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.

Size Price Stock Quantity  
In DMSO USD 302 In stock
USD 270 In stock
USD 370 In stock

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  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MnXNRZBweHSxc3nzJGF{e2G7 MlyxN|AwQDBxMUWwM|I2OCCwTR?= MYWyOE81QC95MjDo NV\sN2FpcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ NGfRSXczPTh6MkW1NC=>
MV411 MWTBdI9xfG:|aYOgRZN{[Xl? MVqzNE85OC9zNUCvNlUxKG6P M3j6clI1NzR6L{eyJIg> NVrIZ|E2cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ NHToRm0zPTh6MkW1NC=>
MGC-803 NYrJUXhWS2WubDDWbYFjcWyrdImgRZN{[Xl? MkXkNE4yNTFyMECgcm0> MnzlO|IhcA>? NFPVW4VqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoH2NlU2QTB6MEW=
SGC-7901 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXiwMlEuOTByMDDuUS=> NX3KflNNPzJiaB?= M{PZZ4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MUWyOVU6ODhyNR?=
MKN-28 M162WmNmdGxiVnnhZoltcXS7IFHzd4F6 NGHsNFQxNjFvMUCwNEBvVQ>? MnPPO|IhcA>? M2LCZYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIq5WG0zPTV7MEiwOS=>
MGC-803 M{[zUmZ2dmO2aX;uJGF{e2G7 NEDUNZIxNjFvMUCwNEBvVQ>? MlLGNlQhcA>? M1O5Xolv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? NV\nTpVCOjV3OUC4NFU>
HCT-116 NIL2cIZHfW6ldHnvckBCe3OjeR?= NXLIRYFwPTCwTR?= M3WxeVI1KGh? NULORpAyTE2VTx?= NWS0[3FNcW6mdXPl[EBIOC:JMTDhdpJme3R? NFi3eYczPTJzMEe5OC=>
HT-29 MV3GeY5kfGmxbjDBd5NigQ>? MlX5OVBvVQ>? Mn3tNlQhcA>? MnTBSG1UVw>? NIXqNJZqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MX6yOVIyODd7NB?=
SCC25 NHLCXItEgXSxeHnjbZR6KEG|c3H5 NXfBeFdKOTBxNUCgcm0> MkHiNlQhcA>? M3;VcoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MWOyOVIxPTR|MB?=
FUDA M3;td2N6fG:6aXPpeJkhSXO|YYm= NGPPWJAyOC93MDDuUS=> M4XBfFI1KGh? NVHJO2JQ\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MYqyOVIxPTR|MB?=
Detroit562 MXLDfZRwgGmlaYT5JGF{e2G7 NXHKRWNGOTBxNUCgcm0> NUW1T5pnOjRiaB?= NUHrWYYx\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MkLUNlUzODV2M{C=
CAL27 NYPsN5lmS3m2b4jpZ4l1gSCDc4PhfS=> Mk\INVAwPTBibl2= MVyyOEBp M2fjcYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MoLlNlUzODV2M{C=
DSH1 NX:1[os1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSTWM2OD14IH7N NV3VTmVsOjR5OES4N|k>
SW-1710 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3STWM2OD14IH7N MYmyOFc5PDh|OR?=
T24 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTdibl2= NUTz[3BEOjR5OES4N|k>
RT112 NEfKN2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTlibl2= MmHzNlQ4QDR6M{m=
639-V NUDQU5h5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPETWM2OD1zMDDuUS=> NUCwfoxZOjR5OES4N|k>
SCaBER NGq0S5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP0TWM2OD1zMDDuUS=> MorZNlQ4QDR6M{m=
BFTC NITXeHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq2XmpKSzVyPUG3JI5O NV63cFVvOjR5OES4N|k>
J82 NFrnNYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe2Z3RKSzVyPUG4JI5O NIPjPZgzPDd6NEizPS=>
HT-1376 NEnGWndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXiz[HgyUUN3ME2yNUBvVQ>? M3Htd|I1Pzh2OEO5
647-V NYTwZ49HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\MR3JKSzVyPUK3JI5O NH7VOpgzPDd6NEizPS=>
UM-UC3 M2HnRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljlTWM2OD1|MzDuUS=> M4rZXVI1Pzh2OEO5
LB831-BLC NGrMcZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;oOYtKSzVyPUO0JI5O MXqyOFc5PDh|OR?=
KU-19-19 NW\EVZVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN4IH7N MnHqNlQ4QDR6M{m=
35612 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\QeFhvUUN3ME2zPEBvVQ>? Ml6zNlQ4QDR6M{m=
5637 NF3NZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3YPHhKSzVyPUS0JI5O MVSyOFc5PDh|OR?=
HT-1197 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTV|IH7N M{jaSlI1Pzh2OEO5
MGH-U3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnYXZlKSzVyPUWzJI5O NI\F[mkzPDd6NEizPS=>
TCCSUP NX\6OlhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrjOmRKSzVyPUG0NkBvVQ>? M3yzTlI1Pzh2OEO5
RT4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjYTWM2OD1zN{OzJI5O MnfYNlQ4QDR6M{m=
SW780 NYfXfYV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\oR2FKSzVyPUO0OVEhdk1? MonHNlQ4QDR6M{m=
RKO Mn3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37qSmlEPTB;NDDuUS=> MWeyOFY5Ojd2Nx?=
LS-411 N NYDJXJpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\USHduUUN3ME21JI5O MV2yOFY5Ojd2Nx?=
SW620 NIrHdWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjrdphKSzVyPUigcm0> MmrkNlQ3QDJ5NEe=
HCT-15 NYKyVXRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fMTWlEPTB;ODDuUS=> MojhNlQ3QDJ5NEe=
HuTu-80 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTF|IH7N MofVNlQ3QDJ5NEe=
HCT 116 NGPqc3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF2IH7N NVzvfZRKOjR4OEK3OFc>
COLO-205 M{LBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfwOJV5UUN3ME2xOEBvVQ>? MX[yOFY5Ojd2Nx?=
NCI-H747 NUfzN|JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTF5IH7N M1jBU|I1Pjh{N{S3
COLO-678 NGHnPWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDobo1KSzVyPUKxJI5O Mnq4NlQ3QDJ5NEe=
LoVo M{HOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjoVllCUUN3ME2yNkBvVQ>? M{[2T|I1Pjh{N{S3
LS-1034 NUDhcW11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrQ[ndKSzVyPUOxJI5O Ml\RNlQ3QDJ5NEe=
SNU-C2B NX;tblRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjsPZBuUUN3ME20OUBvVQ>? MnS2NlQ3QDJ5NEe=
LS-123 NIHlfmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIL5OVlKSzVyPUezJI5O NInxUHkzPDZ6Mke0Oy=>
SK-CO-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnxTWM2OD16MTDuUS=> MnzDNlQ3QDJ5NEe=
HCC2998 M{Gyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF{ODDuUS=> NFfhW5ozPDZ6Mke0Oy=>
MDA-MB-231 MmXjSpVv[3Srb36gRZN{[Xl? M2PwfFExOCCwTR?= MYmzNEBucW5? NIT6e2xqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NYX4NHkxOjR{NEiyOlU>
MDA-MB-435 MkL4SpVv[3Srb36gRZN{[Xl? M1rTR|ExOCCwTR?= MmC4N|AhdWmw NGDxRXRqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NYrqbIlZOjR{NEiyOlU>
BT-20  NWfoV3lyTnWwY4Tpc44hSXO|YYm= M1v5cVExOC9{NUCgcm0> NFTSUmozPCCq MXjy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY> M3jiNVI1OTd|NUSx
MDA-MB-231 NX76cnZuTnWwY4Tpc44hSXO|YYm= NGTSdVkyODBibl2= M3OyPVI1KGh? NGCw[IRqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh MlrPNlQyPzN3NEG=
H82 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPhTWM2OD1|MD6yO{BvVQ>? Mo\ENlQyPjZ3MEW=
GLC4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPMNGFKSzVyPUKwMlQ4KG6P MknsNlQyPjZ3MEW=
H69 M1\ITWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTh|LkO2JI5O NIq2Nm0zPDF4NkWwOS=>
H128 Ml[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzhVZp6UUN3ME22PU42PSCwTR?= M4P3OFI1OTZ4NUC1
H146 MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJ6LkWxJI5O MXOyOFE3PjVyNR?=
H187 NVO3VmhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3G5VmlEPTB;MkSuPVkhdk1? NX:4dHlbOjRzNk[1NFU>
H526 MlXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFW4WpdKSzVyPUKxMlY1KG6P NEHabIQzPDF4NkWwOS=>
N592 M2S0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnLfGJKSzVyPUG0MlEzKG6P MV2yOFE3PjVyNR?=
H620 MkW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvFV3lKSzVyPUOyMlY4KG6P MkixNlQyPjZ3MEW=
H792 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7BTWM2OD12NT6wO{BvVQ>? NInXWJYzPDF4NkWwOS=>
H1173 MmHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTF{Lk[yJI5O MXqyOFE3PjVyNR?=
AC3 M{PtR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJ3Lkmgcm0> M3rITVI1OTZ4NUC1
H82 MlLiSpVv[3Srb36gRZN{[Xl? Mn7WN|Ahdk1? NVraOno{PzJiaB?= MYrpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= M1ToW|I1OTZ4NUC1
GLC4 M{HNVmZ2dmO2aX;uJGF{e2G7 NE\KdHU{OCCwTR?= M{jkdFczKGh? M3Haeolv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M3fxPVI1OTZ4NUC1
H146  Mk\CSpVv[3Srb36gRZN{[Xl? NVvpZWQ1OzBibl2= NYDtUY5uPzJiaB?= MnnqbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 MUSyOFE3PjVyNR?=
OVCAR-5 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYmz[4NCOC1zMECwJI5O NEDFVpQ4OiCq MoSybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NHe2cYszOzlyMEGzOi=>
OVCAR-8 M{D3NmNmdGxiVnnhZoltcXS7IFHzd4F6 Mn31NE0yODByIH7N MUC3NkBp NXGw[mNycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnHtNlM6ODBzM{[=
A1847 Moj3R4VtdCCYaXHibYxqfHliQYPzZZk> NX;FU3RjOC1zMECwJI5O NX\H[4hSPzJiaB?= NXvpfYVUcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MlXKNlM6ODBzM{[=
SKOV-3 NI\IbXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mnu5NE0yODByIH7N MVK3NkBp NHfYN2ZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MYqyN|kxODF|Nh?=
OVCAR-5 MX\BdI9xfG:|aYOgRZN{[Xl? MYmxNE0yODBibl2= NFTzRWozPC92OD:3NkBp M2\LXolv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MknxNlM6ODBzM{[=
OVCAR-8 MoLmRZBweHSxc3nzJGF{e2G7 MofLNVAuOTByIH7N NFLKN2ozPC92OD:3NkBp NYm2SZJocW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> NX:1SmVxOjN7MECxN|Y>
A1847 NEP6cY1CeG:ydH;zbZMhSXO|YYm= NF2zb3YyOC1zMECgcm0> Mnr4NlQwPDhxN{KgbC=> NGfETIhqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 M3q4XlI{QTByMUO2
H2228 NHz3O2VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGC5dm8xNTFyMECgcm0> NV\hO5RCPzJiaB?= MkfiTWM2OD1zMzDuUS=> MkTYNlM2OzN{NkW=
H3122 NUHnSWd[S2WubDDWbYFjcWyrdImgRZN{[Xl? MUWwMVExODBibl2= MWW3NkBp M2faXmlEPTB;MUCgcm0> MlfPNlM2OzN{NkW=
K008 MknhR4VtdCCYaXHibYxqfHliQYPzZZk> Ml7VTWM2OD14MDDuUS=> M3Pn[FI{PDF6NUKz
K028 Mn;hR4VtdCCYaXHibYxqfHliQYPzZZk> MX3JR|UxRTh2IH7N MlTPNlM1OTh3MkO=
K029 NHPnOGFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXrGflFSUUN3ME20OkBvVQ>? NG[wTZAzOzRzOEWyNy=>
M23 MkPuR4VtdCCYaXHibYxqfHliQYPzZZk> NH7CbIdKSzVyPUO3MlUhdk1? NHe1O2IzOzRzOEWyNy=>
K033 NHTOUIFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3;MemlEPTB;N{WuOUBvVQ>? NYfn[5RmOjN2MUi1NlM>
K008 M3jIVWZ2dmO2aX;uJGF{e2G7 MUmyOVAhdk1? M{\OXVI1KGh? MWjpcoR2[2W|IFeyJIFzemW|dB?= NEXKPGIzOzRzOEWyNy=>
K028 NGLjd4hHfW6ldHnvckBCe3OjeR?= M3q0dlI2OCCwTR?= NHfDco8zPCCq NV7KT3h1cW6mdXPld{BIOiCjcoLld5Q> MoXINlM1OTh3MkO=
K029 NIWycHFHfW6ldHnvckBCe3OjeR?= MVOyOVAhdk1? NFXyOXYzPCCq M1T2colv\HWlZYOgS|Eh[XK{ZYP0 NEnKR|UzOzRzOEWyNy=>
M23 MVTGeY5kfGmxbjDBd5NigQ>? MkjhNlUxKG6P MYiyOEBp NIO5c5dqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> NFrzRlMzOzRzOEWyNy=>
K033 M2LIR2Z2dmO2aX;uJGF{e2G7 NGLSSWYzPTBibl2= NG\MUY8zPCCq NWnOZYd6cW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u MWCyN|QyQDV{Mx?=
K008 NUHvbI5VSXCxcITvd4l{KEG|c3H5 NGTSV4cyODBibl2= M3XtSFczKGh? NFjGUHR{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NImyOYIzOzRzOEWyNy=>
K028 MUHBdI9xfG:|aYOgRZN{[Xl? NX;qS4JqOTByIH7N M4nIdFczKGh? NFrmXWp{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MoD0NlM1OTh3MkO=
K029 M{\YTWFxd3C2b4Ppd{BCe3OjeR?= Ml[5NVAxKG6P M2nnZ|czKGh? NIrBbIh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MXeyN|QyQDV{Mx?=
M23 NGXHfGNCeG:ydH;zbZMhSXO|YYm= NHG3clUyODBibl2= MXq3NkBp M{TQ[ZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MXeyN|QyQDV{Mx?=
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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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+45% PEG 300+ddH2O 11mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C4=C3/X C4: LOG(C4):
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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
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID