4 MmDESpVv[3Srb36gRZN{[Xl? MYGzNEBvVQ>? NI\UWlQ4OiCq MmO1bY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MX:yOFE3PjVyNR?=
H146  MVLGeY5kfGmxbjDBd5NigQ>? NFLI[W0{OCCwTR?= MY[3NkBp MlXZbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 M1\mOFI1OTZ4NUC1
OVCAR-5 MoTzR4VtdCCYaXHibYxqfHliQYPzZZk> MWSwMVExODBibl2= NXvYUpUxPzJiaB?= MWnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYjTO5A{OjN7MECxN|Y>
OVCAR-8 MYTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHv5TIQxNTFyMECgcm0> NIfnfpQ4OiCq MY\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M3PzTlI{QTByMUO2
A1847 MmD2R4VtdCCYaXHibYxqfHliQYPzZZk> NWq5c2hFOC1zMECwJI5O NYPze2hyPzJiaB?= NVXxbGVncW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4naUFI{QTByMUO2
SKOV-3 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGiyOHIxNTFyMECgcm0> M1faNFczKGh? M{D4d4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M4XYdFI{QTByMUO2
OVCAR-5 NGq0VFBCeG:ydH;zbZMhSXO|YYm= NYPx[osxOTBvMUCwJI5O MnTUNlQwPDhxN{KgbC=> NGjqU4FqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MojDNlM6ODBzM{[=
OVCAR-8 M32zOWFxd3C2b4Ppd{BCe3OjeR?= NYPy[XN2OTBvMUCwJI5O NVy1WWNKOjRxNEivO|IhcA>? MkjTbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NFPuXYIzOzlyMEGzOi=>
A1847 MkPTRZBweHSxc3nzJGF{e2G7 NHzjU3YyOC1zMECgcm0> M3vH[lI1NzR6L{eyJIg> MkLobY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NE\qSlczOzlyMEGzOi=>
H2228 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnT6NE0yODByIH7N MVm3NkBp M1\EN2lEPTB;MUOgcm0> MYGyN|U{OzJ4NR?=
H3122 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MojsNE0yODByIH7N NXy2U|JCPzJiaB?= M1OyfGlEPTB;MUCgcm0> MlXzNlM2OzN{NkW=
K008 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M13MOGlEPTB;NkCgcm0> NEDEXVMzOzRzOEWyNy=>
K028 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEPwe3dKSzVyPUi0JI5O NHrNVpQzOzRzOEWyNy=>
K029 NGLzVmpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHvWUlNKSzVyPUS2JI5O NF;aOGYzOzRzOEWyNy=>
M23 NIT3XYJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MY\JR|UxRTN5LkWgcm0> NU\pfZo6OjN2MUi1NlM>
K033 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH7pNHRKSzVyPUe1MlUhdk1? NGmwTlAzOzRzOEWyNy=>
K008 Mmn6SpVv[3Srb36gRZN{[Xl? MWeyOVAhdk1? Ml3rNlQhcA>? NEW3TINqdmS3Y3XzJGczKGG{cnXzeC=> NXLBNphmOjN2MUi1NlM>
K028 NFTifGRHfW6ldHnvckBCe3OjeR?= MmfLNlUxKG6P NH\McXozPCCq M1zZU4lv\HWlZYOgS|Ih[XK{ZYP0 M4TieFI{PDF6NUKz
K029 MYrGeY5kfGmxbjDBd5NigQ>? MYeyOVAhdk1? MoqzNlQhcA>? NYjlc45ncW6mdXPld{BIOSCjcoLld5Q> M3jYeFI{PDF6NUKz
M23 NH36[3NHfW6ldHnvckBCe3OjeR?= MVqyOVAhdk1? MViyOEBp MoDUbY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= NX3BeXVZOjN2MUi1NlM>
K033 NGS0b4lHfW6ldHnvckBCe3OjeR?= MWKyOVAhdk1? M{nveVI1KGh? MnXUbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w M1yxflI{PDF6NUKz
K008 MnPKRZBweHSxc3nzJGF{e2G7 NVzTc40xOTByIH7N MmXLO|IhcA>? NXrLR|dGe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MU[yN|QyQDV{Mx?=
K028 MWXBdI9xfG:|aYOgRZN{[Xl? M3v4fFExOCCwTR?= NFjDS4U4OiCq NHLWV4F{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NXnicFJNOjN2MUi1NlM>
K029 MVHBdI9xfG:|aYOgRZN{[Xl? NUnwXYN5OTByIH7N MXq3NkBp MYrzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M4ixNlI{PDF6NUKz
M23 NWGzfHNjSXCxcITvd4l{KEG|c3H5 MnfhNVAxKG6P NG\vW3A4OiCq MXXzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MVGyN|QyQDV{Mx?=
K033 MU\BdI9xfG:|aYOgRZN{[Xl? NV3PZWhKOTByIH7N M{ixV|czKGh? NYXZOYs{e2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NIny[ZQzOzRzOEWyNy=>
RD MlHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXaTWM2OD16IH7N M3T0TlI{OzB|N{Sx
Rh41 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;rcGlEPTB;MUCuOEBvVQ>? NX3YXGppOjN|MEO3OFE>
Rh18 M3L0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXaSZNDUUN3ME22MlIhdk1? MXmyN|MxOzd2MR?=
Rh30 NHzKeWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\ZTWM2OD13Lk[gcm0> NHXsNXUzOzNyM{e0NS=>
BT-12 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rUTWlEPTB;MUSuN{BvVQ>? MXOyN|MxOzd2MR?=
CHLA-266 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT1TWM2OD1{Nz6xJI5O NUHIbYViOjN|MEO3OFE>
TC-71 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTRwNTDuUS=> Mn;vNlM{ODN5NEG=
CHLA-9 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTRwNjDuUS=> MlPsNlM{ODN5NEG=
CHLA-10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fwWGlEPTB;NT63JI5O MWSyN|MxOzd2MR?=
CHLA-258 Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrTSVlKSzVyPU[uOEBvVQ>? MXOyN|MxOzd2MR?=
SJ-GBM2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF{Lkmgcm0> NWr5eGVlOjN|MEO3OFE>
NB-1643 NYDDcpVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS0fmRiUUN3ME23MlQhdk1? MkP4NlM{ODN5NEG=
NB-EBc1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fPfGlEPTB;MU[uPEBvVQ>? M{HKNVI{OzB|N{Sx
CHLA-90 M4qyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPQTWM2OD1{Mj6zJI5O M{LHO|I{OzB|N{Sx
CHLA-136 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr6fnhSUUN3ME2yN{4zKG6P MnvmNlM{ODN5NEG=
NALM-6 NED5U|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFzLkegcm0> Mn64NlM{ODN5NEG=
COG-LL-317 Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETvc2NKSzVyPUSuOEBvVQ>? NYPBZoc2OjN|MEO3OFE>
RS4;11 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHT[FNWUUN3ME2xN{42KG6P MV6yN|MxOzd2MR?=
MOLT-4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nMNWlEPTB;MUCuOkBvVQ>? M{W4WVI{OzB|N{Sx
CCRF-CEM (1) M4C5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF{LkWgcm0> NUO4SVVlOjN|MEO3OFE>
CCRF-CEM (2) NGL2SIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojaTWM2OD15LkKgcm0> NX\YbJNtOjN|MEO3OFE>
Kasumi-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHiSHdOUUN3ME21Mlghdk1? MYqyN|MxOzd2MR?=
Karpas-299 NHjVSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jMVWlEPTB;OT62JI5O NHfqToszOzNyM{e0NS=>
Ramos-RA1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT2TWM2OD15LkSgcm0> MYqyN|MxOzd2MR?=
LNCaP MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPaVmZZUUN3ME24JI5O MlLSNlMyPTJyMES=
VCaP MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDyTWM2OD15IH7N M2W0clI{OTV{MEC0
H1355 NGDz[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTVibl2= MW[yN|AyOjJ2OB?=
H157 NX\pT5Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjT[mJKSzVyPUegcm0> NVjmPVJROjNyMUKyOFg>
H460 MmfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRThibl2= NX3ZPG1WOjNyMUKyOFg>
IA-LM NXfXc3VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rVbGlEPTB;MUCgcm0> MlzUNlMxOTJ{NEi=
HOP-62 NWfNZ21mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTRTWM2OD1zMTDuUS=> M{TFbVI{ODF{MkS4
H23 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFzIH7N NIDMXpUzOzBzMkK0PC=>
H2030 NX32bnNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jES2lEPTB;MUKgcm0> MknTNlMxOTJ{NEi=
H441 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF2IH7N MXyyN|AyOjJ2OB?=
H2212 M1;NXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF5IH7N MkflNlMxOTJ{NEi=
SK-LU-1 NHzyeolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlGzTWM2OD1zODDuUS=> MoS0NlMxOTJ{NEi=
H2009 M2XsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[wR2xKSzVyPUG5JI5O NH\VdWgzOzBzMkK0PC=>
H1792 M{X5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C0T2lEPTB;MkCgcm0> NYHF[W1MOjNyMUKyOFg>
COR-L23 NESySphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJ{IH7N NI\FRXIzOzBzMkK0PC=>
H727 M{nqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPJSJBKSzVyPUK4JI5O NYTKT3pnOjNyMUKyOFg>
H1734 NFe1[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nkTGlEPTB;Mkigcm0> MV[yN|AyOjJ2OB?=
H358 NIDLe5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPVTWM2OD1{OTDuUS=> MVqyN|AyOjJ2OB?=
A549 NVzaWoc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTR|IH7N NFfXSJUzOzBzMkK0PC=>
H2122 MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLYSHlKSzVyPUWzJI5O MmnaNlMxOTJ{NEi=
Calu-1 NGLmO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTV6IH7N NEHhWGozOzBzMkK0PC=>
Calu-6 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTZ2IH7N MnLMNlMxOTJ{NEi=
NCI-H1975 NVnIZ2dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF34PVM1QCCq M3nGVWlEPTB;MU[gcm0> NXPERmJ[OjJzNES2OlU>
NCI-H1975 NV7TR3lNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXFb|FMPzJiaB?= NFvHbGtKSzVyPUigcm0> NUjRbo5mOjJzNES2OlU>

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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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

Dilution Calculator

Dilution Calculator

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

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

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

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Terminated Drug: Ziv-Aflibercept|Drug: Ganetespib Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 2 2014 Phase 1
NCT02008877 Completed Drug: ganetespib|Drug: Sirolimus Malignant Peripheral Nerve Sheath Tumors (MPNST)|Sarcoma Sarcoma Alliance for Research through Collaboration|Synta Pharmaceuticals Corp.|United States Department of Defense December 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Does this inhibitor inhibit both isoforms of HSP90?

  • Answer:

    We don't have the information now and it is not very clear in the literature either. From following two references, it indicates that Ganetespib might be specific to the alpha form “Ganetespib binds to the ATP binding site of Hsp90 alpha with a Kd of 110 nM” http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3477583/

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID