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
USD 270 In stock
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 MXjBdI9xfG:|aYOgRZN{[Xl? M3ft[FMxNzhyL{G1NE8zPTBibl2= Mnq4NlQwPDhxN{KgbC=> NI\V[oZqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NYjuZ|NzOjV6OEK1OVA>
MV411 MXjBdI9xfG:|aYOgRZN{[Xl? NWrPSJU3OzBxOECvNVUxNzJ3MDDuUS=> NXzaWo5FOjRxNEivO|IhcA>? M1jJbIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NIXwfGQzPTh6MkW1NC=>
MGC-803 MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXPhdml7OC5zLUGwNFAhdk1? NYHWXnhDPzJiaB?= NXHYRZRwcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NUnIWG1jOjV3OUC4NFU>
SGC-7901 NFToUJBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmX1NE4yNTFyMECgcm0> Ml7MO|IhcA>? MkiybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NE\Bd20zPTV7MEiwOS=>
MKN-28 M2rlb2NmdGxiVnnhZoltcXS7IFHzd4F6 NVHJfYp2OC5zLUGwNFAhdk1? NIXUVJM4OiCq MUXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NVrrXYxUOjV3OUC4NFU>
MGC-803 NWK4eoM1TnWwY4Tpc44hSXO|YYm= M3K5fFAvOS1zMECwJI5O Mkf6NlQhcA>? NF;5dZlqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? M{nBeVI2PTlyOEC1
HCT-116 NHnzSWxHfW6ldHnvckBCe3OjeR?= M1XoPVUxdk1? NVmwcY1QOjRiaB?= MkPYSG1UVw>? Ml;ibY5lfWOnZDDHNE9IOSCjcoLld5Q> NVizSYxROjV{MUC3PVQ>
HT-29 M{fheWZ2dmO2aX;uJGF{e2G7 MXO1NI5O M4PZWFI1KGh? M2qzWWROW09? MkC4bY5lfWOnZDDHNE9IOSCjcoLld5Q> NU\YUI5yOjV{MUC3PVQ>
SCC25 NWPNfpl4S3m2b4jpZ4l1gSCDc4PhfS=> NFKzNIoyOC93MDDuUS=> M4HtPFI1KGh? MV3k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MVeyOVIxPTR|MB?=
FUDA NVXXTVV{S3m2b4jpZ4l1gSCDc4PhfS=> M2fNRVExNzVyIH7N NHiwb3IzPCCq M1jMcoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NW\2Sms6OjV{MEW0N|A>
Detroit562 NXTjXZZwS3m2b4jpZ4l1gSCDc4PhfS=> MUixNE82OCCwTR?= M2XmbVI1KGh? MXjk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NH;FTHAzPTJyNUSzNC=>
CAL27 MXHDfZRwgGmlaYT5JGF{e2G7 MoHJNVAwPTBibl2= NHHFS3EzPCCq MYHk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MXSyOVIxPTR|MB?=
DSH1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkixTWM2OD14IH7N M4DWUlI1Pzh2OEO5
SW-1710 MmrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nwTWlEPTB;NjDuUS=> M4\2UlI1Pzh2OEO5
T24 MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzjTWM2OD15IH7N NEDlZVUzPDd6NEizPS=>
RT112 NWjpbZFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7jTWM2OD17IH7N NV;t[pVzOjR5OES4N|k>
639-V NGGzVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm4NnJKSzVyPUGwJI5O MWWyOFc5PDh|OR?=
SCaBER NILWUI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PMdWlEPTB;MUCgcm0> NV;IV2F[OjR5OES4N|k>
BFTC MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TmSGlEPTB;MUegcm0> MX[yOFc5PDh|OR?=
J82 NYruUJRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PlTGlEPTB;MUigcm0> M{G0elI1Pzh2OEO5
HT-1376 MofHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJzIH7N M1LBUFI1Pzh2OEO5
647-V M171NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLsTWM2OD1{NzDuUS=> NXzURpg5OjR5OES4N|k>
UM-UC3 NYHVXYxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke5TWM2OD1|MzDuUS=> MVSyOFc5PDh|OR?=
LB831-BLC NEn1bHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln2TWM2OD1|NDDuUS=> MYqyOFc5PDh|OR?=
KU-19-19 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvlTWM2OD1|NjDuUS=> NGnPO2MzPDd6NEizPS=>
35612 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzCTWM2OD1|ODDuUS=> M1\2eVI1Pzh2OEO5
5637 M{TxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnWTWM2OD12NDDuUS=> MU[yOFc5PDh|OR?=
HT-1197 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTV|IH7N MUSyOFc5PDh|OR?=
MGH-U3 M4KzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vNOWlEPTB;NUOgcm0> M1XaOVI1Pzh2OEO5
TCCSUP MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi0SZlqUUN3ME2xOFIhdk1? M2SzblI1Pzh2OEO5
RT4 NWDWO3FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DvNWlEPTB;MUezN{BvVQ>? NVX6RpJOOjR5OES4N|k>
SW780 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTGTWM2OD1|NEWxJI5O NUKwbI8{OjR5OES4N|k>
RKO NVPi[Fl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTRibl2= NYq3SFV6OjR4OEK3OFc>
LS-411 N MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTVibl2= MUOyOFY5Ojd2Nx?=
SW620 NHfnTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7UdnJoUUN3ME24JI5O NUPGb41sOjR4OEK3OFc>
HCT-15 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\iO3VPUUN3ME24JI5O NV72V|hCOjR4OEK3OFc>
HuTu-80 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnPfpViUUN3ME2xN{BvVQ>? MV:yOFY5Ojd2Nx?=
HCT 116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTBflNZUUN3ME2xOEBvVQ>? NYTVXog1OjR4OEK3OFc>
COLO-205 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF2IH7N MlLoNlQ3QDJ5NEe=
NCI-H747 MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfWZW5KSzVyPUG3JI5O MnPuNlQ3QDJ5NEe=
COLO-678 NHr0dW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfiTWM2OD1{MTDuUS=> M3v1NVI1Pjh{N{S3
LoVo MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjUflNnUUN3ME2yNkBvVQ>? M1rZb|I1Pjh{N{S3
LS-1034 NXzIPWFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPJTY46UUN3ME2zNUBvVQ>? M{jhfFI1Pjh{N{S3
SNU-C2B MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13rSWlEPTB;NEWgcm0> M1jT[lI1Pjh{N{S3
LS-123 M1TRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorITWM2OD15MzDuUS=> M1LnZVI1Pjh{N{S3
SK-CO-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX4TWM2OD16MTDuUS=> NXG4[FZPOjR4OEK3OFc>
HCC2998 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLDTWM2OD1zMkigcm0> NUHjVmR[OjR4OEK3OFc>
MDA-MB-231 M1LyRWZ2dmO2aX;uJGF{e2G7 NGjB[XkyODBibl2= Mly4N|AhdWmw NWrDXGw{cW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MmPiNlQzPDh{NkW=
MDA-MB-435 MY\GeY5kfGmxbjDBd5NigQ>? MlraNVAxKG6P MVyzNEBucW5? MoOybY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? M4fRT|I1OjR6Mk[1
BT-20  MnfZSpVv[3Srb36gRZN{[Xl? M4r4blExOC9{NUCgcm0> MlHYNlQhcA>? NHvHZ4xz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? NHvJO2wzPDF5M{W0NS=>
MDA-MB-231 M4n2cmZ2dmO2aX;uJGF{e2G7 NUjKb25WOTByIH7N NHL6T3YzPCCq NVjtV49LcW6qaXLpeJMhfGinIH3p[5JifG:{eTDhcoQhcW64YYPpeoUh[2GyYXPpeJnDqA>? NUjRb2hHOjRzN{O1OFE>
H82 NIK4TYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVeyZ5NKUUN3ME2zNE4zPyCwTR?= NHroTGEzPDF4NkWwOS=>
GLC4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfjPFVKSzVyPUKwMlQ4KG6P NEj4VW0zPDF4NkWwOS=>
H69 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLLTWM2OD16Mz6zOkBvVQ>? NXuwbGlwOjRzNk[1NFU>
H128 M3HOUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjUPXhKSzVyPU[5MlU2KG6P M{HNWVI1OTZ4NUC1
H146 NHLwUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4mzSWlEPTB;MkiuOVEhdk1? MmX2NlQyPjZ3MEW=
H187 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfnZolVUUN3ME2yOE46QSCwTR?= Mn\wNlQyPjZ3MEW=
H526 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\1bGlEPTB;MkGuOlQhdk1? M4rCfVI1OTZ4NUC1
N592 NV63SXJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvBWGM{UUN3ME2xOE4yOiCwTR?= MWqyOFE3PjVyNR?=
H620 MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWxUnpKSzVyPUOyMlY4KG6P NIPJTokzPDF4NkWwOS=>
H792 MkfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHVTWM2OD12NT6wO{BvVQ>? Mle5NlQyPjZ3MEW=
H1173 NFjGSY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLsbFFKSzVyPUGyMlYzKG6P NFntR5gzPDF4NkWwOS=>
AC3 NEe5eJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTJ3Lkmgcm0> MmrCNlQyPjZ3MEW=
H82 Ml;YSpVv[3Srb36gRZN{[Xl? NUX3PGh6OzBibl2= MYm3NkBp NUfPfIhCcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M1u0eFI1OTZ4NUC1
GLC4 M363dWZ2dmO2aX;uJGF{e2G7 MlnuN|Ahdk1? Mnj4O|IhcA>? NFPZTHhqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NUHrT3FxOjRzNk[1NFU>
H146  M{faOWZ2dmO2aX;uJGF{e2G7 M4\GcFMxKG6P NYjDSHlqPzJiaB?= NFTCbJpqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M1OyNFI1OTZ4NUC1
OVCAR-5 MljJR4VtdCCYaXHibYxqfHliQYPzZZk> NF3KWJQxNTFyMECgcm0> NFzCS2M4OiCq NYGySIpVcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVnte|B5OjN7MECxN|Y>
OVCAR-8 Mn35R4VtdCCYaXHibYxqfHliQYPzZZk> MmPONE0yODByIH7N MmnlO|IhcA>? NEHBVIhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlvjNlM6ODBzM{[=
A1847 MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{HhO|AuOTByMDDuUS=> M1GzUVczKGh? M{HRe4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MXmyN|kxODF|Nh?=
SKOV-3 NX[z[YhMS2WubDDWbYFjcWyrdImgRZN{[Xl? MUewMVExODBibl2= MmHGO|IhcA>? MYrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MVOyN|kxODF|Nh?=
OVCAR-5 NIT6WpNCeG:ydH;zbZMhSXO|YYm= NH7tcFQyOC1zMECgcm0> MUGyOE81QC95MjDo MomzbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MYCyN|kxODF|Nh?=
OVCAR-8 NEnHVm9CeG:ydH;zbZMhSXO|YYm= MXixNE0yODBibl2= NHTFS2wzPC92OD:3NkBp NVXXRVFEcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M{fafVI{QTByMUO2
A1847 MWPBdI9xfG:|aYOgRZN{[Xl? Ml3VNVAuOTByIH7N MYmyOE81QC95MjDo NULLe5JJcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyN|kxODF|Nh?=
H2228 NGTtWoVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn[0NE0yODByIH7N NEL1VmE4OiCq NYjIZWF[UUN3ME2xN{BvVQ>? NE\FOFIzOzV|M{K2OS=>
H3122 M1fWR2NmdGxiVnnhZoltcXS7IFHzd4F6 M3G0W|AuOTByMDDuUS=> M{PKV|czKGh? M4XYb2lEPTB;MUCgcm0> MmDvNlM2OzN{NkW=
K008 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVzJR|UxRTZyIH7N NUO1TodKOjN2MUi1NlM>
K028 NU\6bVBlS2WubDDWbYFjcWyrdImgRZN{[Xl? NUD5cXBYUUN3ME24OEBvVQ>? NF3sblYzOzRzOEWyNy=>
K029 NXTjcFNLS2WubDDWbYFjcWyrdImgRZN{[Xl? MojZTWM2OD12NjDuUS=> MU[yN|QyQDV{Mx?=
M23 NFfYWIpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHTHdJVKSzVyPUO3MlUhdk1? MWiyN|QyQDV{Mx?=
K033 NV\jfWRuS2WubDDWbYFjcWyrdImgRZN{[Xl? Mly5TWM2OD15NT61JI5O MX2yN|QyQDV{Mx?=
K008 NHjQTVdHfW6ldHnvckBCe3OjeR?= Mn\qNlUxKG6P M2TGb|I1KGh? MmHxbY5lfWOnczDHNkBienKnc4S= M4HmOFI{PDF6NUKz
K028 M2\RRWZ2dmO2aX;uJGF{e2G7 NFz4RmYzPTBibl2= NGW5No0zPCCq M3\kcYlv\HWlZYOgS|Ih[XK{ZYP0 MkO5NlM1OTh3MkO=
K029 MWfGeY5kfGmxbjDBd5NigQ>? NGTyRoIzPTBibl2= M{H5eFI1KGh? NYXRVoZbcW6mdXPld{BIOSCjcoLld5Q> MnzVNlM1OTh3MkO=
M23 M1XDNGZ2dmO2aX;uJGF{e2G7 MXiyOVAhdk1? M3rvOFI1KGh? Mm\6bY5lfWOnczDHNUBidmRiR{KvUUBienKnc4S= NHvZW3UzOzRzOEWyNy=>
K033 MkWzSpVv[3Srb36gRZN{[Xl? MUmyOVAhdk1? NHrXNlgzPCCq MlSxbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NWPZO5kxOjN2MUi1NlM>
K008 MXrBdI9xfG:|aYOgRZN{[Xl? MlnlNVAxKG6P MVy3NkBp M2n3XJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NFHrd3YzOzRzOEWyNy=>
K028 MmryRZBweHSxc3nzJGF{e2G7 M{G1XlExOCCwTR?= NE[4XnE4OiCq NUnQPYJne2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= MXmyN|QyQDV{Mx?=
K029 NWLtfI9ESXCxcITvd4l{KEG|c3H5 MX:xNFAhdk1? MWm3NkBp M{nsXZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NFOwT2IzOzRzOEWyNy=>
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CHLA-136 NGLuZ3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJ|LkKgcm0> M1H2fVI{OzB|N{Sx
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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 individually and in order:
5% DMSO+45% PEG 300+ddH2O
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).

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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:

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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.

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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 (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