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 NVzlPWxMSXCxcITvd4l{KEG|c3H5 NED4ZYg{OC96MD:xOVAwOjVyIH7N M3POS|I1NzR6L{eyJIg> MkDZbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz MmjsNlU5QDJ3NUC=
MV411 M{H5c2Fxd3C2b4Ppd{BCe3OjeR?= NEmxe2c{OC96MD:xOVAwOjVyIH7N MUiyOE81QC95MjDo NETUT4RqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> NFH0NpUzPTh6MkW1NC=>
MGC-803 MnK4R4VtdCCYaXHibYxqfHliQYPzZZk> MVmwMlEuOTByMDDuUS=> Mmn1O|IhcA>? M1\MTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{PEOFI2PTlyOEC1
SGC-7901 MnPPR4VtdCCYaXHibYxqfHliQYPzZZk> M4myPVAvOS1zMECwJI5O MlTSO|IhcA>? MkCxbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NIPJUpEzPTV7MEiwOS=>
MKN-28 M2m1dmNmdGxiVnnhZoltcXS7IFHzd4F6 MWSwMlEuOTByMDDuUS=> M4X0OlczKGh? NF7PS2pqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MW[yOVU6ODhyNR?=
MGC-803 MV\GeY5kfGmxbjDBd5NigQ>? NWLkSnVEOC5zLUGwNFAhdk1? NUewV4hMOjRiaB?= NYrtNnJXcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 NWnGSo83OjV3OUC4NFU>
HCT-116 M3LLZmZ2dmO2aX;uJGF{e2G7 NUDB[IpXPTCwTR?= NX23UWpSOjRiaB?= Mn\5SG1UVw>? NUHydYZ4cW6mdXPl[EBIOC:JMTDhdpJme3R? NEnCdGwzPTJzMEe5OC=>
HT-29 NUfodJU5TnWwY4Tpc44hSXO|YYm= MUK1NI5O NFm2PXAzPCCq MWTEUXNQ MV;pcoR2[2WmIFewM2cyKGG{cnXzeC=> M13B[|I2OjFyN{m0
SCC25 MXzDfZRwgGmlaYT5JGF{e2G7 NWDJNY9TOTBxNUCgcm0> MnXoNlQhcA>? Mnri[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NF:wVZozPTJyNUSzNC=>
FUDA M2XxbGN6fG:6aXPpeJkhSXO|YYm= NHuxXWcyOC93MDDuUS=> MUmyOEBp M{OwUIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MnHUNlUzODV2M{C=
Detroit562 MV;DfZRwgGmlaYT5JGF{e2G7 NUCzUnhiOTBxNUCgcm0> NG\OWYYzPCCq Mlro[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M3O0[FI2OjB3NEOw
CAL27 NHrUbZVEgXSxeHnjbZR6KEG|c3H5 MmC3NVAwPTBibl2= MkDFNlQhcA>? NGPhVWhl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MoTzNlUzODV2M{C=
DSH1 Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTZibl2= NIC0XoozPDd6NEizPS=>
SW-1710 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm3RnFKSzVyPU[gcm0> M4XSUlI1Pzh2OEO5
T24 NFfYR|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXENGRKSzVyPUegcm0> NFnJeWgzPDd6NEizPS=>
RT112 NHqyTnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPhRWhwUUN3ME25JI5O NYTRbmg5OjR5OES4N|k>
639-V MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFyIH7N M3PKOFI1Pzh2OEO5
SCaBER MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[zRXNKUUN3ME2xNEBvVQ>? NYDh[JZVOjR5OES4N|k>
BFTC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPzfWdoUUN3ME2xO{BvVQ>? MYWyOFc5PDh|OR?=
J82 NXXncGNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvvW2VoUUN3ME2xPEBvVQ>? NVThNYlxOjR5OES4N|k>
HT-1376 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPZTWM2OD1{MTDuUS=> Mm[wNlQ4QDR6M{m=
647-V NXW5VJpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJ5IH7N NWrVd2M1OjR5OES4N|k>
UM-UC3 M371Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN|IH7N M{fQXVI1Pzh2OEO5
LB831-BLC M13YSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLvTWM2OD1|NDDuUS=> M{fHO|I1Pzh2OEO5
KU-19-19 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTN4IH7N M3;5[FI1Pzh2OEO5
35612 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPCdVBkUUN3ME2zPEBvVQ>? MnnwNlQ4QDR6M{m=
5637 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDWTWM2OD12NDDuUS=> Mk\aNlQ4QDR6M{m=
HT-1197 NH;vfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\FbGlEPTB;NUOgcm0> NYDmZlB[OjR5OES4N|k>
MGH-U3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XBd2lEPTB;NUOgcm0> NXHo[FRGOjR5OES4N|k>
TCCSUP M3vPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f5TWlEPTB;MUSyJI5O NXHKeYlGOjR5OES4N|k>
RT4 NYjSb3hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrJVG1KSzVyPUG3N|Mhdk1? NUTJcYt{OjR5OES4N|k>
SW780 NETPbI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfhUmMyUUN3ME2zOFUyKG6P NUi4foNxOjR5OES4N|k>
RKO NUPH[o9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPmOmJTUUN3ME20JI5O Mk\mNlQ3QDJ5NEe=
LS-411 N MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq0UZNKSzVyPUWgcm0> MYOyOFY5Ojd2Nx?=
SW620 NEjaToxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknxTWM2OD16IH7N M2jyVVI1Pjh{N{S3
HCT-15 NGK1[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S1T2lEPTB;ODDuUS=> MYOyOFY5Ojd2Nx?=
HuTu-80 M{LoTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTF|IH7N NH7CUGYzPDZ6Mke0Oy=>
HCT 116 NFG2[mVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLzZolKSzVyPUG0JI5O NGntR|MzPDZ6Mke0Oy=>
COLO-205 NVTsR2prT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln5TWM2OD1zNDDuUS=> Ml\vNlQ3QDJ5NEe=
NCI-H747 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\xfmlEPTB;MUegcm0> M2LCU|I1Pjh{N{S3
COLO-678 M1;jVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PJ[mlEPTB;MkGgcm0> MXiyOFY5Ojd2Nx?=
LoVo NW\aWGpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ{IH7N MYSyOFY5Ojd2Nx?=
LS-1034 NF3zbZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHvTWM2OD1|MTDuUS=> M{DLN|I1Pjh{N{S3
SNU-C2B NVTYWFNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3hTWM2OD12NTDuUS=> M1zaTVI1Pjh{N{S3
LS-123 MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKxTWM2OD15MzDuUS=> MUWyOFY5Ojd2Nx?=
SK-CO-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjyTWM2OD16MTDuUS=> MlPzNlQ3QDJ5NEe=
HCC2998 M1ToOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjndHVCUUN3ME2xNlghdk1? NXzLUlFUOjR4OEK3OFc>
MDA-MB-231 NFuzfotHfW6ldHnvckBCe3OjeR?= M4LGPVExOCCwTR?= M1PBXlMxKG2rbh?= M3vG[4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z NILHWIIzPDJ2OEK2OS=>
MDA-MB-435 MXfGeY5kfGmxbjDBd5NigQ>? NGXLUpQyODBibl2= Ml;sN|AhdWmw M{HU[4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z MWSyOFI1QDJ4NR?=
BT-20  M33wUGZ2dmO2aX;uJGF{e2G7 MmDPNVAxNzJ3MDDuUS=> NF3yZnMzPCCq MXXy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> MnzaNlQyPzN3NEG=
MDA-MB-231 MlLNSpVv[3Srb36gRZN{[Xl? MlPyNVAxKG6P MmTWNlQhcA>? M4n2U4lvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> NYrvNWRpOjRzN{O1OFE>
H82 M37pZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S2dmlEPTB;M{CuNlchdk1? NXruTXNXOjRzNk[1NFU>
GLC4 M3fKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLwTWM2OD1{MD60O{BvVQ>? MXyyOFE3PjVyNR?=
H69 NYLnXGxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH1TWM2OD16Mz6zOkBvVQ>? NYPKcHBEOjRzNk[1NFU>
H128 NXW1bFVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\NTWM2OD14OT61OUBvVQ>? NXjKVWU3OjRzNk[1NFU>
H146 NH;FcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7QWVZ6UUN3ME2yPE42OSCwTR?= NYPvPWhDOjRzNk[1NFU>
H187 NIHLe2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfyTWM2OD1{ND65PUBvVQ>? NHn6OGczPDF4NkWwOS=>
H526 MnHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4foWGlEPTB;MkGuOlQhdk1? NXLwcndzOjRzNk[1NFU>
N592 M4GxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jDW2lEPTB;MUSuNVIhdk1? NGjSZ2czPDF4NkWwOS=>
H620 NHfNUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLOSXk2UUN3ME2zNk43PyCwTR?= M4Hje|I1OTZ4NUC1
H792 NF61[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR3LkC3JI5O MYWyOFE3PjVyNR?=
H1173 M3fSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfjNGlKSzVyPUGyMlYzKG6P MU[yOFE3PjVyNR?=
AC3 NEn3c|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXHcnhKSzVyPUK1Mlkhdk1? NIHDb|AzPDF4NkWwOS=>
H82 NHr3cpRHfW6ldHnvckBCe3OjeR?= NXvkbnFrOzBibl2= NFTrfmc4OiCq NHHrV4FqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NHLxN4ozPDF4NkWwOS=>
GLC4 M4Xwc2Z2dmO2aX;uJGF{e2G7 MVizNEBvVQ>? Mo\5O|IhcA>? NYWxT3F4cW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NYW2bGt{OjRzNk[1NFU>
H146  NEfkSGxHfW6ldHnvckBCe3OjeR?= MnHqN|Ahdk1? NWXxW5BVPzJiaB?= M2\ndIlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NWXYSFJWOjRzNk[1NFU>
OVCAR-5 NGC4WYtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlPKNE0yODByIH7N M3;BfVczKGh? NF\rO3JqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlHwNlM6ODBzM{[=
OVCAR-8 NXGxNFZPS2WubDDWbYFjcWyrdImgRZN{[Xl? NIXGdY0xNTFyMECgcm0> NX[wcIQxPzJiaB?= MkfCbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MlXZNlM6ODBzM{[=
A1847 NYPiS2kzS2WubDDWbYFjcWyrdImgRZN{[Xl? NGLiZ|gxNTFyMECgcm0> MUW3NkBp MlTtbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NX;ufnhzOjN7MECxN|Y>
SKOV-3 MX\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFO4UW0xNTFyMECgcm0> M{\DUFczKGh? M3K5VolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYDDepV2OjN7MECxN|Y>
OVCAR-5 Ml[yRZBweHSxc3nzJGF{e2G7 Ml;aNVAuOTByIH7N M1T4[FI1NzR6L{eyJIg> MmrVbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MoDuNlM6ODBzM{[=
OVCAR-8 NEfZOldCeG:ydH;zbZMhSXO|YYm= NXrsXGR7OTBvMUCwJI5O NXvBcGNJOjRxNEivO|IhcA>? NUnN[mJYcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M1LSfFI{QTByMUO2
A1847 MVXBdI9xfG:|aYOgRZN{[Xl? MoixNVAuOTByIH7N NWfGdW5ZOjRxNEivO|IhcA>? NXTzZYw2cW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NVXYWXZ5OjN7MECxN|Y>
H2228 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn6wNE0yODByIH7N MWK3NkBp MoDFTWM2OD1zMzDuUS=> NWXRNmg3OjN3M{OyOlU>
H3122 M4rW[mNmdGxiVnnhZoltcXS7IFHzd4F6 MYWwMVExODBibl2= MonwO|IhcA>? M{XxT2lEPTB;MUCgcm0> Mn31NlM2OzN{NkW=
K008 M17IVGNmdGxiVnnhZoltcXS7IFHzd4F6 MV3JR|UxRTZyIH7N NEnIXoozOzRzOEWyNy=>
K028 NXy2b2U2S2WubDDWbYFjcWyrdImgRZN{[Xl? NIfBflhKSzVyPUi0JI5O MVyyN|QyQDV{Mx?=
K029 NFrCWFlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1vm[mlEPTB;NE[gcm0> NWH6S3B{OjN2MUi1NlM>
M23 M{XYUmNmdGxiVnnhZoltcXS7IFHzd4F6 NULvdlFwUUN3ME2zO{42KG6P M1jsbFI{PDF6NUKz
K033 NEezbpRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmjLTWM2OD15NT61JI5O NUjJ[3piOjN2MUi1NlM>
K008 NIHifGtHfW6ldHnvckBCe3OjeR?= MYSyOVAhdk1? M3T5[FI1KGh? MmLybY5lfWOnczDHNkBienKnc4S= NUPVS3BNOjN2MUi1NlM>
K028 Ml2wSpVv[3Srb36gRZN{[Xl? Mn35NlUxKG6P MojMNlQhcA>? M3L4PIlv\HWlZYOgS|Ih[XK{ZYP0 NXTkPGxyOjN2MUi1NlM>
K029 MXzGeY5kfGmxbjDBd5NigQ>? MkOwNlUxKG6P NUXsXm5HOjRiaB?= NFH0[XVqdmS3Y3XzJGcyKGG{cnXzeC=> MkPiNlM1OTh3MkO=
M23 NEf1ZZpHfW6ldHnvckBCe3OjeR?= NUDoUGptOjVyIH7N M1OxSFI1KGh? NEni[XRqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> M3XFSVI{PDF6NUKz
K033 NVjmOW1YTnWwY4Tpc44hSXO|YYm= NH;jXZczPTBibl2= NH3vfJEzPCCq MlmwbY5lfWOnczDhJI1w\GW|dDDpcoNz\WG|ZTDpckBIOSCyb4D1cIF1cW:w Mlf6NlM1OTh3MkO=
K008 MYPBdI9xfG:|aYOgRZN{[Xl? NVf5coFpOTByIH7N NWHXTolTPzJiaB?= M4TmNZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M{H2d|I{PDF6NUKz
K028 NXzYb406SXCxcITvd4l{KEG|c3H5 MnvJNVAxKG6P M4TZc|czKGh? MoWwd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MUCyN|QyQDV{Mx?=
K029 NELhWVRCeG:ydH;zbZMhSXO|YYm= NXLybmtVOTByIH7N MorVO|IhcA>? MnPmd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? MoewNlM1OTh3MkO=
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Rh18 MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;Nc4hKSzVyPU[uNkBvVQ>? NIn1OGwzOzNyM{e0NS=>
Rh30 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTVwNjDuUS=> MlO4NlM{ODN5NEG=
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CHLA-266 Mo\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTJ5LkGgcm0> NGq0cWUzOzNyM{e0NS=>
TC-71 M{jmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fpZmlEPTB;ND61JI5O NETrd|YzOzNyM{e0NS=>
CHLA-9 NFLHSXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL0TWM2OD12Lk[gcm0> Mk\iNlM{ODN5NEG=
CHLA-10 M{PDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTVwNzDuUS=> NU\KSY1UOjN|MEO3OFE>
CHLA-258 NFi0dWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTZwNDDuUS=> M2jiRVI{OzB|N{Sx
SJ-GBM2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF{Lkmgcm0> NGTEW4ozOzNyM{e0NS=>
NB-1643 NX7IPJljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7YOYFKSzVyPUeuOEBvVQ>? M1X4W|I{OzB|N{Sx
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CHLA-90 M{HUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P2UGlEPTB;MkKuN{BvVQ>? NEDqOIszOzNyM{e0NS=>
CHLA-136 NHK3NWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PYSWlEPTB;MkOuNkBvVQ>? MXGyN|MxOzd2MR?=
NALM-6 NGXMVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofJTWM2OD1zMT63JI5O Mn[wNlM{ODN5NEG=
COG-LL-317 NYTNeoF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmWyTWM2OD12LkSgcm0> NX\lcGR[OjN|MEO3OFE>
RS4;11 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XLVmlEPTB;MUOuOUBvVQ>? M4LG[FI{OzB|N{Sx
MOLT-4 NV7WdVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnoNI9KSzVyPUGwMlYhdk1? NXnK[2VROjN|MEO3OFE>
CCRF-CEM (1) NWXGSVd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF{LkWgcm0> NUfJNXU3OjN|MEO3OFE>
CCRF-CEM (2) MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTdwMjDuUS=> MlTwNlM{ODN5NEG=
Kasumi-1 M{HGZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rGWGlEPTB;NT64JI5O MWGyN|MxOzd2MR?=
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VCaP NGjBeHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LPVGlEPTB;NzDuUS=> NFjTfI4zOzF3MkCwOC=>
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H157 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;KPWlEPTB;NzDuUS=> Ml3xNlMxOTJ{NEi=
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HOP-62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrSTWM2OD1zMTDuUS=> NYXX[nJ{OjNyMUKyOFg>
H23 MmPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH61bI9KSzVyPUGxJI5O M2XyVFI{ODF{MkS4
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H441 M2DLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTBTWM2OD1zNDDuUS=> MVmyN|AyOjJ2OB?=
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H2009 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfRTWM2OD1zOTDuUS=> M1jqPFI{ODF{MkS4
H1792 NETmfmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPSTWM2OD1{MDDuUS=> Mnr2NlMxOTJ{NEi=
COR-L23 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7BfWg1UUN3ME2yNkBvVQ>? MUCyN|AyOjJ2OB?=
H727 NEfhdHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rpSGlEPTB;Mkigcm0> NVqwW|diOjNyMUKyOFg>
H1734 M1XPSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTNTWM2OD1{ODDuUS=> NVvRcWpLOjNyMUKyOFg>
H358 M3LjdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfETWM2OD1{OTDuUS=> M4HmZ|I{ODF{MkS4
A549 M4LL[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjIR4ZKSzVyPUSzJI5O MoPaNlMxOTJ{NEi=
H2122 NGXrTJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXSXolKSzVyPUWzJI5O MXqyN|AyOjJ2OB?=
Calu-1 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTV6IH7N Mmm1NlMxOTJ{NEi=
Calu-6 NXm5b5lWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTZ2IH7N MY[yN|AyOjJ2OB?=
NCI-H1975 M2XPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUi0PEBp MYrJR|UxRTF4IH7N NH;iSlkzOjF2NE[2OS=>
NCI-H1975 NFfsZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXr2TGRtPzJiaB?= M334VmlEPTB;ODDuUS=> MkPKNlIyPDR4NkW=

... 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).

The Serial Dilution Calculator Equation

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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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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
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