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 NHnZSYlCeG:ydH;zbZMhSXO|YYm= M3fqOFMxNzhyL{G1NE8zPTBibl2= MViyOE81QC95MjDo MkXqbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NY\KSZdQOjV6OEK1OVA>
MV411 NGfiOYNCeG:ydH;zbZMhSXO|YYm= M2nUVlMxNzhyL{G1NE8zPTBibl2= NWLNc3NNOjRxNEivO|IhcA>? NF7lRVBqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> M1LoSFI2QDh{NUWw
MGC-803 MmfUR4VtdCCYaXHibYxqfHliQYPzZZk> M36yPVAvOS1zMECwJI5O NHLxd4U4OiCq MonsbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MUOyOVU6ODhyNR?=
SGC-7901 M3;0O2NmdGxiVnnhZoltcXS7IFHzd4F6 NFrPU4gxNjFvMUCwNEBvVQ>? NWHod41nPzJiaB?= M1HyWolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NVnjcIJNOjV3OUC4NFU>
MKN-28 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWCwMlEuOTByMDDuUS=> NILp[4Q4OiCq MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2fDVFI2PTlyOEC1
MGC-803 M4HDPWZ2dmO2aX;uJGF{e2G7 NFLOVW8xNjFvMUCwNEBvVQ>? NVmy[Zp2OjRiaB?= NV3C[HZLcW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 M1\2RlI2PTlyOEC1
HCT-116 M{i2UWZ2dmO2aX;uJGF{e2G7 MYC1NI5O MnTONlQhcA>? NIXFdJpFVVOR MYfpcoR2[2WmIFewM2cyKGG{cnXzeC=> M2rob|I2OjFyN{m0
HT-29 M4rHVmZ2dmO2aX;uJGF{e2G7 MWe1NI5O MoSxNlQhcA>? M4rJeWROW09? MX3pcoR2[2WmIFewM2cyKGG{cnXzeC=> NH;wRoozPTJzMEe5OC=>
SCC25 NIn5bFlEgXSxeHnjbZR6KEG|c3H5 NGD5T2IyOC93MDDuUS=> NUTkcnVvOjRiaB?= NHzEcZhl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NVLuZWluOjV{MEW0N|A>
FUDA MmPlR5l1d3irY3n0fUBCe3OjeR?= NH\0TXgyOC93MDDuUS=> MUmyOEBp MnrR[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M2rDbVI2OjB3NEOw
Detroit562 NHzj[WNEgXSxeHnjbZR6KEG|c3H5 M3e0S|ExNzVyIH7N NGnD[GYzPCCq NYTkOWpL\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MY[yOVIxPTR|MB?=
CAL27 MXnDfZRwgGmlaYT5JGF{e2G7 NUnvbnM5OTBxNUCgcm0> M4\KPFI1KGh? MoDt[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MXGyOVIxPTR|MB?=
DSH1 NGnFdW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P5NGlEPTB;NjDuUS=> NULU[|I1OjR5OES4N|k>
SW-1710 NX;jNFF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jyeWlEPTB;NjDuUS=> MkfVNlQ4QDR6M{m=
T24 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PiXGlEPTB;NzDuUS=> NIPBSoEzPDd6NEizPS=>
RT112 NEC1fGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjUc|VJUUN3ME25JI5O NVvGfnMxOjR5OES4N|k>
639-V MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFWyZ|ZKSzVyPUGwJI5O M1u4VFI1Pzh2OEO5
SCaBER MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFyIH7N MoTLNlQ4QDR6M{m=
BFTC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi3TpJKSzVyPUG3JI5O NEDKboQzPDd6NEizPS=>
J82 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF6IH7N NUfyTYE6OjR5OES4N|k>
HT-1376 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH3WFhkUUN3ME2yNUBvVQ>? Ml;iNlQ4QDR6M{m=
647-V NEXRZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\aTWM2OD1{NzDuUS=> M2e4NlI1Pzh2OEO5
UM-UC3 NFTZWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnZNoZuUUN3ME2zN{BvVQ>? NUe1fpJTOjR5OES4N|k>
LB831-BLC MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfsT5k3UUN3ME2zOEBvVQ>? MYGyOFc5PDh|OR?=
KU-19-19 MnLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfMOohKSzVyPUO2JI5O M4\xd|I1Pzh2OEO5
35612 M{SyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTN6IH7N NV3WR2FqOjR5OES4N|k>
5637 NHvYb2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H1WmlEPTB;NESgcm0> NWDLZ3BKOjR5OES4N|k>
HT-1197 M2T6Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTV|IH7N MVqyOFc5PDh|OR?=
MGH-U3 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFOwXW1KSzVyPUWzJI5O NY\jeIlQOjR5OES4N|k>
TCCSUP MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK3TWM2OD1zNEKgcm0> NV3ZVHM1OjR5OES4N|k>
RT4 M2Xz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DwXGlEPTB;MUezN{BvVQ>? MXqyOFc5PDh|OR?=
SW780 NHjPcHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3T5TmlEPTB;M{S1NUBvVQ>? NXnIVoU1OjR5OES4N|k>
RKO MoT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrW[VFqUUN3ME20JI5O M3G0ZVI1Pjh{N{S3
LS-411 N NEH0Rm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknOTWM2OD13IH7N MVuyOFY5Ojd2Nx?=
SW620 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRThibl2= NFn3S20zPDZ6Mke0Oy=>
HCT-15 M3XNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnUOpJTUUN3ME24JI5O M3LweVI1Pjh{N{S3
HuTu-80 MnHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF|IH7N NWPDUWJLOjR4OEK3OFc>
HCT 116 M1XZemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LyeWlEPTB;MUSgcm0> M1PkUFI1Pjh{N{S3
COLO-205 NY\PWpg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDuTWM2OD1zNDDuUS=> MnzDNlQ3QDJ5NEe=
NCI-H747 NUTQW412T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3qfJhFUUN3ME2xO{BvVQ>? M4rHfFI1Pjh{N{S3
COLO-678 NIjKe3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n0UGlEPTB;MkGgcm0> NGq4Ro8zPDZ6Mke0Oy=>
LoVo NE\aW4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTJ{IH7N MnfBNlQ3QDJ5NEe=
LS-1034 NHf2VW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XvfWlEPTB;M{Ggcm0> MmXUNlQ3QDJ5NEe=
SNU-C2B M3;JSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjSTHlKSzVyPUS1JI5O MX2yOFY5Ojd2Nx?=
LS-123 NGTXZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfMfYlrUUN3ME23N{BvVQ>? M2jNclI1Pjh{N{S3
SK-CO-1 NXPuO3I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W5R2lEPTB;OEGgcm0> NH\OOpMzPDZ6Mke0Oy=>
HCC2998 MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjJT|hlUUN3ME2xNlghdk1? MWmyOFY5Ojd2Nx?=
MDA-MB-231 NH\RbHNHfW6ldHnvckBCe3OjeR?= MY[xNFAhdk1? NVvHcmhlOzBibXnu MWLpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MXeyOFI1QDJ4NR?=
MDA-MB-435 MX;GeY5kfGmxbjDBd5NigQ>? MVGxNFAhdk1? M4HvXFMxKG2rbh?= MXzpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MmO3NlQzPDh{NkW=
BT-20  MXHGeY5kfGmxbjDBd5NigQ>? NXzIcmx2OTByL{K1NEBvVQ>? NYD6RWNZOjRiaB?= MnLMdoV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH M33yOlI1OTd|NUSx
MDA-MB-231 NUTXU5NoTnWwY4Tpc44hSXO|YYm= MkHBNVAxKG6P Mn;kNlQhcA>? NV;zW5l7cW6qaXLpeJMhfGinIH3p[5JifG:{eTDhcoQhcW64YYPpeoUh[2GyYXPpeJnDqA>? NGfid4UzPDF5M{W0NS=>
H82 M{TpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNyLkK3JI5O NFzVbpczPDF4NkWwOS=>
GLC4 NVTtUHlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHZSWcyUUN3ME2yNE41PyCwTR?= M3r1N|I1OTZ4NUC1
H69 NGr1O2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW1UnFKSzVyPUizMlM3KG6P M2e1dlI1OTZ4NUC1
H128 NWjySHJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OwSmlEPTB;NkmuOVUhdk1? MkjONlQyPjZ3MEW=
H146 NHXNNZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\VTWM2OD1{OD61NUBvVQ>? NFLse3YzPDF4NkWwOS=>
H187 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\Z[VBKSzVyPUK0Mlk6KG6P NH\xRo0zPDF4NkWwOS=>
H526 NXrrSJFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LYRWlEPTB;MkGuOlQhdk1? MXiyOFE3PjVyNR?=
N592 NUDTdI5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\xfmlEPTB;MUSuNVIhdk1? NUTWcGV7OjRzNk[1NFU>
H620 NH3RS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXB[HpnUUN3ME2zNk43PyCwTR?= NE\DXpEzPDF4NkWwOS=>
H792 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfFS3VKSzVyPUS1MlA4KG6P Mn[wNlQyPjZ3MEW=
H1173 NGfHOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;qWGlEPTB;MUKuOlIhdk1? NVHLXW83OjRzNk[1NFU>
AC3 NGC2UHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XidGlEPTB;MkWuPUBvVQ>? NEnGWG4zPDF4NkWwOS=>
H82 MkTiSpVv[3Srb36gRZN{[Xl? M2XIXlMxKG6P NWLEcVhiPzJiaB?= MYHpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= Mm[0NlQyPjZ3MEW=
GLC4 MmnUSpVv[3Srb36gRZN{[Xl? M334SlMxKG6P NH7oV4I4OiCq NILpRnZqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MnLxNlQyPjZ3MEW=
H146  M2nvdWZ2dmO2aX;uJGF{e2G7 M3Hy[VMxKG6P NIPKXoo4OiCq M2Lrb4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> NEPXZpUzPDF4NkWwOS=>
OVCAR-5 NEPFV3BE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXGwMVExODBibl2= MoHKO|IhcA>? NVXaTlAxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3vjSFI{QTByMUO2
OVCAR-8 NHuxXVJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIr6NnAxNTFyMECgcm0> MkDkO|IhcA>? NW[5RZNpcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Ml7FNlM6ODBzM{[=
A1847 NGTnV2RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1XselAuOTByMDDuUS=> NWPjTm1oPzJiaB?= NVv5R2g6cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4nrXVI{QTByMUO2
SKOV-3 MnHaR4VtdCCYaXHibYxqfHliQYPzZZk> M2j2XVAuOTByMDDuUS=> NHfvO2Q4OiCq NVO1b45LcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NFq0[4czOzlyMEGzOi=>
OVCAR-5 NWrxXnh7SXCxcITvd4l{KEG|c3H5 MYGxNE0yODBibl2= MUOyOE81QC95MjDo NEfBZ|ZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MYiyN|kxODF|Nh?=
OVCAR-8 M2\PXmFxd3C2b4Ppd{BCe3OjeR?= NVHkR3dZOTBvMUCwJI5O MXKyOE81QC95MjDo M363XIlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= M2HvdlI{QTByMUO2
A1847 MVPBdI9xfG:|aYOgRZN{[Xl? M3TWUFExNTFyMDDuUS=> MlH1NlQwPDhxN{KgbC=> MnPqbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NV\nT|dzOjN7MECxN|Y>
H2228 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUPQcYpvOC1zMECwJI5O NXK4[3o1PzJiaB?= MVHJR|UxRTF|IH7N NUfoRVREOjN3M{OyOlU>
H3122 MljqR4VtdCCYaXHibYxqfHliQYPzZZk> NHrGS4gxNTFyMECgcm0> NWfiNZR1PzJiaB?= MkXNTWM2OD1zMDDuUS=> M1f1flI{PTN|Mk[1
K008 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVjJR|UxRTZyIH7N MVSyN|QyQDV{Mx?=
K028 NUjCeZk3S2WubDDWbYFjcWyrdImgRZN{[Xl? M1LhfWlEPTB;OESgcm0> NWOyZndUOjN2MUi1NlM>
K029 M2PSRmNmdGxiVnnhZoltcXS7IFHzd4F6 M{jwfWlEPTB;NE[gcm0> MX2yN|QyQDV{Mx?=
M23 M3vWS2NmdGxiVnnhZoltcXS7IFHzd4F6 MV3JR|UxRTN5LkWgcm0> NGr0Tm0zOzRzOEWyNy=>
K033 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYDzOoVIUUN3ME23OU42KG6P M2H1V|I{PDF6NUKz
K008 MV;GeY5kfGmxbjDBd5NigQ>? NYPB[HIyOjVyIH7N NXf1N5lbOjRiaB?= MkLlbY5lfWOnczDHNkBienKnc4S= NVP1UopxOjN2MUi1NlM>
K028 MXLGeY5kfGmxbjDBd5NigQ>? MkDXNlUxKG6P NGDEcmMzPCCq MYXpcoR2[2W|IFeyJIFzemW|dB?= NWTKZWhzOjN2MUi1NlM>
K029 NX;BTVE4TnWwY4Tpc44hSXO|YYm= NXX3WXQ2OjVyIH7N MkfQNlQhcA>? M3nQSolv\HWlZYOgS|Eh[XK{ZYP0 M1Lic|I{PDF6NUKz
M23 MWDGeY5kfGmxbjDBd5NigQ>? MW[yOVAhdk1? NIXzNpIzPCCq NUjl[oFVcW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> NUTpNJRjOjN2MUi1NlM>
K033 MkPTSpVv[3Srb36gRZN{[Xl? Mnf5NlUxKG6P Mn3tNlQhcA>? MUTpcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? NXj5cWd7OjN2MUi1NlM>
K008 MYHBdI9xfG:|aYOgRZN{[Xl? M{nOdFExOCCwTR?= M1LHc|czKGh? MmXBd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NXTMbXZHOjN2MUi1NlM>
K028 NFO0eYRCeG:ydH;zbZMhSXO|YYm= NFnwSHAyODBibl2= MmnrO|IhcA>? MXTzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ M4PxT|I{PDF6NUKz
K029 NF[yN3NCeG:ydH;zbZMhSXO|YYm= MofMNVAxKG6P M{LuTFczKGh? NHvwR2t{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MnHFNlM1OTh3MkO=
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SJ-GBM2 M2rHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zzd2lEPTB;MUKuPUBvVQ>? NUfQW24zOjN|MEO3OFE>
NB-1643 MnjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLPWVhtUUN3ME23MlQhdk1? NHLnTG4zOzNyM{e0NS=>
NB-EBc1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T2[GlEPTB;MU[uPEBvVQ>? Mn;ENlM{ODN5NEG=
CHLA-90 M17POmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTpTWM2OD1{Mj6zJI5O MoDCNlM{ODN5NEG=
CHLA-136 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\ZemlEPTB;MkOuNkBvVQ>? M3vBU|I{OzB|N{Sx
NALM-6 NIHhS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFzLkegcm0> NHfJbVIzOzNyM{e0NS=>
COG-LL-317 NV71c2x3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTaNI9KSzVyPUSuOEBvVQ>? NYfhNGVTOjN|MEO3OFE>
RS4;11 M1z3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP1XoRpUUN3ME2xN{42KG6P M4\pb|I{OzB|N{Sx
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CCRF-CEM (1) MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TZNmlEPTB;MUKuOUBvVQ>? NE\5[4YzOzNyM{e0NS=>
CCRF-CEM (2) MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\QTWM2OD15LkKgcm0> Mk\ENlM{ODN5NEG=
Kasumi-1 M{nRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MomwTWM2OD13Lkigcm0> NI\qTFIzOzNyM{e0NS=>
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HOP-62 MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD2UIw4UUN3ME2xNUBvVQ>? MWGyN|AyOjJ2OB?=
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H1792 NIjhdmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTNTWM2OD1{MDDuUS=> M4TYc|I{ODF{MkS4
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H727 MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHINnYxUUN3ME2yPEBvVQ>? M3zEUFI{ODF{MkS4
H1734 M4HZcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfRN4lKSzVyPUK4JI5O MX:yN|AyOjJ2OB?=
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A549 M2HTfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13WN2lEPTB;NEOgcm0> MmfENlMxOTJ{NEi=
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NCI-H1975 NXz3SHRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojBOFghcA>? MVLJR|UxRTF4IH7N NFf1[m4zOjF2NE[2OS=>
NCI-H1975 M1rQU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\lb4c4OiCq MXXJR|UxRThibl2= NIHOenEzOjF2NE[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).

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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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