Ganetespib (STA-9090)

For research use only. Not for use in humans.

目录号：S1159

Ganetespib (STA-9090) Chemical Structure

Molecular Weight(MW): 364.4

Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2472.01 现货
RMB 2187.96 现货
RMB 3025.86 现货
RMB 8763.3 现货
RMB 20229.3 现货
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客户使用Selleck生产的Ganetespib (STA-9090)发表文献31篇：

产品安全说明书

HSP (e.g. HSP90)抑制剂选择性比较

生物活性

产品描述 Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。
靶点
HSP90 [1]
(OSA 8 cells)
4 nM
体外研究

Ganetespib对恶性肥大细胞系的50%抑制浓度(IC50)比对17-AAG低10-15倍，表明三唑酮类HSP90抑制剂可能比格尔德霉素类抑制剂具有更高的效能。[1] Ganetespib抑制MG63细胞系，IC50为43 nM。[1] Ganetespib结合于Hsp90的N末端ATP结合域，通过引起多重致瘤性Hsp90受体蛋白，包括HER2/neu，突变型EGFR，Akt，c-Kit，IGF-1R，PDGFRα，Jak1，Jak2，STAT3，STAT5，HIF-1α，CDC2和c-Met 以及Wilms' tumor 1的降解，成为一种有效的Hsp90的抑制剂。[2] Ganetespib，在纳摩尔级低浓度下，有效阻滞细胞增殖，并诱导广泛的人肿瘤细胞系凋亡，并且对许多受体酪氨酸激酶抑制剂-和tanespimycin-耐受的细胞系也具有作用。Ganetespib在一系列固体和血液肿瘤细胞系，包括那些对小分子酪氨酸激酶抑制剂耐受的表达突变激酶的细胞系，都表现出有效的细胞毒性。[3] Ganetespib治疗快速引起已知的Hsp90受体蛋白降解，表现出高于ansamycin抑制剂17-AAG的效能，并且在较短的暴露时间下也具有持续的活性。[3]在另一个研究中，Ganetespib诱导恶性犬肥大细胞系凋亡。Ganetespib在非常低的浓度下，有效作用于C2和BR犬恶性肥大细胞，IC50分别为19和4 nM，而17-AAG抑制C2和BR犬恶性肥大细胞的IC50分别为958和44 nM。[4]100 nM Ganetespib处理24小时后，所有处理过的细胞系，包括C2和BMCMCs细胞中WT和突变型Kit的表达被下调。然而，Ganetespib处理后不影响PI3K或HSP90的表达。[4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 MnT5RZBweHSxc3nzJGF{e2G7 M1v4W|MxNzhyL{G1NE8zPTBibl2= NH20dZozPC92OD:3NkBp NVr2ZYd[cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MljtNlU5QDJ3NUC=
MV411 MWHBdI9xfG:|aYOgRZN{[Xl? MWSzNE85OC9zNUCvNlUxKG6P MVWyOE81QC95MjDo M{GwNYlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> MnjNNlU5QDJ3NUC=
MGC-803 NIPuZZlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEPXOI0xNjFvMUCwNEBvVQ>? MnHPO|IhcA>? NYfQNWNvcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3fTS|I2PTlyOEC1
SGC-7901 NFXWO2lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MojONE4yNTFyMECgcm0> NGfxT3U4OiCq NWDOWGNvcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWD6U2RFOjV3OUC4NFU>
MKN-28 MmnER4VtdCCYaXHibYxqfHliQYPzZZk> NHXkZVQxNjFvMUCwNEBvVQ>? MmfBO|IhcA>? NIHqT45qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoP6NlU2QTB6MEW=
MGC-803 MmntSpVv[3Srb36gRZN{[Xl? MVewMlEuOTByMDDuUS=> MkS3NlQhcA>? MUDpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> MUmyOVU6ODhyNR?=
HCT-116 NIrxeWpHfW6ldHnvckBCe3OjeR?= NWHKWIlHPTCwTR?= NU[4fVdoOjRiaB?= MlzESG1UVw>? NWfUOnVlcW6mdXPl[EBIOC:JMTDhdpJme3R? NWDyTJUyOjV{MUC3PVQ>
HT-29 MlXLSpVv[3Srb36gRZN{[Xl? M1jZelUxdk1? MV[yOEBp MknBSG1UVw>? NGjTTnBqdmS3Y3XkJGcxN0dzIHHydoV{fA>? MYOyOVIyODd7NB?=
SCC25 MW\DfZRwgGmlaYT5JGF{e2G7 NVi5PWxSOTBxNUCgcm0> MXiyOEBp M3\QRYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M3zNWVI2OjB3NEOw
FUDA MX7DfZRwgGmlaYT5JGF{e2G7 M3[2ZlExNzVyIH7N NY\oOVZROjRiaB?= MnjN[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MVqyOVIxPTR|MB?=
Detroit562 MoqzR5l1d3irY3n0fUBCe3OjeR?= MknwNVAwPTBibl2= NXLEUmR1OjRiaB?= NVvPTnR1\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MXKyOVIxPTR|MB?=
CAL27 M3viSmN6fG:6aXPpeJkhSXO|YYm= MVyxNE82OCCwTR?= MmjGNlQhcA>? NIWwclZl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NGjzXJYzPTJyNUSzNC=>
DSH1 NGnLbW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFOzSXNKSzVyPU[gcm0> Mnn6NlQ4QDR6M{m=
SW-1710 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLkZplJUUN3ME22JI5O NFnlTZgzPDd6NEizPS=>
T24 NHi0[lNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjSTWM2OD15IH7N M2DISFI1Pzh2OEO5
RT112 Mm[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXaXotKSzVyPUmgcm0> MVWyOFc5PDh|OR?=
639-V MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDBTWM2OD1zMDDuUS=> MUSyOFc5PDh|OR?=
SCaBER MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M363SmlEPTB;MUCgcm0> MYKyOFc5PDh|OR?=
BFTC MorkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fUT2lEPTB;MUegcm0> M3nxTVI1Pzh2OEO5
J82 NFfafG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrNTWM2OD1zODDuUS=> MknoNlQ4QDR6M{m=
HT-1376 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\BfodKSzVyPUKxJI5O NWnm[3RLOjR5OES4N|k>
647-V MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn0VmsyUUN3ME2yO{BvVQ>? MX:yOFc5PDh|OR?=
UM-UC3 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX63bY1RUUN3ME2zN{BvVQ>? MoDTNlQ4QDR6M{m=
LB831-BLC M4fWR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnkNnRGUUN3ME2zOEBvVQ>? MVyyOFc5PDh|OR?=
KU-19-19 M3\WW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL2OVdDUUN3ME2zOkBvVQ>? MlzLNlQ4QDR6M{m=
35612 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M12yZmlEPTB;M{igcm0> MmPQNlQ4QDR6M{m=
5637 M4PMUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TlTGlEPTB;NESgcm0> M3[3SVI1Pzh2OEO5
HT-1197 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LQNWlEPTB;NUOgcm0> MkfPNlQ4QDR6M{m=
MGH-U3 M4PmXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj2OYM6UUN3ME21N{BvVQ>? Ml;CNlQ4QDR6M{m=
TCCSUP NHjJ[oJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TLVWlEPTB;MUSyJI5O M{nYNlI1Pzh2OEO5
RT4 NYi2V2t5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjhTVN6UUN3ME2xO|M{KG6P NFfQW|MzPDd6NEizPS=>
SW780 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1u3[mlEPTB;M{S1NUBvVQ>? M3HDcVI1Pzh2OEO5
RKO MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHGNlJKSzVyPUSgcm0> NGjGRmgzPDZ6Mke0Oy=>
LS-411 N Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[wN3Y2UUN3ME21JI5O NVrwdnBNOjR4OEK3OFc>
SW620 NGnzPVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PIOWlEPTB;ODDuUS=> NYr0Tnp6OjR4OEK3OFc>
HCT-15 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRThibl2= NYOwV3dFOjR4OEK3OFc>
HuTu-80 M12wU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrrTFZKSzVyPUGzJI5O M{HFZ|I1Pjh{N{S3
HCT 116 M2DZcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK4ZlRZUUN3ME2xOEBvVQ>? NWDxPItQOjR4OEK3OFc>
COLO-205 NFm1RolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3POVGlEPTB;MUSgcm0> MVGyOFY5Ojd2Nx?=
NCI-H747 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILzenFKSzVyPUG3JI5O MXyyOFY5Ojd2Nx?=
COLO-678 NEmxW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJzIH7N NYLPOlBMOjR4OEK3OFc>
LoVo NHPPcHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJ{IH7N NGDpe4YzPDZ6Mke0Oy=>
LS-1034 M3n4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7Xb2VKSzVyPUOxJI5O MlnoNlQ3QDJ5NEe=
SNU-C2B MkLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnv[YY4UUN3ME20OUBvVQ>? NGjFfoozPDZ6Mke0Oy=>
LS-123 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HIT2lEPTB;N{Ogcm0> NX6zXVE1OjR4OEK3OFc>
SK-CO-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDZcItKSzVyPUixJI5O M3XVVlI1Pjh{N{S3
HCC2998 NFv5SnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITG[YlKSzVyPUGyPEBvVQ>? NEnuOZAzPDZ6Mke0Oy=>
MDA-MB-231 M4XVeGZ2dmO2aX;uJGF{e2G7 M3fyXlExOCCwTR?= NUnndpVNOzBibXnu MXPpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NYTJW2FnOjR{NEiyOlU>
MDA-MB-435 M1G2eWZ2dmO2aX;uJGF{e2G7 M37ucVExOCCwTR?= M2TtNVMxKG2rbh?= NUK1fmFZcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= MVeyOFI1QDJ4NR?=
BT-20  M1;FT2Z2dmO2aX;uJGF{e2G7 M{W0dFExOC9{NUCgcm0> NH;1Z2kzPCCq NEKxNo1z\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? NXHWVWJQOjRzN{O1OFE>
MDA-MB-231 NGG1V3NHfW6ldHnvckBCe3OjeR?= NISyVZMyODBibl2= NITqZngzPCCq MmrRbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> NETaNJQzPDF5M{W0NS=>
H82 M2C5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fFVWlEPTB;M{CuNlchdk1? MkfZNlQyPjZ3MEW=
GLC4 NF7ifmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJyLkS3JI5O MWmyOFE3PjVyNR?=
H69 NY\mO4hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTh|LkO2JI5O MVSyOFE3PjVyNR?=
H128 M4nrdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPPUXZCUUN3ME22PU42PSCwTR?= MoPoNlQyPjZ3MEW=
H146 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnwUmZsUUN3ME2yPE42OSCwTR?= NWLpbFdzOjRzNk[1NFU>
H187 M3H2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTFUVVuUUN3ME2yOE46QSCwTR?= NFX2WpczPDF4NkWwOS=>
H526 Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj6d5VKSzVyPUKxMlY1KG6P NFPFS4MzPDF4NkWwOS=>
N592 M1\hbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnOPVdKSzVyPUG0MlEzKG6P MmfsNlQyPjZ3MEW=
H620 Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN{Lk[3JI5O NHTWTYUzPDF4NkWwOS=>
H792 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTR3LkC3JI5O NF\L[nEzPDF4NkWwOS=>
H1173 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF{Lk[yJI5O NG\qSYQzPDF4NkWwOS=>
AC3 NWHhdZFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ3Lkmgcm0> NWC4ZXU{OjRzNk[1NFU>
H82 MoLVSpVv[3Srb36gRZN{[Xl? MYOzNEBvVQ>? NYnxd4xIPzJiaB?= NEHNWJNqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NYDacVRWOjRzNk[1NFU>
GLC4 M{O5d2Z2dmO2aX;uJGF{e2G7 NVvKN5BROzBibl2= MYe3NkBp NYqyU4d4cW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M{TuSlI1OTZ4NUC1
H146  NIrjRXdHfW6ldHnvckBCe3OjeR?= MXWzNEBvVQ>? M2TPOFczKGh? MV;pcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NHTrNo0zPDF4NkWwOS=>
OVCAR-5 M3f1eWNmdGxiVnnhZoltcXS7IFHzd4F6 MmfGNE0yODByIH7N NIrrVGQ4OiCq MXzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MlezNlM6ODBzM{[=
OVCAR-8 NGG2SlFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUG4RYQzOC1zMECwJI5O NGH2U5Y4OiCq NXPoeZZUcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVzTem5DOjN7MECxN|Y>
A1847 NFzHR5NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX\JOGttOC1zMECwJI5O M{LRRVczKGh? MVzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4e5SFI{QTByMUO2
SKOV-3 NWjVcYNbS2WubDDWbYFjcWyrdImgRZN{[Xl? MoK0NE0yODByIH7N M1HsU|czKGh? M3uyb4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MUGyN|kxODF|Nh?=
OVCAR-5 NYOyVlVvSXCxcITvd4l{KEG|c3H5 MXixNE0yODBibl2= MVOyOE81QC95MjDo NHrqdGRqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NHP1SZMzOzlyMEGzOi=>
OVCAR-8 NVz1UYU1SXCxcITvd4l{KEG|c3H5 M4\BSVExNTFyMDDuUS=> M3n2dFI1NzR6L{eyJIg> M1nPdIlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= NFexVWozOzlyMEGzOi=>
A1847 MV\BdI9xfG:|aYOgRZN{[Xl? NEjwSGsyOC1zMECgcm0> NF3FWmMzPC92OD:3NkBp NF;GVY5qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NWi0UXdEOjN7MECxN|Y>
H2228 NYHGU5ZJS2WubDDWbYFjcWyrdImgRZN{[Xl? M4izelAuOTByMDDuUS=> M4O0SlczKGh? NFizbFlKSzVyPUGzJI5O MkfjNlM2OzN{NkW=
H3122 NYiyWmNLS2WubDDWbYFjcWyrdImgRZN{[Xl? NVrRbnpXOC1zMECwJI5O Mk\DO|IhcA>? NGC2XoRKSzVyPUGwJI5O NYHFVolJOjN3M{OyOlU>
K008 NWXwSlhHS2WubDDWbYFjcWyrdImgRZN{[Xl? MUDJR|UxRTZyIH7N MU[yN|QyQDV{Mx?=
K028 NETURYRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFHYeFRKSzVyPUi0JI5O M4TNelI{PDF6NUKz
K029 MkPJR4VtdCCYaXHibYxqfHliQYPzZZk> NYK1UnRXUUN3ME20OkBvVQ>? NUnGfo1YOjN2MUi1NlM>
M23 NFzRSo5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUHJR|UxRTN5LkWgcm0> NIniU5kzOzRzOEWyNy=>
K033 M1HSdGNmdGxiVnnhZoltcXS7IFHzd4F6 MXrJR|UxRTd3LkWgcm0> NV7xemRWOjN2MUi1NlM>
K008 NWXmRYJTTnWwY4Tpc44hSXO|YYm= NX3LeHJEOjVyIH7N Ml;iNlQhcA>? NVW5WZNIcW6mdXPld{BIOiCjcoLld5Q> MWqyN|QyQDV{Mx?=
K028 NVvQRW9oTnWwY4Tpc44hSXO|YYm= NW\yWVNtOjVyIH7N M2fQVFI1KGh? NXz3bWlMcW6mdXPld{BIOiCjcoLld5Q> NVfZWHVWOjN2MUi1NlM>
K029 Mn;USpVv[3Srb36gRZN{[Xl? NXzYeIVQOjVyIH7N MmTsNlQhcA>? M3nWbYlv\HWlZYOgS|Eh[XK{ZYP0 NVnROZk5OjN2MUi1NlM>
M23 MUnGeY5kfGmxbjDBd5NigQ>? MUeyOVAhdk1? NWXu[XpGOjRiaB?= NVO5[pBScW6mdXPld{BIOSCjbnSgS|IwVSCjcoLld5Q> M1HocVI{PDF6NUKz
K033 MoWxSpVv[3Srb36gRZN{[Xl? NIm0coMzPTBibl2= NVnWb4xIOjRiaB?= NE[3SmVqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36= MYOyN|QyQDV{Mx?=
K008 NVX1VWlQSXCxcITvd4l{KEG|c3H5 M4\3elExOCCwTR?= NHHwe3Q4OiCq NF\nbpJ{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NYnJOFNzOjN2MUi1NlM>
K028 MlnYRZBweHSxc3nzJGF{e2G7 NF;VbJoyODBibl2= MkDwO|IhcA>? Ml7kd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NXG1XWlnOjN2MUi1NlM>
K029 M4nlNGFxd3C2b4Ppd{BCe3OjeR?= NGfRdpcyODBibl2= NWfvcXN5PzJiaB?= MUDzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NGjvcIgzOzRzOEWyNy=>
M23 MmPkRZBweHSxc3nzJGF{e2G7 MVmxNFAhdk1? NXfpNFVpPzJiaB?= M2HUSpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M1[w[FI{PDF6NUKz
K033 M3K3bGFxd3C2b4Ppd{BCe3OjeR?= Mn3NNVAxKG6P NULhTmJHPzJiaB?= M2PJSJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NFLWOWozOzRzOEWyNy=>
RD M{HZemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkThTWM2OD16IH7N MmHuNlM{ODN5NEG=
Rh41 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17QdmlEPTB;MUCuOEBvVQ>? NWXYc|ZROjN|MEO3OFE>
Rh18 NFLpNIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nle2lEPTB;Nj6yJI5O MV2yN|MxOzd2MR?=
Rh30 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTVwNjDuUS=> MYCyN|MxOzd2MR?=
BT-12 M4LsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LuT2lEPTB;MUSuN{BvVQ>? MVGyN|MxOzd2MR?=
CHLA-266 M1;hTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPacnRKSzVyPUK3MlEhdk1? MmDYNlM{ODN5NEG=
TC-71 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTRwNTDuUS=> NHTlNHQzOzNyM{e0NS=>
CHLA-9 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfZeYZKUUN3ME20MlYhdk1? M2nKfVI{OzB|N{Sx
CHLA-10 M2DRW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fq[WlEPTB;NT63JI5O M1vLR|I{OzB|N{Sx
CHLA-258 NW\ZSHhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfodHNMUUN3ME22MlQhdk1? MXGyN|MxOzd2MR?=
SJ-GBM2 NUD3XIJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUCyOIdtUUN3ME2xNk46KG6P M3uwNFI{OzB|N{Sx
NB-1643 M1e4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nLOWlEPTB;Nz60JI5O NIX0ZoMzOzNyM{e0NS=>
NB-EBc1 NEXXTXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjPTWM2OD1zNj64JI5O M1XyZlI{OzB|N{Sx
CHLA-90 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTNdGZKSzVyPUKyMlMhdk1? Mk[3NlM{ODN5NEG=
CHLA-136 NEjMcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnDTWM2OD1{Mz6yJI5O NX;4[YtpOjN|MEO3OFE>
NALM-6 NVjVRmtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHVd|hKSzVyPUGxMlchdk1? MVyyN|MxOzd2MR?=
COG-LL-317 M3fqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XhXGlEPTB;ND60JI5O M4n6dVI{OzB|N{Sx
RS4;11 MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF|LkWgcm0> NILxb|UzOzNyM{e0NS=>
MOLT-4 M2Pxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TrWWlEPTB;MUCuOkBvVQ>? NFO0VYgzOzNyM{e0NS=>
CCRF-CEM (1) MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXkeZVKSzVyPUGyMlUhdk1? MWSyN|MxOzd2MR?=
CCRF-CEM (2) MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfRS2NKSzVyPUeuNkBvVQ>? M1nZUlI{OzB|N{Sx
Kasumi-1 NIWwbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTVwODDuUS=> MkXKNlM{ODN5NEG=
Karpas-299 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTlwNjDuUS=> NX3mWFg1OjN|MEO3OFE>
Ramos-RA1 NED0OnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3sNJNnUUN3ME23MlQhdk1? NEXlW3UzOzNyM{e0NS=>
LNCaP M1fyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW1TWM2OD16IH7N MoX2NlMyPTJyMES=
VCaP NVLze4Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTdibl2= NVLvVphXOjNzNUKwNFQ>
H1355 Mkj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nW[mlEPTB;NTDuUS=> Ml3lNlMxOTJ{NEi=
H157 MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTdibl2= NEn3R5EzOzBzMkK0PC=>
H460 NEnwSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3weo1KSzVyPUigcm0> NXTnTmNCOjNyMUKyOFg>
IA-LM MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfXVYxPUUN3ME2xNEBvVQ>? Mnf3NlMxOTJ{NEi=
HOP-62 M2eyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFzIH7N MYmyN|AyOjJ2OB?=
H23 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvvTWM2OD1zMTDuUS=> NVHWcFhxOjNyMUKyOFg>
H2030 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF{IH7N Mk\TNlMxOTJ{NEi=
H441 M2\kcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL1TWM2OD1zNDDuUS=> NEOyNnAzOzBzMkK0PC=>
H2212 MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3VRmlKSzVyPUG3JI5O M3;HfFI{ODF{MkS4
SK-LU-1 NHrwb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOyTWM2OD1zODDuUS=> M{[2WFI{ODF{MkS4
H2009 M2HzOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF7IH7N M3nCZ|I{ODF{MkS4
H1792 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX3Vo1KSzVyPUKwJI5O NHLPelczOzBzMkK0PC=>
COR-L23 M4\XT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHtd|k5UUN3ME2yNkBvVQ>? NVPvc4x7OjNyMUKyOFg>
H727 MorFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\sTWM2OD1{ODDuUS=> M17SdVI{ODF{MkS4
H1734 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ6IH7N M{HkWVI{ODF{MkS4
H358 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne3TWM2OD1{OTDuUS=> NGHrfpMzOzBzMkK0PC=>
A549 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S4NGlEPTB;NEOgcm0> M33wXVI{ODF{MkS4
H2122 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\4TWM2OD13MzDuUS=> M4LDT|I{ODF{MkS4
Calu-1 NV32OVBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrxT5pTUUN3ME21PEBvVQ>? M2fLbFI{ODF{MkS4
Calu-6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTZ2IH7N NYf4WW1POjNyMUKyOFg>
NCI-H1975 NIew[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTGfGM1QCCq MUHJR|UxRTF4IH7N NUjmToxVOjJzNES2OlU>
NCI-H1975 M3H1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moi3O|IhcA>? MXnJR|UxRThibl2= MkHTNlIyPDR4NkW=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK; 

PubMed: 23418523     


Downregulation of multiple signaling pathways by ganetespib in melanoma cells.A. Cells were treated with indicated amounts of ganetespib for 24 h. B-RAF and N-RAS mutational status of each cell line is indicated.

p27(Kip1) / p21 (Cip1) / Cyclin D1 / Cyclin E / Cyclin B1 / CDK1 / CDK2 / CDK4; 

PubMed: 23418523     


Alterations in expression of multiple cell cycle regulating proteins induced by ganetespib. Cells were treated with indicated amounts of ganetespib for 48 h and analyzed by Western blot analysis. Relative expression levels of proteins (treated vs. control䲧疝Ỵ疞㧀疜膉痘 

Survivin / Bcl-2 / Bcl-xl / Mcl-1; 

PubMed: 23418523     


Effect of ganetespib on the expression of antiapoptotic proteins. Cells were treated with ganetespib for 48 h and analyzed using Western blot analysis. Relative expression levels of proteins are indicated.

B-RAF / C-RAF / N-RAS ; 

PubMed: 23418523     


Effect of ganetespib on B-RAF, C-RAF and N-RAS expression in melanoma cells.Cells were treated with indicated amounts of ganetespib for 48 h and subjected to Western blot analysis.

HER2 / p-STAT3 / BIM ; 

PubMed: 25077897     


NCI-H1975 cells were incubated with the indicated concentrations of ganetespib for 24 h. Cell lysates were analyzed by Western blotting.

CDK1 / Cyclin D1 / Cyclin B1 / p27; 

PubMed: 29717218     


Cropped Western blot images of the indicated cell cycle regulators are shown in ganetespib-treated (0–300 nM for 16 hours) BT474 and SKBR3 cells. 

c-PARP / c-caspase 3 / caspase 8 / c-caspase 8 / caspase 9 / c-caspase 9; 

PubMed: 29717218     


Cropped images of Western blots at the target molecular weights for the indicated apoptotic markers are shown in ganetespib-treated (0, 10, 30, 100, 300 nM for 16 hours) BT474 and SKBR3 cells. 

ErbB2 / pErbB2 / Src / pSrc / mTOR / pmTOR / Bad / pBad / GSK3 / pGSK3; 

PubMed: 29717218     


Ganetespib inhibits RTK signaling in ErbB2+ breast cancer cells. BT474 and SKBR3 cells were treated with ganetespib (0, 10, 30, 100, or 300 nM) for 16 hours, followed by Western blot analysis (cropped images) of the expression and activation/phosphorylati䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖

Wee1 / p-Wee1 / Chk1 / p-Chk1; 

PubMed: 27834954     


Hsp90 inhibition degrades the G2/M checkpoint kinases Wee1 and Chk1. The cells were treated with 200 nM ganetespib and 75 μM carboplatin for 24 h followed by immunoblot analysis. Carboplatin treatment leads to the activation of Chk1, indicated by phospho—䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ

23418523 25077897 29717218 27834954
Growth inhibition assay
Cell viability ; 

PubMed: 23418523     


A. Ganetespib reduced viability. Cells were treated with varying amounts of ganetespib for 72 h and subjected to MTS assay. Data are expressed as mean±SD of three independent experiments. B. Mutational status and ganetespib IC50 of cell lines.

23418523
体内研究 Ganetespib给药导致几种肿瘤异种移植模型的小鼠体内肿瘤显著缩减，且似乎毒性较低。此外，与tanespimycin相比，Ganetespib具有更好的肿瘤渗透性。[2]在恶性肥大细胞和OSA异种移植模型中，Ganetespib抑制体内肿瘤生长。 Ganetespib(25 mg/kg/day，3天)重复两个周期显著抑制肿瘤生长，%T/C值为18。Ganetespib能够被很好的耐受，载体对照和Ganetespib组相对于研究开始时的平均体重改变在第17天使分别为+0.3% 和-8.1%。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：[1]
- 合并
  • Cell lines: OSA细胞
  • Concentrations: 0.001-1μM
  • Incubation Time: 5天
  • Method: 将1.5 × 103 OSA细胞接种于96孔板，在包含10%血清的完全培养基中培养过夜，以测定50%抑制浓度。板在第5天采集，随后用0.001，0.005，0.01，0.05，0.1，0.5和1 μM Ganetespib处理并分析。荧光测量使用酶标仪在485 nm激发波长和530 nm发射检测波长下进行。相对细胞数以对照孔的百分比计算：样品吸光度/DMSO处理的细胞吸光度× 100。
    (Only for Reference)
动物实验：[4]
- 合并
  • Animal Models: 雌性严重的联合免疫缺陷(SCID)小鼠
  • Dosages: 25 mg/kg/day，持续 3 天
  • Administration: 尾部静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 40 mg/mL (109.76 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
5% DMSO+45% PEG 300+ddH2O
 11mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 364.4
化学式

C20H20N4O3
CAS号 888216-25-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02192541 Terminated Drug: Ziv-Aflibercept|Drug: Ganetespib Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 2 2014 Phase 1
NCT02008877 Completed Drug: ganetespib|Drug: Sirolimus Malignant Peripheral Nerve Sheath Tumors (MPNST)|Sarcoma Sarcoma Alliance for Research through Collaboration|Synta Pharmaceuticals Corp.|United States Department of Defense December 2013 Phase 1|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    Does this inhibitor inhibit both isoforms of HSP90?

  • 回答：

    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/

Selleck产品目录册

HSP (e.g. HSP90) Signaling Pathway Map

HSP (e.g. HSP90) Inhibitors with Unique Features

  • 选择性强的HSP90抑制剂

    NVP-BEP800 : HSP90β-selective, IC50=58 nM.

  • 活性最高的HSP90抑制剂

    KW-2478 : HSP90, IC50=3.8 nM.

  • 用于临床的HSP90抑制剂

    17-AAG (Tanespimycin) : Phase III for Gastrointestinal Stromal Tumors.

  • 最新的HSP90抑制剂

    XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

相关HSP (e.g. HSP90)产品

  • PU-H71 New

    PU-H71是有效的选择性HSP90抑制剂，IC50为51 nM。

  • KNK437 New

    KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。

  • VER155008 New

    VER-155008是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。

  • Tanespimycin (17-AAG)

    Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 2。

    Features:17-AAG对正常细胞的毒性很小。

  • Luminespib (NVP-AUY922)

    Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。

  • Alvespimycin (17-DMAG) HCl

    Alvespimycin (17-DMAG) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。

    Features:17-DMAG是抗生素Geldanamycin 的合成衍生物，比现有抗生素具有较低的肝毒性，比相似衍生物17-AAG效果和有效性更强。

  • Geldanamycin

    Geldanamycin是一种天然的HSP90抑制剂，Kd为1.2 μM，特异性干扰糖皮质激素受体（GR）/HSP联合。

  • HSP990 (NVP-HSP990)

    NVP-HSP990（HSP990）是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。

  • Elesclomol (STA-4783)

    Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。

  • Onalespib (AT13387)

    Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID