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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USD 370 In stock
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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 M3rFWWFxd3C2b4Ppd{BCe3OjeR?= MWOzNE85OC9zNUCvNlUxKG6P MUSyOE81QC95MjDo NILPOmRqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> M1zCOFI2QDh{NUWw
MV411 MWLBdI9xfG:|aYOgRZN{[Xl? Mn3JN|AwQDBxMUWwM|I2OCCwTR?= M{PYZlI1NzR6L{eyJIg> MnfqbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MnHSNlU5QDJ3NUC=
MGC-803 MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGribYkxNjFvMUCwNEBvVQ>? NEPMWlg4OiCq MX7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M1[yUVI2PTlyOEC1
SGC-7901 NXHPW4xPS2WubDDWbYFjcWyrdImgRZN{[Xl? NGSz[GExNjFvMUCwNEBvVQ>? NXLkfXJsPzJiaB?= M33OWIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHnSfWEzPTV7MEiwOS=>
MKN-28 NWHydHp4S2WubDDWbYFjcWyrdImgRZN{[Xl? MWqwMlEuOTByMDDuUS=> NEDtOWc4OiCq MWDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXv4VG5HOjV3OUC4NFU>
MGC-803 M{\4PGZ2dmO2aX;uJGF{e2G7 MVewMlEuOTByMDDuUS=> MWOyOEBp NWrVW3VncW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NUDKV|N7OjV3OUC4NFU>
HCT-116 NWC4eFM3TnWwY4Tpc44hSXO|YYm= MWK1NI5O NHXxUZkzPCCq NGTCWZVFVVOR NVXvVWVPcW6mdXPl[EBIOC:JMTDhdpJme3R? M2nVZVI2OjFyN{m0
HT-29 MkDNSpVv[3Srb36gRZN{[Xl? NWCzSoRRPTCwTR?= MWCyOEBp NXLNN|B4TE2VTx?= MX3pcoR2[2WmIFewM2cyKGG{cnXzeC=> M2DvcFI2OjFyN{m0
SCC25 NUC0OXJZS3m2b4jpZ4l1gSCDc4PhfS=> NGP2TYEyOC93MDDuUS=> MVeyOEBp MVnk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M2fyOFI2OjB3NEOw
FUDA NEPzSHhEgXSxeHnjbZR6KEG|c3H5 M3rjNVExNzVyIH7N MXmyOEBp MlzW[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MXmyOVIxPTR|MB?=
Detroit562 M1zMT2N6fG:6aXPpeJkhSXO|YYm= MljpNVAwPTBibl2= NYnscYlxOjRiaB?= NVXQZXNT\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M1PxVVI2OjB3NEOw
CAL27 MmDZR5l1d3irY3n0fUBCe3OjeR?= MX[xNE82OCCwTR?= NWjWbY1IOjRiaB?= M4nPeIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NYLHc2dzOjV{MEW0N|A>
DSH1 NWfrbZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\RZm8{UUN3ME22JI5O M1TE[VI1Pzh2OEO5
SW-1710 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[ybWlEPTB;NjDuUS=> Ml3nNlQ4QDR6M{m=
T24 NGT5cI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjEeVBKSzVyPUegcm0> M1LKRlI1Pzh2OEO5
RT112 NYHWW5k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LjdWlEPTB;OTDuUS=> MoG0NlQ4QDR6M{m=
639-V MkTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zwWmlEPTB;MUCgcm0> MXWyOFc5PDh|OR?=
SCaBER NVKwWZFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT6cpRjUUN3ME2xNEBvVQ>? M4jLNlI1Pzh2OEO5
BFTC M{jIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF5IH7N NEHiXlgzPDd6NEizPS=>
J82 NEOxcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTF6IH7N MWSyOFc5PDh|OR?=
HT-1376 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXEW|RKSzVyPUKxJI5O NHW4RmYzPDd6NEizPS=>
647-V MlnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\nTWM2OD1{NzDuUS=> M2O4elI1Pzh2OEO5
UM-UC3 NGjaR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvkd2lyUUN3ME2zN{BvVQ>? NHzMc2MzPDd6NEizPS=>
LB831-BLC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvlWWJ3UUN3ME2zOEBvVQ>? NYDYeGMxOjR5OES4N|k>
KU-19-19 Mlm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXpd5lKSzVyPUO2JI5O NIPvcXczPDd6NEizPS=>
35612 NYq5PWNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzTd5dKSzVyPUO4JI5O MnvKNlQ4QDR6M{m=
5637 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO5XmpKSzVyPUS0JI5O MWOyOFc5PDh|OR?=
HT-1197 M13aW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXaTWM2OD13MzDuUS=> NYHOU|NyOjR5OES4N|k>
MGH-U3 M3vaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS4R2lxUUN3ME21N{BvVQ>? MnfuNlQ4QDR6M{m=
TCCSUP NFK0c3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\KTGlEPTB;MUSyJI5O MXuyOFc5PDh|OR?=
RT4 NXOwZWd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF5M{Ogcm0> MlPnNlQ4QDR6M{m=
SW780 NGfyU2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN2NUGgcm0> MUiyOFc5PDh|OR?=
RKO MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW2eYRDUUN3ME20JI5O NFLBN5AzPDZ6Mke0Oy=>
LS-411 N MmD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\oTWM2OD13IH7N MkHLNlQ3QDJ5NEe=
SW620 M{jQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrWRlZKSzVyPUigcm0> NV7odXJnOjR4OEK3OFc>
HCT-15 MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzhOFA4UUN3ME24JI5O NFHpZ|gzPDZ6Mke0Oy=>
HuTu-80 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF|IH7N M4n6eVI1Pjh{N{S3
HCT 116 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLPTWM2OD1zNDDuUS=> NGLPWXEzPDZ6Mke0Oy=>
COLO-205 M4DZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\O[2hKSzVyPUG0JI5O M2GzOFI1Pjh{N{S3
NCI-H747 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF5IH7N MmPSNlQ3QDJ5NEe=
COLO-678 M{jLfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrEdZpWUUN3ME2yNUBvVQ>? NFzxWGUzPDZ6Mke0Oy=>
LoVo NHy5eW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\EVGlEPTB;MkKgcm0> Mof1NlQ3QDJ5NEe=
LS-1034 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjxcG1lUUN3ME2zNUBvVQ>? NHfBWoUzPDZ6Mke0Oy=>
SNU-C2B NXTndZhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTR3IH7N NVGyZoV5OjR4OEK3OFc>
LS-123 MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrEWJNTUUN3ME23N{BvVQ>? NYHjbHlDOjR4OEK3OFc>
SK-CO-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HX[mlEPTB;OEGgcm0> MoGxNlQ3QDJ5NEe=
HCC2998 NITR[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Xqd2lEPTB;MUK4JI5O NX;5Ro0{OjR4OEK3OFc>
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? NF;0[lAyODBibl2= M4XOVlMxKG2rbh?= MkfSbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NG\wdpEzPDJ2OEK2OS=>
MDA-MB-435 NF7Zb5RHfW6ldHnvckBCe3OjeR?= MlXQNVAxKG6P MmjGN|AhdWmw NWnrUpRkcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NUfVdYxGOjR{NEiyOlU>
BT-20  NFnJW4ZHfW6ldHnvckBCe3OjeR?= MVWxNFAwOjVyIH7N NXnGW|E6OjRiaB?= MUjy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> MluyNlQyPzN3NEG=
MDA-MB-231 NVvZe415TnWwY4Tpc44hSXO|YYm= NEL5TmgyODBibl2= Mm\0NlQhcA>? M3rh[YlvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> MVyyOFE4OzV2MR?=
H82 M3Oyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPVVGVKSzVyPUOwMlI4KG6P Mn3VNlQyPjZ3MEW=
GLC4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33oOmlEPTB;MkCuOFchdk1? M{S0dlI1OTZ4NUC1
H69 NEPNTnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojWTWM2OD16Mz6zOkBvVQ>? MmDMNlQyPjZ3MEW=
H128 NYnkWoVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTZ7LkW1JI5O NWG5dJJsOjRzNk[1NFU>
H146 M{GxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzucYZKSzVyPUK4MlUyKG6P NYfPZ45WOjRzNk[1NFU>
H187 NWn2b3J[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3IXXVZUUN3ME2yOE46QSCwTR?= NEfVOo4zPDF4NkWwOS=>
H526 NGLPcYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[4fmlEPTB;MkGuOlQhdk1? MmOwNlQyPjZ3MEW=
N592 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTNTWM2OD1zND6xNkBvVQ>? MnLTNlQyPjZ3MEW=
H620 Mnq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:yenZrUUN3ME2zNk43PyCwTR?= MYCyOFE3PjVyNR?=
H792 NHrUO2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LaR2lEPTB;NEWuNFchdk1? MVGyOFE3PjVyNR?=
H1173 Ml3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF{Lk[yJI5O MXSyOFE3PjVyNR?=
AC3 M2fFWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLiT2JKSzVyPUK1Mlkhdk1? NFXPdVMzPDF4NkWwOS=>
H82 NU\abJRoTnWwY4Tpc44hSXO|YYm= NVnMOGhVOzBibl2= MnuyO|IhcA>? MWTpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NVnUTHNzOjRzNk[1NFU>
GLC4 NHi0[VRHfW6ldHnvckBCe3OjeR?= MWezNEBvVQ>? MVi3NkBp NEjIcZNqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NHn0dFUzPDF4NkWwOS=>
H146  NXvCfYRbTnWwY4Tpc44hSXO|YYm= NILiV2I{OCCwTR?= MV63NkBp MkCxbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NGrseoozPDF4NkWwOS=>
OVCAR-5 M1XaSGNmdGxiVnnhZoltcXS7IFHzd4F6 NYnzeWk4OC1zMECwJI5O MlvGO|IhcA>? M1;ES4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MWGyN|kxODF|Nh?=
OVCAR-8 NWrCRWF7S2WubDDWbYFjcWyrdImgRZN{[Xl? MV2wMVExODBibl2= M33ucFczKGh? MnznbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NHi0VGMzOzlyMEGzOi=>
A1847 M2jTe2NmdGxiVnnhZoltcXS7IFHzd4F6 MUSwMVExODBibl2= NUTreYJYPzJiaB?= MlXqbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NICwPW0zOzlyMEGzOi=>
SKOV-3 NYH3O2k5S2WubDDWbYFjcWyrdImgRZN{[Xl? NGf6fncxNTFyMECgcm0> Ml\UO|IhcA>? M{PNW4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NVX2NIR7OjN7MECxN|Y>
OVCAR-5 MYXBdI9xfG:|aYOgRZN{[Xl? Mnm2NVAuOTByIH7N NHXYb|EzPC92OD:3NkBp MmPjbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NFXZW2QzOzlyMEGzOi=>
OVCAR-8 MVnBdI9xfG:|aYOgRZN{[Xl? M3j2ZVExNTFyMDDuUS=> MoTENlQwPDhxN{KgbC=> NUG3ZmhTcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MXSyN|kxODF|Nh?=
A1847 MUTBdI9xfG:|aYOgRZN{[Xl? MoHBNVAuOTByIH7N M4KzNlI1NzR6L{eyJIg> MlrXbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NV7nUpJlOjN7MECxN|Y>
H2228 MljBR4VtdCCYaXHibYxqfHliQYPzZZk> MlT2NE0yODByIH7N NFrQVWo4OiCq MX;JR|UxRTF|IH7N MYOyN|U{OzJ4NR?=
H3122 M1jI[mNmdGxiVnnhZoltcXS7IFHzd4F6 MWqwMVExODBibl2= NVPiNWJGPzJiaB?= NHnNcmNKSzVyPUGwJI5O NGjTT3YzOzV|M{K2OS=>
K008 NELwdHZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX\JR|UxRTZyIH7N NX;QbYtrOjN2MUi1NlM>
K028 NICx[YFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYnJR|UxRTh2IH7N NIraWIMzOzRzOEWyNy=>
K029 MmXiR4VtdCCYaXHibYxqfHliQYPzZZk> MXzJR|UxRTR4IH7N NHHkdYozOzRzOEWyNy=>
M23 M1zt[GNmdGxiVnnhZoltcXS7IFHzd4F6 M{H5VWlEPTB;M{euOUBvVQ>? MXmyN|QyQDV{Mx?=
K033 NGHQcnZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4nBXGlEPTB;N{WuOUBvVQ>? Mlv3NlM1OTh3MkO=
K008 NIjKWldHfW6ldHnvckBCe3OjeR?= MWqyOVAhdk1? MkL2NlQhcA>? MUHpcoR2[2W|IFeyJIFzemW|dB?= NYD3UZdQOjN2MUi1NlM>
K028 NHnZfo5HfW6ldHnvckBCe3OjeR?= MYCyOVAhdk1? MYiyOEBp NFPOcFJqdmS3Y3XzJGczKGG{cnXzeC=> M1fic|I{PDF6NUKz
K029 MmTISpVv[3Srb36gRZN{[Xl? M1q1XFI2OCCwTR?= MWOyOEBp MYrpcoR2[2W|IFexJIFzemW|dB?= MUGyN|QyQDV{Mx?=
M23 MoTUSpVv[3Srb36gRZN{[Xl? MoixNlUxKG6P NH3a[44zPCCq Ml2xbY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= NWnNfo1tOjN2MUi1NlM>
K033 NU[zcXhtTnWwY4Tpc44hSXO|YYm= NXXBOJhzOjVyIH7N M2rXNlI1KGh? M{HWNolv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= NYjqOHZpOjN2MUi1NlM>
K008 MmLPRZBweHSxc3nzJGF{e2G7 NEHyWGEyODBibl2= NIrTeYs4OiCq MnXud4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NF\aVJQzOzRzOEWyNy=>
K028 NHTJT5hCeG:ydH;zbZMhSXO|YYm= M1q4T|ExOCCwTR?= MVi3NkBp NHfCdmJ{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| Mn7mNlM1OTh3MkO=
K029 MnrmRZBweHSxc3nzJGF{e2G7 NYC5dIFNOTByIH7N MYG3NkBp MX3zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M2joT|I{PDF6NUKz
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CHLA-9 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OwOWlEPTB;ND62JI5O Mn;1NlM{ODN5NEG=
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NB-EBc1 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPEfVFSUUN3ME2xOk45KG6P M1;iOlI{OzB|N{Sx
CHLA-90 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJ{LkOgcm0> M2rQRVI{OzB|N{Sx
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NALM-6 NIfLVWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorCTWM2OD1zMT63JI5O MnHYNlM{ODN5NEG=
COG-LL-317 NIXPfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTRwNDDuUS=> NUeyeoFOOjN|MEO3OFE>
RS4;11 NXn2fVFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXoNHRiUUN3ME2xN{42KG6P NEewc44zOzNyM{e0NS=>
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Kasumi-1 NGDV[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDQOI1KSzVyPUWuPEBvVQ>? M2jpTFI{OzB|N{Sx
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H157 M3uxZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTdibl2= MUSyN|AyOjJ2OB?=
H460 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3njTGlEPTB;ODDuUS=> Ml74NlMxOTJ{NEi=
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HOP-62 M3vLfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFzIH7N NH\sS4EzOzBzMkK0PC=>
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H1792 NH\iUYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPiNXcyUUN3ME2yNEBvVQ>? MlvmNlMxOTJ{NEi=
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H2122 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLZW3lvUUN3ME21N{BvVQ>? NGLZOWczOzBzMkK0PC=>
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NCI-H1975 NI[wT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\PdFczKGh? MULJR|UxRThibl2= NH\QPGEzOjF2NE[2OS=>

... 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:
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
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

  • Serial Dilutions

  • Computed Result

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    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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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 Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Completed Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 9, 2014 Phase 1
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 --
NCT02389751 Active, not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. April 2015 Phase 1
NCT02334319 Terminated Stage I Hypopharyngeal Squamous Cell Carcinoma|Stage I Laryngeal Squamous Cell Carcinoma|Stage I Oral Cavity Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma|Stage II Hypopharyngeal Squamous Cell Carcinoma|Stage II Laryngeal Squamous Cell Carcinoma|Stage II Oral Cavity Squamous Cell Carcinoma|Stage II Oropharyngeal Squamous Cell Carcinoma|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma Emory University|Synta Pharmaceuticals Corp. December 2014 Phase 1
NCT02261805 Terminated Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 Phase 1|Phase 2
NCT02272478 Recruiting Acute Myeloid Leukaemia|Myelodysplastic Syndrome Cardiff University|Cancer Research UK October 2014 Phase 3

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID