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 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46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
NCI-H1975 MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;GO|IhcA>? MUTJR|UxRThibl2= NFrhNY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG0OFY3PSd-MkKxOFQ3PjV:L3G+
NCI-H1975 NEHWTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nqbVQ5KGh? MkXPTWM2OD1zNjDuUS=> NXzzVGlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOFQ3PjVpPkKyNVQ1PjZ3PD;hQi=>
Calu-6 NWHncI05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTZ2IH7N NFHWd3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
Calu-1 M4TpXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTqclBmUUN3ME21PEBvVQ>? NFvidXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
H2122 M3ftbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vLcWlEPTB;NUOgcm0> NEfhUo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
A549 M{XvO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfkWpNyUUN3ME20N{BvVQ>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
H358 NWntUWRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDQWZdKSzVyPUK5JI5O Mme1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
H1734 M{TUNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ6IH7N MmXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
H727 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXYWW1KSzVyPUK4JI5O NHLKcG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
COR-L23 MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TxZWlEPTB;MkKgcm0> NGPUb|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
H1792 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDQbHVKSzVyPUKwJI5O NUT1bmJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H2009 NXHhS5JoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjvcnFKSzVyPUG5JI5O NHz6bmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
SK-LU-1 MlHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLCTWM2OD1zODDuUS=> NX3GOpF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H2212 NUjkbI9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIqwenhKSzVyPUG3JI5O M3zoeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
H441 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\XZWlEPTB;MUSgcm0> NUPKV4sxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H2030 M3jmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTF{IH7N MmrXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
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HOP-62 NFT6TIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXUVGJQUUN3ME2xNUBvVQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
IA-LM MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfsR21KSzVyPUGwJI5O MkXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
H460 NWK2UZlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DGUmlEPTB;ODDuUS=> MnGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
H157 MoTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTuS2dKSzVyPUegcm0> Moe3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ|MEGyNlQ5RC:jPh?=
H1355 M{jJVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTVibl2= M{P2T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
VCaP M1e2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILuTmVKSzVyPUegcm0> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF3MkCwOEc,OjNzNUKwNFQ9N2F-
LNCaP MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDlTWM2OD16IH7N MmXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNUKwNFQoRjJ|MUWyNFA1RC:jPh?=
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Kasumi-1 NUPOb5pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTVwODDuUS=> Moj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEO3OFEoRjJ|M{CzO|QyRC:jPh?=
CCRF-CEM (2) MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TOfmlEPTB;Nz6yJI5O MmLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEO3OFEoRjJ|M{CzO|QyRC:jPh?=
CCRF-CEM (1) NF72VWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm1TWM2OD1zMj61JI5O MmKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEO3OFEoRjJ|M{CzO|QyRC:jPh?=
MOLT-4 M{Wwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2iwNmlEPTB;MUCuOkBvVQ>? NWf3SIlkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFM4PDFpPkKzN|A{PzRzPD;hQi=>
RS4;11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7ydYdKSzVyPUGzMlUhdk1? MmTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEO3OFEoRjJ|M{CzO|QyRC:jPh?=
COG-LL-317 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTi[WMyUUN3ME20MlQhdk1? NIrNeYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwN|c1OSd-MkOzNFM4PDF:L3G+
NALM-6 M3Wzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjYboJKSzVyPUGxMlchdk1? MlrvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MEO3OFEoRjJ|M{CzO|QyRC:jPh?=
CHLA-136 M13YPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvMXXlKSzVyPUKzMlIhdk1? NVHleFI3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFM4PDFpPkKzN|A{PzRzPD;hQi=>
CHLA-90 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XlS2lEPTB;MkKuN{BvVQ>? M3TvU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CzO|QyLz5{M{OwN|c1OTxxYU6=
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NB-1643 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\TN41KSzVyPUeuOEBvVQ>? M{fkRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{CzO|QyLz5{M{OwN|c1OTxxYU6=
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CHLA-258 NU\jPWVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL5d3pKSzVyPU[uOEBvVQ>? NUDUVJN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFM4PDFpPkKzN|A{PzRzPD;hQi=>
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SJ-GBM2 NFLpOoZyUFSVIHHzd4F6 MnzLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NWH4e25kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MULxTHRUKGG|c3H5 Ml;ldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M{XwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NYDKeVRseUiWUzDhd5NigQ>? NVK2XYc1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NWTEdWx[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 M{Hz[JFJXFNiYYPzZZk> MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MUXxTHRUKGG|c3H5 MmTMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? MnrlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... 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、SDS / 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、SDS / 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/

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