Ganetespib (STA-9090)

For research use only. Not for use in humans.

目录号:S1159

Ganetespib (STA-9090) Chemical Structure

CAS No. 888216-25-9

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35篇:

产品安全说明书

HSP (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 MmLzRZBweHSxc3nzJGF{e2G7 MXmzNE85OC9zNUCvNlUxKG6P M1TENlI1NzR6L{eyJIg> M4jseYlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> NWK0O2xoOjV6OEK1OVA>
MV411 MY\BdI9xfG:|aYOgRZN{[Xl? MUizNE85OC9zNUCvNlUxKG6P NYW2SIlCOjRxNEivO|IhcA>? MWPpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= MkfSNlU5QDJ3NUC=
MGC-803 NHPkc2JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mnq0NE4yNTFyMECgcm0> M3jSdVczKGh? MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkHVNlU2QTB6MEW=
SGC-7901 Mn65R4VtdCCYaXHibYxqfHliQYPzZZk> NXfxdHFTOC5zLUGwNFAhdk1? MX[3NkBp MVXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NVHhdoxYOjV3OUC4NFU>
MKN-28 NUTUfJA6S2WubDDWbYFjcWyrdImgRZN{[Xl? M4DPfVAvOS1zMECwJI5O MmTPO|IhcA>? NHjhSYJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlrTNlU2QTB6MEW=
MGC-803 NH3PcZBHfW6ldHnvckBCe3OjeR?= MorGNE4yNTFyMECgcm0> MkXhNlQhcA>? M3q4Solv\HWlZYOgS|IwVSClZXzsMYN6[2ynIHHydoV{fA>? NYjodGlXOjV3OUC4NFU>
HCT-116 M4TqNWZ2dmO2aX;uJGF{e2G7 MX61NI5O NVXxUHVLOjRiaB?= NEfVeoNFVVOR M1LtVIlv\HWlZXSgS|AwTzFiYYLy[ZN1 NXHrO3hXOjV{MUC3PVQ>
HT-29 NEjvXYpHfW6ldHnvckBCe3OjeR?= NF;0[HQ2OG6P NF3Z[GIzPCCq MXjEUXNQ MlfzbY5lfWOnZDDHNE9IOSCjcoLld5Q> MX2yOVIyODd7NB?=
SCC25 NILrSGpEgXSxeHnjbZR6KEG|c3H5 MUexNE82OCCwTR?= NHjQSHczPCCq NVi1eGpv\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 MV2yOVIxPTR|MB?=
FUDA NELLdlhEgXSxeHnjbZR6KEG|c3H5 M3;XXlExNzVyIH7N M3L6UFI1KGh? NUDONWVt\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 M1OzU|I2OjB3NEOw
Detroit562 NFPkN4FEgXSxeHnjbZR6KEG|c3H5 NXrTRXN3OTBxNUCgcm0> M3:2OlI1KGh? NFX3TGhl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MX2yOVIxPTR|MB?=
CAL27 NEjubmNEgXSxeHnjbZR6KEG|c3H5 MmD4NVAwPTBibl2= MUiyOEBp Ml3q[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M3HnT|I2OjB3NEOw
DSH1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITifpNKSzVyPU[gcm0> MV6yOFc5PDh|OR?=
SW-1710 NXvrO2o2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH3TWM2OD14IH7N NIjUTo4zPDd6NEizPS=>
T24 M2rnNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdibl2= MXuyOFc5PDh|OR?=
RT112 NGT5fVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTlibl2= NIjNNpIzPDd6NEizPS=>
639-V M4q1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\DcZNKSzVyPUGwJI5O MXeyOFc5PDh|OR?=
SCaBER MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TpTmlEPTB;MUCgcm0> NETiR4szPDd6NEizPS=>
BFTC NGTJVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTF5IH7N NVS4Ro1XOjR5OES4N|k>
J82 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF6IH7N NVH5eJVPOjR5OES4N|k>
HT-1376 NHvuN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXflfmpUUUN3ME2yNUBvVQ>? M3nw[lI1Pzh2OEO5
647-V NVHIbHNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHiTWM2OD1{NzDuUS=> MVWyOFc5PDh|OR?=
UM-UC3 M{fhbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHLTWM2OD1|MzDuUS=> M3XYWVI1Pzh2OEO5
LB831-BLC M1zSRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHhTWM2OD1|NDDuUS=> NVTuXXd{OjR5OES4N|k>
KU-19-19 M{mzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\ZVmlEPTB;M{[gcm0> NWSySIR6OjR5OES4N|k>
35612 MlXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3CUHA6UUN3ME2zPEBvVQ>? NInw[JAzPDd6NEizPS=>
5637 Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFO1e5NKSzVyPUS0JI5O MWCyOFc5PDh|OR?=
HT-1197 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTV|IH7N M1;aVFI1Pzh2OEO5
MGH-U3 M{jKWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3wTWM2OD13MzDuUS=> MX6yOFc5PDh|OR?=
TCCSUP M2rBemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj3eJNKSzVyPUG0NkBvVQ>? MUWyOFc5PDh|OR?=
RT4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\tWpBKSzVyPUG3N|Mhdk1? NH;rbHAzPDd6NEizPS=>
SW780 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTN2NUGgcm0> NUiwWIJKOjR5OES4N|k>
RKO MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPLd3ZlUUN3ME20JI5O NX\yXXhWOjR4OEK3OFc>
LS-411 N NF3qfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7DTWM2OD13IH7N MnPTNlQ3QDJ5NEe=
SW620 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRThibl2= MVuyOFY5Ojd2Nx?=
HCT-15 NIXyfJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;qe2lEPTB;ODDuUS=> M3PHS|I1Pjh{N{S3
HuTu-80 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\EcFNuUUN3ME2xN{BvVQ>? NVXaXotIOjR4OEK3OFc>
HCT 116 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfLW5BWUUN3ME2xOEBvVQ>? MoLXNlQ3QDJ5NEe=
COLO-205 M2TzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX1TWM2OD1zNDDuUS=> Mlf1NlQ3QDJ5NEe=
NCI-H747 NIrzZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF5IH7N MlziNlQ3QDJ5NEe=
COLO-678 M4C0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn4bHhtUUN3ME2yNUBvVQ>? MmHoNlQ3QDJ5NEe=
LoVo MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK3dW5DUUN3ME2yNkBvVQ>? Mn\oNlQ3QDJ5NEe=
LS-1034 Mkn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNzIH7N NVnLT5FsOjR4OEK3OFc>
SNU-C2B M3vC[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTR3IH7N MkLQNlQ3QDJ5NEe=
LS-123 NH71fVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTd|IH7N NV;UflZ7OjR4OEK3OFc>
SK-CO-1 NXLrOnJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjsUWVSUUN3ME24NUBvVQ>? NEXydFQzPDZ6Mke0Oy=>
HCC2998 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e1TGlEPTB;MUK4JI5O MoLyNlQ3QDJ5NEe=
MDA-MB-231 NFO5W4hHfW6ldHnvckBCe3OjeR?= M1X4PVExOCCwTR?= MmrQN|AhdWmw MVnpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NYPtSVlvOjR{NEiyOlU>
MDA-MB-435 NWHkNIZbTnWwY4Tpc44hSXO|YYm= NWfiPGc3OTByIH7N MkfkN|AhdWmw NIq0ZlhqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NVewdJZGOjR{NEiyOlU>
BT-20  NGP2OYZHfW6ldHnvckBCe3OjeR?= NXHLSnRUOTByL{K1NEBvVQ>? MnzzNlQhcA>? Mne1doV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH NHuwTY0zPDF5M{W0NS=>
MDA-MB-231 NICyVIhHfW6ldHnvckBCe3OjeR?= Mo\lNVAxKG6P MXiyOEBp MWrpcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg NV;2[GZwOjRzN{O1OFE>
H82 NV[zeI1mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHjd|dtUUN3ME2zNE4zPyCwTR?= NWC1Tnh1OjRzNk[1NFU>
GLC4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LJ[WlEPTB;MkCuOFchdk1? M3PHTVI1OTZ4NUC1
H69 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD3[YxlUUN3ME24N{4{PiCwTR?= NGPBO|kzPDF4NkWwOS=>
H128 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTTfmtIUUN3ME22PU42PSCwTR?= M3\aOVI1OTZ4NUC1
H146 NEOxXGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ6LkWxJI5O NX7UdmY2OjRzNk[1NFU>
H187 NHvjR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHLfZd1UUN3ME2yOE46QSCwTR?= MnnvNlQyPjZ3MEW=
H526 NF6yPIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn3T5FKSzVyPUKxMlY1KG6P NV7hfIh3OjRzNk[1NFU>
N592 NX70WmJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS0TWM2OD1zND6xNkBvVQ>? MlfCNlQyPjZ3MEW=
H620 MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN{Lk[3JI5O NX21VYl6OjRzNk[1NFU>
H792 NIHkUVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkexTWM2OD12NT6wO{BvVQ>? MkDCNlQyPjZ3MEW=
H1173 NVP2OGlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTDO3V4UUN3ME2xNk43OiCwTR?= MkfmNlQyPjZ3MEW=
AC3 M{XS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrDNGY5UUN3ME2yOU46KG6P NVjBcINTOjRzNk[1NFU>
H82 MVPGeY5kfGmxbjDBd5NigQ>? M2S2RlMxKG6P MY[3NkBp NVHEbIVNcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NHjxTFUzPDF4NkWwOS=>
GLC4 M2fHR2Z2dmO2aX;uJGF{e2G7 M2TibVMxKG6P Mo\HO|IhcA>? NFjqclFqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MX:yOFE3PjVyNR?=
H146  NVjIeG52TnWwY4Tpc44hSXO|YYm= M1vjO|MxKG6P NX2ycIM5PzJiaB?= NEjoTZVqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NFjmSmwzPDF4NkWwOS=>
OVCAR-5 MlXjR4VtdCCYaXHibYxqfHliQYPzZZk> M13KdlAuOTByMDDuUS=> MWW3NkBp M4j4SYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWDGRo5uOjN7MECxN|Y>
OVCAR-8 NXjncWdZS2WubDDWbYFjcWyrdImgRZN{[Xl? MYKwMVExODBibl2= M1T4SVczKGh? MWPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NHTINJQzOzlyMEGzOi=>
A1847 NV;5Xmd[S2WubDDWbYFjcWyrdImgRZN{[Xl? M2PZOFAuOTByMDDuUS=> MYO3NkBp M2rnZYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MUCyN|kxODF|Nh?=
SKOV-3 M3XRSGNmdGxiVnnhZoltcXS7IFHzd4F6 M1[x[lAuOTByMDDuUS=> NETBXZA4OiCq MUTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFPxPIIzOzlyMEGzOi=>
OVCAR-5 M4TP[GFxd3C2b4Ppd{BCe3OjeR?= NEXnblQyOC1zMECgcm0> MnjPNlQwPDhxN{KgbC=> MojqbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MU[yN|kxODF|Nh?=
OVCAR-8 MljBRZBweHSxc3nzJGF{e2G7 M{\jNlExNTFyMDDuUS=> NVjSWmxYOjRxNEivO|IhcA>? NV7QVJFvcW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboTsfS=> M3H1NFI{QTByMUO2
A1847 Mkn1RZBweHSxc3nzJGF{e2G7 NUXHXFZLOTBvMUCwJI5O MnjjNlQwPDhxN{KgbC=> MnPkbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= MYmyN|kxODF|Nh?=
H2228 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXW3[FBqOC1zMECwJI5O NI\JRZc4OiCq NETuTHVKSzVyPUGzJI5O NV;6WIdEOjN3M{OyOlU>
H3122 NWSxW2tYS2WubDDWbYFjcWyrdImgRZN{[Xl? NVG3d3ZPOC1zMECwJI5O NGf2TpY4OiCq NF3BbXRKSzVyPUGwJI5O NWjWToZvOjN3M{OyOlU>
K008 MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3fUUmlEPTB;NkCgcm0> MVOyN|QyQDV{Mx?=
K028 MlrPR4VtdCCYaXHibYxqfHliQYPzZZk> NYfsTIs4UUN3ME24OEBvVQ>? MoDWNlM1OTh3MkO=
K029 Mnq2R4VtdCCYaXHibYxqfHliQYPzZZk> MXXJR|UxRTR4IH7N NGTIO2kzOzRzOEWyNy=>
M23 NHP1fnlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEPBe5lKSzVyPUO3MlUhdk1? MViyN|QyQDV{Mx?=
K033 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1TrNmlEPTB;N{WuOUBvVQ>? M4DSdFI{PDF6NUKz
K008 NVrlRmV[TnWwY4Tpc44hSXO|YYm= MVuyOVAhdk1? MWSyOEBp M4DW[olv\HWlZYOgS|Ih[XK{ZYP0 NGjBTWQzOzRzOEWyNy=>
K028 NUCwWlVqTnWwY4Tpc44hSXO|YYm= MlO5NlUxKG6P MVKyOEBp NXvUdmRzcW6mdXPld{BIOiCjcoLld5Q> MWeyN|QyQDV{Mx?=
K029 MkO4SpVv[3Srb36gRZN{[Xl? M1rUR|I2OCCwTR?= M1K4SlI1KGh? NIKw[npqdmS3Y3XzJGcyKGG{cnXzeC=> MVmyN|QyQDV{Mx?=
M23 NGS5O|BHfW6ldHnvckBCe3OjeR?= MlrkNlUxKG6P MYmyOEBp NGTNVHZqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> MWWyN|QyQDV{Mx?=
K033 MVrGeY5kfGmxbjDBd5NigQ>? NHvhXXEzPTBibl2= MVSyOEBp M4[zSYlv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= NIXqT2wzOzRzOEWyNy=>
K008 NWm0XHh4SXCxcITvd4l{KEG|c3H5 MkXENVAxKG6P M4KzOVczKGh? MkXjd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NUTafI42OjN2MUi1NlM>
K028 NUexc3lVSXCxcITvd4l{KEG|c3H5 NWDKfHR1OTByIH7N M{jQ[lczKGh? NXqxSWVSe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= Mkn6NlM1OTh3MkO=
K029 MUTBdI9xfG:|aYOgRZN{[Xl? M{L5[VExOCCwTR?= MYq3NkBp M3LZe5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? Ml64NlM1OTh3MkO=
M23 MkPsRZBweHSxc3nzJGF{e2G7 M2fqRlExOCCwTR?= NGWxVWI4OiCq MVLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MYKyN|QyQDV{Mx?=
K033 NH7uWoVCeG:ydH;zbZMhSXO|YYm= MW[xNFAhdk1? MofHO|IhcA>? M1SxcpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? Mn\mNlM1OTh3MkO=
RD MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjte4RZUUN3ME24JI5O MWWyN|MxOzd2MR?=
Rh41 NGLuSWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnL1TWM2OD1zMD60JI5O MnPWNlM{ODN5NEG=
Rh18 NF3pfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEO5Ro9KSzVyPU[uNkBvVQ>? NITVbJUzOzNyM{e0NS=>
Rh30 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTVwNjDuUS=> MlrqNlM{ODN5NEG=
BT-12 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELnUXZKSzVyPUG0MlMhdk1? MYWyN|MxOzd2MR?=
CHLA-266 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:3TWM2OD1{Nz6xJI5O MonJNlM{ODN5NEG=
TC-71 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTRwNTDuUS=> NUnrcolFOjN|MEO3OFE>
CHLA-9 M2TLS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTRwNjDuUS=> MV6yN|MxOzd2MR?=
CHLA-10 NELrbIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjMe|ZKSzVyPUWuO{BvVQ>? NYTnb5lHOjN|MEO3OFE>
CHLA-258 NHfQNVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P1RWlEPTB;Nj60JI5O MlnINlM{ODN5NEG=
SJ-GBM2 NYLuWYFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXuTWM2OD1zMj65JI5O NUPLXFFHOjN|MEO3OFE>
NB-1643 NULURop[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZOmRKSzVyPUeuOEBvVQ>? NH3pWo0zOzNyM{e0NS=>
NB-EBc1 NX\TVJVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTF4Lkigcm0> MlTPNlM{ODN5NEG=
CHLA-90 NF[wTXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\PblZKSzVyPUKyMlMhdk1? Ml;uNlM{ODN5NEG=
CHLA-136 MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT5TWM2OD1{Mz6yJI5O MlXnNlM{ODN5NEG=
NALM-6 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFzLkegcm0> M{jvZ|I{OzB|N{Sx
COG-LL-317 M3G5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mny3TWM2OD12LkSgcm0> M{PGXFI{OzB|N{Sx
RS4;11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXaTWM2OD1zMz61JI5O MYeyN|MxOzd2MR?=
MOLT-4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrCWWQyUUN3ME2xNE43KG6P NFTPV3kzOzNyM{e0NS=>
CCRF-CEM (1) NWfMd2l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF{LkWgcm0> NELCbGwzOzNyM{e0NS=>
CCRF-CEM (2) NXzZfJhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPhTWM2OD15LkKgcm0> MUWyN|MxOzd2MR?=
Kasumi-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTVwODDuUS=> Moe1NlM{ODN5NEG=
Karpas-299 NI[0XoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDqTWM2OD17Lk[gcm0> MVuyN|MxOzd2MR?=
Ramos-RA1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW1WZZKSzVyPUeuOEBvVQ>? NIq4dmUzOzNyM{e0NS=>
LNCaP NXzv[JpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTZZY9KSzVyPUigcm0> MlGzNlMyPTJyMES=
VCaP NED1XIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHiNIVKSzVyPUegcm0> NH\SVWgzOzF3MkCwOC=>
H1355 NHXTfZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTVibl2= NELOeWIzOzBzMkK0PC=>
H157 M3TKeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\VOYtwUUN3ME23JI5O MU[yN|AyOjJ2OB?=
H460 NEjkUYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRThibl2= MkXUNlMxOTJ{NEi=
IA-LM NXGx[pBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7xbYpKSzVyPUGwJI5O NEm1elEzOzBzMkK0PC=>
HOP-62 M3L5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPVUFBKSzVyPUGxJI5O NUHMXIx{OjNyMUKyOFg>
H23 MkfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLGTWM2OD1zMTDuUS=> MWCyN|AyOjJ2OB?=
H2030 NX74SYU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D1[mlEPTB;MUKgcm0> Mo\INlMxOTJ{NEi=
H441 NWfGOYJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvLbplYUUN3ME2xOEBvVQ>? MlHGNlMxOTJ{NEi=
H2212 NFy3WYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmzTWM2OD1zNzDuUS=> MUWyN|AyOjJ2OB?=
SK-LU-1 M4LYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTF6IH7N NGnXR48zOzBzMkK0PC=>
H2009 M{nGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK0TWM2OD1zOTDuUS=> MWSyN|AyOjJ2OB?=
H1792 M1\IRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTJyIH7N M3XG[VI{ODF{MkS4
COR-L23 M4[4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ{IH7N MmTYNlMxOTJ{NEi=
H727 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqyRXdKSzVyPUK4JI5O NIe2WpozOzBzMkK0PC=>
H1734 NX:3TZNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTJ6IH7N MYGyN|AyOjJ2OB?=
H358 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XPfGlEPTB;Mkmgcm0> NHvSNVAzOzBzMkK0PC=>
A549 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3GzU2lEPTB;NEOgcm0> NGi1O5UzOzBzMkK0PC=>
H2122 M3Tsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT6OGpWUUN3ME21N{BvVQ>? NUXvTlE4OjNyMUKyOFg>
Calu-1 NVTrWlk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXHOZBKSzVyPUW4JI5O M2fFWVI{ODF{MkS4
Calu-6 NUftO3l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jacmlEPTB;NkSgcm0> NVvK[VB5OjNyMUKyOFg>
NCI-H1975 MoTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXVOFghcA>? NIjwWXpKSzVyPUG2JI5O MU[yNlE1PDZ4NR?=
NCI-H1975 Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvRTYk4OiCq NGDvcIFKSzVyPUigcm0> NGCwbpEzOjF2NE[2OS=>

... 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
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

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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/

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

相关HSP (HSP90)产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID