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
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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 Mo[3RZBweHSxc3nzJGF{e2G7 MoH4N|AwQDBxMUWwM|I2OCCwTR?= NVrmOXBbOjRxNEivO|IhcA>? NH:5PGdqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NX\vTZRLOjV6OEK1OVA>
MV411 NFHuSnZCeG:ydH;zbZMhSXO|YYm= Ml61N|AwQDBxMUWwM|I2OCCwTR?= M2XaSFI1NzR6L{eyJIg> NVu3RlV2cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ M4rkOFI2QDh{NUWw
MGC-803 NH\Nb4RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFToVpYxNjFvMUCwNEBvVQ>? NX3aeYxuPzJiaB?= NY\EfnB{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWeyOVU6ODhyNR?=
SGC-7901 NETXO3pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1TweFAvOS1zMECwJI5O MmXQO|IhcA>? NGK0OGZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M{nxeVI2PTlyOEC1
MKN-28 MofSR4VtdCCYaXHibYxqfHliQYPzZZk> MVWwMlEuOTByMDDuUS=> M{Hi[VczKGh? NV;Wd21wcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnLUNlU2QTB6MEW=
MGC-803 MlrISpVv[3Srb36gRZN{[Xl? M4DqUFAvOS1zMECwJI5O NWL6Z2EzOjRiaB?= MoHjbY5lfWOnczDHNk9OKGOnbHytZ5lkdGViYYLy[ZN1 NITPfFAzPTV7MEiwOS=>
HCT-116 NXHXeHNoTnWwY4Tpc44hSXO|YYm= MXy1NI5O Mn7vNlQhcA>? NG\RV3hFVVOR Mlv0bY5lfWOnZDDHNE9IOSCjcoLld5Q> M4PzXVI2OjFyN{m0
HT-29 MXvGeY5kfGmxbjDBd5NigQ>? M3rOZ|Uxdk1? M4TMc|I1KGh? MULEUXNQ MnHibY5lfWOnZDDHNE9IOSCjcoLld5Q> M1nIZ|I2OjFyN{m0
SCC25 NHWx[3NEgXSxeHnjbZR6KEG|c3H5 NEO0cmsyOC93MDDuUS=> MV6yOEBp NGfYOoRl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MXmyOVIxPTR|MB?=
FUDA M3HER2N6fG:6aXPpeJkhSXO|YYm= NV64WFFJOTBxNUCgcm0> M3vJTFI1KGh? NYHtb3RD\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M1PlflI2OjB3NEOw
Detroit562 NH31OnZEgXSxeHnjbZR6KEG|c3H5 NVLoPIRTOTBxNUCgcm0> NHz0T4szPCCq M3jIfoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NGXJNogzPTJyNUSzNC=>
CAL27 NEfR[5dEgXSxeHnjbZR6KEG|c3H5 MmHDNVAwPTBibl2= NV\mVVRROjRiaB?= NV74WVVo\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NYHoVY9xOjV{MEW0N|A>
DSH1 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jlO2lEPTB;NjDuUS=> MXiyOFc5PDh|OR?=
SW-1710 NIS5SotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j2RWlEPTB;NjDuUS=> NGDmOHYzPDd6NEizPS=>
T24 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjaOYluUUN3ME23JI5O MWiyOFc5PDh|OR?=
RT112 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnnN3VZUUN3ME25JI5O MlnvNlQ4QDR6M{m=
639-V M{nvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXMPG9KSzVyPUGwJI5O MX:yOFc5PDh|OR?=
SCaBER M1Lid2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Hjc2lEPTB;MUCgcm0> MU[yOFc5PDh|OR?=
BFTC M{DsUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfOTWM2OD1zNzDuUS=> NIPqTpEzPDd6NEizPS=>
J82 MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF6IH7N MW[yOFc5PDh|OR?=
HT-1376 NV;yPWd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXabnF4UUN3ME2yNUBvVQ>? NH3sXJczPDd6NEizPS=>
647-V MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vNeWlEPTB;Mkegcm0> M1rLd|I1Pzh2OEO5
UM-UC3 NITUWnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnsOm9HUUN3ME2zN{BvVQ>? MVWyOFc5PDh|OR?=
LB831-BLC MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjrTWM2OD1|NDDuUS=> M4npXFI1Pzh2OEO5
KU-19-19 MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[wTWM2OD1|NjDuUS=> MkPXNlQ4QDR6M{m=
35612 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv4OnhTUUN3ME2zPEBvVQ>? NYjveYltOjR5OES4N|k>
5637 M4DjUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rQUGlEPTB;NESgcm0> MUeyOFc5PDh|OR?=
HT-1197 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7vTWM2OD13MzDuUS=> MVuyOFc5PDh|OR?=
MGH-U3 NUPZSpVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXSTWM2OD13MzDuUS=> NG\WU4szPDd6NEizPS=>
TCCSUP NEWz[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3LUGJKSzVyPUG0NkBvVQ>? NEPkVY8zPDd6NEizPS=>
RT4 M{HiZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrqZ3oyUUN3ME2xO|M{KG6P M3TxdlI1Pzh2OEO5
SW780 M4HFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW3TWM2OD1|NEWxJI5O M4nhZ|I1Pzh2OEO5
RKO MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[4TWM2OD12IH7N Mn\mNlQ3QDJ5NEe=
LS-411 N MkmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTtTWM2OD13IH7N MmfVNlQ3QDJ5NEe=
SW620 NI[yPZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jsdmlEPTB;ODDuUS=> MkHnNlQ3QDJ5NEe=
HCT-15 M3\P[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnYTWM2OD16IH7N NULOWVZPOjR4OEK3OFc>
HuTu-80 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTF|IH7N MXeyOFY5Ojd2Nx?=
HCT 116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonwTWM2OD1zNDDuUS=> NHrYZZUzPDZ6Mke0Oy=>
COLO-205 NGjFcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIj3cpFKSzVyPUG0JI5O NGT6TJEzPDZ6Mke0Oy=>
NCI-H747 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPLcYJKSzVyPUG3JI5O MnfmNlQ3QDJ5NEe=
COLO-678 NHLTVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPIZVVKSzVyPUKxJI5O MlXVNlQ3QDJ5NEe=
LoVo M{fGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ{IH7N NFLuU40zPDZ6Mke0Oy=>
LS-1034 MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7TTWM2OD1|MTDuUS=> NX33cIhmOjR4OEK3OFc>
SNU-C2B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXriOFVkUUN3ME20OUBvVQ>? NYi1fIhVOjR4OEK3OFc>
LS-123 NUTkOIg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;H[lZKSzVyPUezJI5O MVGyOFY5Ojd2Nx?=
SK-CO-1 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRThzIH7N NILTcHEzPDZ6Mke0Oy=>
HCC2998 NUn3T5lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF{ODDuUS=> NVL2O3hxOjR4OEK3OFc>
MDA-MB-231 MmDMSpVv[3Srb36gRZN{[Xl? NVThZ49GOTByIH7N NEG1e|E{OCCvaX6= M{CzUIlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MX2yOFI1QDJ4NR?=
MDA-MB-435 M3PZdGZ2dmO2aX;uJGF{e2G7 NIr6W|kyODBibl2= Mkj2N|AhdWmw NIXOWGpqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= M1m2RlI1OjR6Mk[1
BT-20  NVTobVF1TnWwY4Tpc44hSXO|YYm= M1uyR|ExOC9{NUCgcm0> NF7tU5kzPCCq MUXy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> MYOyOFE4OzV2MR?=
MDA-MB-231 MlfJSpVv[3Srb36gRZN{[Xl? NYTkNolxOTByIH7N NIq4UoszPCCq MnzobY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> M{XtN|I1OTd|NUSx
H82 NIHWUWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojXTWM2OD1|MD6yO{BvVQ>? MXiyOFE3PjVyNR?=
GLC4 M2H5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3zTWM2OD1{MD60O{BvVQ>? NFXnb|czPDF4NkWwOS=>
H69 M2e3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTh|LkO2JI5O NYCwWFFROjRzNk[1NFU>
H128 MlzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZ7LkW1JI5O MorGNlQyPjZ3MEW=
H146 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn1TWM2OD1{OD61NUBvVQ>? M2i1fFI1OTZ4NUC1
H187 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLPcYhKSzVyPUK0Mlk6KG6P MXeyOFE3PjVyNR?=
H526 NVHiOJI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJzLk[0JI5O MX6yOFE3PjVyNR?=
N592 NWTaTJRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;2TWM2OD1zND6xNkBvVQ>? MoLSNlQyPjZ3MEW=
H620 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTN{Lk[3JI5O NYnrdYZ5OjRzNk[1NFU>
H792 MmXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR3LkC3JI5O MVeyOFE3PjVyNR?=
H1173 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rYOWlEPTB;MUKuOlIhdk1? NX7NZ4pKOjRzNk[1NFU>
AC3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXTTWM2OD1{NT65JI5O MYqyOFE3PjVyNR?=
H82 MVzGeY5kfGmxbjDBd5NigQ>? MnjZN|Ahdk1? NHLrdHU4OiCq MV;pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NIDUTpIzPDF4NkWwOS=>
GLC4 M2LGbmZ2dmO2aX;uJGF{e2G7 M2rjc|MxKG6P MmGzO|IhcA>? MkL1bY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NVizdmFrOjRzNk[1NFU>
H146  M3\ESmZ2dmO2aX;uJGF{e2G7 MY[zNEBvVQ>? NUi2bmdVPzJiaB?= NVqwW4hCcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NHnmS5gzPDF4NkWwOS=>
OVCAR-5 NV;xenI2S2WubDDWbYFjcWyrdImgRZN{[Xl? MYCwMVExODBibl2= NET0Z|U4OiCq MnP0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MWOyN|kxODF|Nh?=
OVCAR-8 Mmr5R4VtdCCYaXHibYxqfHliQYPzZZk> NIC5NmgxNTFyMECgcm0> NHvwW5E4OiCq NVLvO|NVcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnfHNlM6ODBzM{[=
A1847 M3rUSGNmdGxiVnnhZoltcXS7IFHzd4F6 NYPkVY9EOC1zMECwJI5O MWe3NkBp M1zkT4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{LpZlI{QTByMUO2
SKOV-3 NX22Xpc{S2WubDDWbYFjcWyrdImgRZN{[Xl? NVzhZnJnOC1zMECwJI5O NGHZeHQ4OiCq NXThXlBzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHXZSZIzOzlyMEGzOi=>
OVCAR-5 MmLmRZBweHSxc3nzJGF{e2G7 NVr5cpZlOTBvMUCwJI5O M{P2dFI1NzR6L{eyJIg> NF3F[|VqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MVeyN|kxODF|Nh?=
OVCAR-8 MYnBdI9xfG:|aYOgRZN{[Xl? MlHHNVAuOTByIH7N MWmyOE81QC95MjDo NXL4O4htcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MUGyN|kxODF|Nh?=
A1847 MlH1RZBweHSxc3nzJGF{e2G7 NGK2fWQyOC1zMECgcm0> M1nK[|I1NzR6L{eyJIg> MojBbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NHP0PWIzOzlyMEGzOi=>
H2228 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVX1VWh[OC1zMECwJI5O M1fNN|czKGh? M4X1fmlEPTB;MUOgcm0> M3K1elI{PTN|Mk[1
H3122 MlmzR4VtdCCYaXHibYxqfHliQYPzZZk> NVXjdFNpOC1zMECwJI5O NXXBSpVsPzJiaB?= MXHJR|UxRTFyIH7N NH3iWWszOzV|M{K2OS=>
K008 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWTJR|UxRTZyIH7N NYPGc|U1OjN2MUi1NlM>
K028 MnO0R4VtdCCYaXHibYxqfHliQYPzZZk> MnTUTWM2OD16NDDuUS=> M{jscFI{PDF6NUKz
K029 Ml;3R4VtdCCYaXHibYxqfHliQYPzZZk> MmrOTWM2OD12NjDuUS=> NYTjPFdYOjN2MUi1NlM>
M23 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEn5cGJKSzVyPUO3MlUhdk1? NVjFeWVrOjN2MUi1NlM>
K033 NX;wVIlJS2WubDDWbYFjcWyrdImgRZN{[Xl? MnfvTWM2OD15NT61JI5O M1i5U|I{PDF6NUKz
K008 NGLId2FHfW6ldHnvckBCe3OjeR?= NET6T|MzPTBibl2= MVqyOEBp M1rYfYlv\HWlZYOgS|Ih[XK{ZYP0 Mn3FNlM1OTh3MkO=
K028 NHSzWFlHfW6ldHnvckBCe3OjeR?= NIfsXWQzPTBibl2= NEPKbGIzPCCq MkPBbY5lfWOnczDHNkBienKnc4S= MUiyN|QyQDV{Mx?=
K029 NHnCXXFHfW6ldHnvckBCe3OjeR?= M136W|I2OCCwTR?= Mke3NlQhcA>? Mn2wbY5lfWOnczDHNUBienKnc4S= Mn[zNlM1OTh3MkO=
M23 MXjGeY5kfGmxbjDBd5NigQ>? M2H4[FI2OCCwTR?= NIXvSWwzPCCq MXzpcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= NVzjbYZKOjN2MUi1NlM>
K033 NWHUOpZsTnWwY4Tpc44hSXO|YYm= NIL6fFQzPTBibl2= Ml;mNlQhcA>? MY\pcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? NYHrfHR5OjN2MUi1NlM>
K008 MmTwRZBweHSxc3nzJGF{e2G7 MnvZNVAxKG6P NXq2N4c6PzJiaB?= NIjidFV{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NVmxZ49UOjN2MUi1NlM>
K028 NFLuOodCeG:ydH;zbZMhSXO|YYm= NGrGOoUyODBibl2= MVW3NkBp M2nnb5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M1Oz[|I{PDF6NUKz
K029 MXHBdI9xfG:|aYOgRZN{[Xl? M1L6WlExOCCwTR?= MkTjO|IhcA>? Mmfid4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M2O2cFI{PDF6NUKz
M23 MlnPRZBweHSxc3nzJGF{e2G7 MlvmNVAxKG6P NGr2Z2Y4OiCq M1HTPZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MoTWNlM1OTh3MkO=
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CHLA-10 M4rScWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP6SFdqUUN3ME21Mlchdk1? M{\5flI{OzB|N{Sx
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SJ-GBM2 NH;xN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rLeWlEPTB;MUKuPUBvVQ>? NWjCTVB3OjN|MEO3OFE>
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CHLA-90 NFLrb5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJ{LkOgcm0> M3\zS|I{OzB|N{Sx
CHLA-136 NUjtW|FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJ|LkKgcm0> M4\uNFI{OzB|N{Sx
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COG-LL-317 NFLJemlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTRwNDDuUS=> NEfYNm8zOzNyM{e0NS=>
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CCRF-CEM (1) MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTF{LkWgcm0> NUTNSIp3OjN|MEO3OFE>
CCRF-CEM (2) NFq0T5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjFXmdKSzVyPUeuNkBvVQ>? MUWyN|MxOzd2MR?=
Kasumi-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLpTWM2OD13Lkigcm0> NXzTNWdNOjN|MEO3OFE>
Karpas-299 M{D1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTlwNjDuUS=> M37uclI{OzB|N{Sx
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H1355 NWL5UG1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLK[XZXUUN3ME21JI5O NGDHUpMzOzBzMkK0PC=>
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HOP-62 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33qdWlEPTB;MUGgcm0> NEC2XFczOzBzMkK0PC=>
H23 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnE[nlDUUN3ME2xNUBvVQ>? NHL0fo8zOzBzMkK0PC=>
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H2212 NXTQW2xQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf1WpZ2UUN3ME2xO{BvVQ>? NXvmdZA{OjNyMUKyOFg>
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H1792 NUjsXmM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\vN5dKSzVyPUKwJI5O MlzXNlMxOTJ{NEi=
COR-L23 Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELiWJBKSzVyPUKyJI5O MU[yN|AyOjJ2OB?=
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NCI-H1975 NVLTcmdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLROHA4OiCq Mlj6TWM2OD16IH7N NFTxOWMzOjF2NE[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)

  • Mass
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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 )

  • C1
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    C2
    V2

* 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):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
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