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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Cited by 8 Publications

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 NVuxbpN{SXCxcITvd4l{KEG|c3H5 MnvRN|AwQDBxMUWwM|I2OCCwTR?= NFTOO3MzPC92OD:3NkBp MUDpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= NYXTN4g2OjV6OEK1OVA>
MV411 NUnEdIdYSXCxcITvd4l{KEG|c3H5 MkHTN|AwQDBxMUWwM|I2OCCwTR?= MnTZNlQwPDhxN{KgbC=> MmixbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NGO2fVEzPTh6MkW1NC=>
MGC-803 NIH2UHpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEXGTJAxNjFvMUCwNEBvVQ>? NX;GXZpEPzJiaB?= MkjTbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mm[5NlU2QTB6MEW=
SGC-7901 NXXNbnY6S2WubDDWbYFjcWyrdImgRZN{[Xl? MkTMNE4yNTFyMECgcm0> NXj2TJVIPzJiaB?= MWLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MoO2NlU2QTB6MEW=
MKN-28 NEntR5RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnX2NE4yNTFyMECgcm0> MYO3NkBp NF7xNGJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MkjyNlU2QTB6MEW=
MGC-803 M2jUdmZ2dmO2aX;uJGF{e2G7 M2j4TlAvOS1zMECwJI5O NIHVW|gzPCCq Ml\mbY5lfWOnczDHNk9OKGOnbHytZ5lkdGViYYLy[ZN1 NFjuN3kzPTV7MEiwOS=>
HCT-116 NVjyWINOTnWwY4Tpc44hSXO|YYm= NI\ueoU2OG6P M3zhb|I1KGh? M2TUeGROW09? MmrwbY5lfWOnZDDHNE9IOSCjcoLld5Q> MkP2NlUzOTB5OUS=
HT-29 NYi5RpdzTnWwY4Tpc44hSXO|YYm= Mn3WOVBvVQ>? NEfRRWkzPCCq NUHQNoE5TE2VTx?= NV\XR2lzcW6mdXPl[EBIOC:JMTDhdpJme3R? M1jxelI2OjFyN{m0
SCC25 MUnDfZRwgGmlaYT5JGF{e2G7 NYTJeGQxOTBxNUCgcm0> MY[yOEBp NUn2dIRn\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MlzENlUzODV2M{C=
FUDA M{HOS2N6fG:6aXPpeJkhSXO|YYm= NUTRUJZjOTBxNUCgcm0> MoTENlQhcA>? NX3BT5Ni\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MmrBNlUzODV2M{C=
Detroit562 NV;iTHZxS3m2b4jpZ4l1gSCDc4PhfS=> M4rhO|ExNzVyIH7N NYD3VYxyOjRiaB?= NVjyeFRs\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NUnZNG97OjV{MEW0N|A>
CAL27 MnH0R5l1d3irY3n0fUBCe3OjeR?= M{\lS|ExNzVyIH7N NX7VZ2VkOjRiaB?= NVP1[3RS\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MWKyOVIxPTR|MB?=
DSH1 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;QVWR{UUN3ME22JI5O M4fweVI1Pzh2OEO5
SW-1710 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\aXGlEPTB;NjDuUS=> M2K4O|I1Pzh2OEO5
T24 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPxO3g4UUN3ME23JI5O M4XV[VI1Pzh2OEO5
RT112 NFfnN4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M176WmlEPTB;OTDuUS=> M2TOc|I1Pzh2OEO5
639-V M4DmTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfJUGZMUUN3ME2xNEBvVQ>? M2HHelI1Pzh2OEO5
SCaBER MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PK[2lEPTB;MUCgcm0> Mo\1NlQ4QDR6M{m=
BFTC NHLvVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTHTWM2OD1zNzDuUS=> NH73NIIzPDd6NEizPS=>
J82 MlzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\1[YdWUUN3ME2xPEBvVQ>? NFi1[pMzPDd6NEizPS=>
HT-1376 NF62TndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrmRZhKSzVyPUKxJI5O NUTNZ45zOjR5OES4N|k>
647-V NInZcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH6NZJ4UUN3ME2yO{BvVQ>? MYeyOFc5PDh|OR?=
UM-UC3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfIOI5JUUN3ME2zN{BvVQ>? NFjT[YEzPDd6NEizPS=>
LB831-BLC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTN2IH7N MnHGNlQ4QDR6M{m=
KU-19-19 NV\RfWw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTN4IH7N MXuyOFc5PDh|OR?=
35612 NIPrTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3HeFJKSzVyPUO4JI5O NG\m[2YzPDd6NEizPS=>
5637 NWC5SXlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTR2IH7N MoXMNlQ4QDR6M{m=
HT-1197 M4XndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrQTWM2OD13MzDuUS=> MkT2NlQ4QDR6M{m=
MGH-U3 NFjMUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf0TWM2OD13MzDuUS=> NWXGXHZyOjR5OES4N|k>
TCCSUP MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjKXGJKSzVyPUG0NkBvVQ>? M2HlOVI1Pzh2OEO5
RT4 M4TlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjxdG9KSzVyPUG3N|Mhdk1? M17pVVI1Pzh2OEO5
SW780 NUnMfJBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[yNGlEPTB;M{S1NUBvVQ>? M4jZdVI1Pzh2OEO5
RKO MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTYTWM2OD12IH7N NGHmZlQzPDZ6Mke0Oy=>
LS-411 N MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPq[HVKSzVyPUWgcm0> NVH2NVkyOjR4OEK3OFc>
SW620 NUi2fFJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRThibl2= M2K5OlI1Pjh{N{S3
HCT-15 NU\5[JZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn6TWM2OD16IH7N Ml7sNlQ3QDJ5NEe=
HuTu-80 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoixTWM2OD1zMzDuUS=> M3XZVVI1Pjh{N{S3
HCT 116 NILCS3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7JTWM2OD1zNDDuUS=> MWGyOFY5Ojd2Nx?=
COLO-205 NGnIbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DTTmlEPTB;MUSgcm0> MXKyOFY5Ojd2Nx?=
NCI-H747 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF5IH7N MX6yOFY5Ojd2Nx?=
COLO-678 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrLbGVKSzVyPUKxJI5O MoTxNlQ3QDJ5NEe=
LoVo NWP2TotwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUi4XVNyUUN3ME2yNkBvVQ>? NYL0TZZQOjR4OEK3OFc>
LS-1034 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTNzIH7N NFLpbIgzPDZ6Mke0Oy=>
SNU-C2B NELYN|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H5U2lEPTB;NEWgcm0> MWGyOFY5Ojd2Nx?=
LS-123 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXNSGcyUUN3ME23N{BvVQ>? MlrJNlQ3QDJ5NEe=
SK-CO-1 MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm5W4hnUUN3ME24NUBvVQ>? MlH6NlQ3QDJ5NEe=
HCC2998 MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrzbGVKSzVyPUGyPEBvVQ>? NH\JboozPDZ6Mke0Oy=>
MDA-MB-231 NXjSXWJSTnWwY4Tpc44hSXO|YYm= Mny0NVAxKG6P NETNZos{OCCvaX6= NVnLT4VqcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NGfHW3EzPDJ2OEK2OS=>
MDA-MB-435 MnLDSpVv[3Srb36gRZN{[Xl? M{DwfFExOCCwTR?= M2j0b|MxKG2rbh?= NWfCN5BTcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MlHVNlQzPDh{NkW=
BT-20  MWLGeY5kfGmxbjDBd5NigQ>? MXKxNFAwOjVyIH7N NF;Fd48zPCCq NV7t[|R5emW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI NUXtcVJ[OjRzN{O1OFE>
MDA-MB-231 MoDVSpVv[3Srb36gRZN{[Xl? MkTKNVAxKG6P MX:yOEBp M3e2UYlvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> M1Hhe|I1OTd|NUSx
H82 Mo\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnsS3czUUN3ME2zNE4zPyCwTR?= NIG5UoYzPDF4NkWwOS=>
GLC4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJyLkS3JI5O NWLMfnRmOjRzNk[1NFU>
H69 NV7GV2NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXmXmpKSzVyPUizMlM3KG6P NXLRNFhSOjRzNk[1NFU>
H128 Ml;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTZ7LkW1JI5O M3fCUlI1OTZ4NUC1
H146 MkH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknUTWM2OD1{OD61NUBvVQ>? MUiyOFE3PjVyNR?=
H187 MofuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPnTWM2OD1{ND65PUBvVQ>? MVyyOFE3PjVyNR?=
H526 NFTDUmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTsTWM2OD1{MT62OEBvVQ>? M3iwTlI1OTZ4NUC1
N592 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTF2LkGyJI5O NGHoZoUzPDF4NkWwOS=>
H620 M3PxZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPJTWM2OD1|Mj62O{BvVQ>? MXqyOFE3PjVyNR?=
H792 NFzL[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfLTWM2OD12NT6wO{BvVQ>? NV:5eWNKOjRzNk[1NFU>
H1173 M3zXcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTF{Lk[yJI5O MYqyOFE3PjVyNR?=
AC3 M3vIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILQTHVKSzVyPUK1Mlkhdk1? NYTrXnJYOjRzNk[1NFU>
H82 NWTIc|F[TnWwY4Tpc44hSXO|YYm= M2XzPVMxKG6P NI\NVFk4OiCq NFXy[2hqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NW\iRWNpOjRzNk[1NFU>
GLC4 NWTub3ZlTnWwY4Tpc44hSXO|YYm= MlOzN|Ahdk1? NYnrToViPzJiaB?= NGq3b4dqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M{PQT|I1OTZ4NUC1
H146  Mo[0SpVv[3Srb36gRZN{[Xl? MXKzNEBvVQ>? M2[yfFczKGh? M1Gycolv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NHHERYIzPDF4NkWwOS=>
OVCAR-5 NYnLbJZMS2WubDDWbYFjcWyrdImgRZN{[Xl? NGq1O3AxNTFyMECgcm0> M4nPfVczKGh? NVTCS2Q2cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NELnR5gzOzlyMEGzOi=>
OVCAR-8 NUnLNoZmS2WubDDWbYFjcWyrdImgRZN{[Xl? MU[wMVExODBibl2= Mn7DO|IhcA>? MYPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NISzNXUzOzlyMEGzOi=>
A1847 MkXyR4VtdCCYaXHibYxqfHliQYPzZZk> MmraNE0yODByIH7N NIWxT5I4OiCq NGHwTppqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NETUO|MzOzlyMEGzOi=>
SKOV-3 MlzPR4VtdCCYaXHibYxqfHliQYPzZZk> MmPINE0yODByIH7N MWq3NkBp MnrNbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NV24SVlQOjN7MECxN|Y>
OVCAR-5 MUfBdI9xfG:|aYOgRZN{[Xl? MlOxNVAuOTByIH7N MkHNNlQwPDhxN{KgbC=> MXnpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MUeyN|kxODF|Nh?=
OVCAR-8 NXTQNGZtSXCxcITvd4l{KEG|c3H5 NUj3b|dTOTBvMUCwJI5O MWWyOE81QC95MjDo NUfUe|ExcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> MVWyN|kxODF|Nh?=
A1847 NHW5cmlCeG:ydH;zbZMhSXO|YYm= M1f4blExNTFyMDDuUS=> M3fpNlI1NzR6L{eyJIg> NF;uSI1qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 Mle3NlM6ODBzM{[=
H2228 NW[2XlZzS2WubDDWbYFjcWyrdImgRZN{[Xl? MUmwMVExODBibl2= M2jYVVczKGh? M2D5OmlEPTB;MUOgcm0> NXjTU41iOjN3M{OyOlU>
H3122 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkfrNE0yODByIH7N MYm3NkBp NXPHPGV2UUN3ME2xNEBvVQ>? NHe4cIgzOzV|M{K2OS=>
K008 M1HnSGNmdGxiVnnhZoltcXS7IFHzd4F6 NVHVSJNKUUN3ME22NEBvVQ>? Mn:yNlM1OTh3MkO=
K028 NVf2PXhDS2WubDDWbYFjcWyrdImgRZN{[Xl? MYDJR|UxRTh2IH7N Ml75NlM1OTh3MkO=
K029 Mnv2R4VtdCCYaXHibYxqfHliQYPzZZk> MVHJR|UxRTR4IH7N M3Hn[|I{PDF6NUKz
M23 M1HseWNmdGxiVnnhZoltcXS7IFHzd4F6 MUfJR|UxRTN5LkWgcm0> MXuyN|QyQDV{Mx?=
K033 NFLX[3JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHXQV|dKSzVyPUe1MlUhdk1? NUnwNZA4OjN2MUi1NlM>
K008 M3\nOWZ2dmO2aX;uJGF{e2G7 MUWyOVAhdk1? NYfOfVFvOjRiaB?= Mmm1bY5lfWOnczDHNkBienKnc4S= NXfFeHJLOjN2MUi1NlM>
K028 NWfp[2tuTnWwY4Tpc44hSXO|YYm= Ml7HNlUxKG6P MXeyOEBp MlPSbY5lfWOnczDHNkBienKnc4S= NYPhNWpDOjN2MUi1NlM>
K029 M1nkfWZ2dmO2aX;uJGF{e2G7 M{fEfFI2OCCwTR?= NVrnSHdtOjRiaB?= NYjnWJNMcW6mdXPld{BIOSCjcoLld5Q> NFK5flAzOzRzOEWyNy=>
M23 NYXwUXpwTnWwY4Tpc44hSXO|YYm= MViyOVAhdk1? MlPZNlQhcA>? NUfyZZFncW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> NF62OHMzOzRzOEWyNy=>
K033 Mke4SpVv[3Srb36gRZN{[Xl? MYSyOVAhdk1? NYK5bZhxOjRiaB?= MmHDbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w NGrifmYzOzRzOEWyNy=>
K008 M1zxRWFxd3C2b4Ppd{BCe3OjeR?= MmK1NVAxKG6P MkC0O|IhcA>? Ml;Gd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MlL6NlM1OTh3MkO=
K028 NYf3V3NNSXCxcITvd4l{KEG|c3H5 NFfa[VUyODBibl2= MWO3NkBp MoXRd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NH;F[HMzOzRzOEWyNy=>
K029 NFyzfmVCeG:ydH;zbZMhSXO|YYm= MlXBNVAxKG6P NXrGNXJuPzJiaB?= M{jlTZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NH;qSlMzOzRzOEWyNy=>
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CHLA-258 MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml65TWM2OD14LkSgcm0> NETNVVkzOzNyM{e0NS=>
SJ-GBM2 NGHvT3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIficmJKSzVyPUGyMlkhdk1? NWnoV|J6OjN|MEO3OFE>
NB-1643 NIW2bYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ewSWlEPTB;Nz60JI5O M1zlO|I{OzB|N{Sx
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RS4;11 M{SzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIniXmpKSzVyPUGzMlUhdk1? NGLsWZUzOzNyM{e0NS=>
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CCRF-CEM (1) NGThfXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjYTWM2OD1zMj61JI5O MXuyN|MxOzd2MR?=
CCRF-CEM (2) Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\HN5BKSzVyPUeuNkBvVQ>? M1zkR|I{OzB|N{Sx
Kasumi-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjDZVBKSzVyPUWuPEBvVQ>? MVKyN|MxOzd2MR?=
Karpas-299 NYXo[4JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\pd2lEPTB;OT62JI5O MWmyN|MxOzd2MR?=
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H1355 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPKXnRFUUN3ME21JI5O MkfwNlMxOTJ{NEi=
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HOP-62 NULsd|gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XZRmlEPTB;MUGgcm0> NHnydXMzOzBzMkK0PC=>
H23 M2Xh[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDpblFKSzVyPUGxJI5O NHnZVoUzOzBzMkK0PC=>
H2030 NVjSfIlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLlTWM2OD1zMjDuUS=> MV2yN|AyOjJ2OB?=
H441 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDPfI5KSzVyPUG0JI5O MYeyN|AyOjJ2OB?=
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H1792 NXrvNmxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nkR2lEPTB;MkCgcm0> MXyyN|AyOjJ2OB?=
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H727 NHnaUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHj0UpZKSzVyPUK4JI5O M1fjSFI{ODF{MkS4
H1734 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJ6IH7N MWqyN|AyOjJ2OB?=
H358 NInJR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;WVoJMUUN3ME2yPUBvVQ>? M4HEXFI{ODF{MkS4
A549 NFX1W3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXWcmtKSzVyPUSzJI5O Mn7PNlMxOTJ{NEi=
H2122 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f0OGlEPTB;NUOgcm0> M3fNelI{ODF{MkS4
Calu-1 NF6xcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTV6IH7N NWK0WlBkOjNyMUKyOFg>
Calu-6 NIPIcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDjTWM2OD14NDDuUS=> M3nBTVI{ODF{MkS4
NCI-H1975 NWHHdmJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlznOFghcA>? NVn3PZFlUUN3ME2xOkBvVQ>? NVfVfXRtOjJzNES2OlU>
NCI-H1975 M3zadGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnxO|IhcA>? NHPwb3VKSzVyPUigcm0> NHOzZnQzOjF2NE[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(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

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
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1

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

Related HSP (e.g. HSP90) Products4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID