Ganetespib (STA-9090)

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  
RMB 2472.01 现货
RMB 2187.96 现货
RMB 3025.86 现货
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客户使用Selleck该产品发表文献8篇:

客户使用该产品的3个实验数据:

  • 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.

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 NIPuOVVCeG:ydH;zbZMhSXO|YYm= NXvrR2EzOzBxOECvNVUxNzJ3MDDuUS=> MkDaNlQwPDhxN{KgbC=> NYrlTmh6cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ NF;HNpczPTh6MkW1NC=>
MV411 MnK2RZBweHSxc3nzJGF{e2G7 NWjoV2dxOzBxOECvNVUxNzJ3MDDuUS=> MVWyOE81QC95MjDo NXHacFNRcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ MYKyOVg5OjV3MB?=
MGC-803 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXvBToVLOC5zLUGwNFAhdk1? MVm3NkBp Mo\WbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MnfpNlU2QTB6MEW=
SGC-7901 M2\Pb2NmdGxiVnnhZoltcXS7IFHzd4F6 Ml7VNE4yNTFyMECgcm0> MlXXO|IhcA>? NEHaXGdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MmDNNlU2QTB6MEW=
MKN-28 MkjSR4VtdCCYaXHibYxqfHliQYPzZZk> MXiwMlEuOTByMDDuUS=> Mn;MO|IhcA>? M4\lcYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NWDaZ|NROjV3OUC4NFU>
MGC-803 MWHGeY5kfGmxbjDBd5NigQ>? NXrBVXk5OC5zLUGwNFAhdk1? MUCyOEBp MWjpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> NWjTTGtwOjV3OUC4NFU>
HCT-116 M{TMVWZ2dmO2aX;uJGF{e2G7 MlHWOVBvVQ>? NWXOUmVYOjRiaB?= Mn3NSG1UVw>? NHHxU45qdmS3Y3XkJGcxN0dzIHHydoV{fA>? NXKyZpF1OjV{MUC3PVQ>
HT-29 MkLiSpVv[3Srb36gRZN{[Xl? M3rkVFUxdk1? MlvoNlQhcA>? M{G2XWROW09? NFH2fGtqdmS3Y3XkJGcxN0dzIHHydoV{fA>? NH;kR4MzPTJzMEe5OC=>
SCC25 M3eyOmN6fG:6aXPpeJkhSXO|YYm= NVvkZXBOOTBxNUCgcm0> MWOyOEBp M33oeIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NWTN[3prOjV{MEW0N|A>
FUDA NWPuT5F4S3m2b4jpZ4l1gSCDc4PhfS=> MXmxNE82OCCwTR?= M{T1dlI1KGh? M{O4NoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NYXQZlI2OjV{MEW0N|A>
Detroit562 NULQW5ZNS3m2b4jpZ4l1gSCDc4PhfS=> NV;1bVNROTBxNUCgcm0> NYe4c5dPOjRiaB?= MX7k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M4P2[lI2OjB3NEOw
CAL27 MWTDfZRwgGmlaYT5JGF{e2G7 NI\QSFMyOC93MDDuUS=> NFe3O3MzPCCq M2XzOYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NH;aeGczPTJyNUSzNC=>
DSH1 NFGxNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTZibl2= M4fv[FI1Pzh2OEO5
SW-1710 M1PnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\KTZZKSzVyPU[gcm0> MnTQNlQ4QDR6M{m=
T24 MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Kx[2lEPTB;NzDuUS=> NWKybZFEOjR5OES4N|k>
RT112 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLmOmNKSzVyPUmgcm0> MW[yOFc5PDh|OR?=
639-V NWHNU3lrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jNSWlEPTB;MUCgcm0> MYmyOFc5PDh|OR?=
SCaBER NIm3d5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nWe2lEPTB;MUCgcm0> M3fxUlI1Pzh2OEO5
BFTC M{TIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX5fYJKSzVyPUG3JI5O M3;LblI1Pzh2OEO5
J82 M2DKc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF6IH7N MnXSNlQ4QDR6M{m=
HT-1376 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K5XWlEPTB;MkGgcm0> MUeyOFc5PDh|OR?=
647-V NXfsSph2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ5IH7N NFntNVUzPDd6NEizPS=>
UM-UC3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfhTWM2OD1|MzDuUS=> NILH[VIzPDd6NEizPS=>
LB831-BLC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTN2IH7N NVnofpdCOjR5OES4N|k>
KU-19-19 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDm[nFKSzVyPUO2JI5O MXuyOFc5PDh|OR?=
35612 M2HMNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:yb2lEPTB;M{igcm0> NUjDOWtmOjR5OES4N|k>
5637 MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPkTWM2OD12NDDuUS=> M1rhNFI1Pzh2OEO5
HT-1197 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTV|IH7N M3LyV|I1Pzh2OEO5
MGH-U3 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;vcGlEPTB;NUOgcm0> NX\obnBVOjR5OES4N|k>
TCCSUP NFfCendIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\rTWM2OD1zNEKgcm0> NVn0bIFFOjR5OES4N|k>
RT4 MnG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF5M{Ogcm0> M4nke|I1Pzh2OEO5
SW780 NEnPe3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHweGRKSzVyPUO0OVEhdk1? NIP2[VAzPDd6NEizPS=>
RKO NVrqcXByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W3SWlEPTB;NDDuUS=> NE\kO2QzPDZ6Mke0Oy=>
LS-411 N NXjXe|BQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTVibl2= M2e4TlI1Pjh{N{S3
SW620 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRThibl2= MmPyNlQ3QDJ5NEe=
HCT-15 MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H4NmlEPTB;ODDuUS=> MViyOFY5Ojd2Nx?=
HuTu-80 NX3CT41MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;XOm5UUUN3ME2xN{BvVQ>? NED4NlczPDZ6Mke0Oy=>
HCT 116 NVPQVmVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\kZmlEPTB;MUSgcm0> NXOxUmN6OjR4OEK3OFc>
COLO-205 NWrYUGZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqzOmdKSzVyPUG0JI5O M{H5[FI1Pjh{N{S3
NCI-H747 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDmXW5KSzVyPUG3JI5O MXuyOFY5Ojd2Nx?=
COLO-678 MlT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjwe5Q3UUN3ME2yNUBvVQ>? MoX4NlQ3QDJ5NEe=
LoVo MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\SR2dKSzVyPUKyJI5O NGi4fJMzPDZ6Mke0Oy=>
LS-1034 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S0eGlEPTB;M{Ggcm0> MmHkNlQ3QDJ5NEe=
SNU-C2B M{DSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HDbWlEPTB;NEWgcm0> NWTnPItuOjR4OEK3OFc>
LS-123 M17GOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L1fmlEPTB;N{Ogcm0> NH7p[ZgzPDZ6Mke0Oy=>
SK-CO-1 M{e2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYG2bWNmUUN3ME24NUBvVQ>? MUGyOFY5Ojd2Nx?=
HCC2998 MorRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnKUVMyUUN3ME2xNlghdk1? M1XSeFI1Pjh{N{S3
MDA-MB-231 MVzGeY5kfGmxbjDBd5NigQ>? NGrjPZAyODBibl2= NVjrb2N2OzBibXnu NWX5OJpYcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= M1HYZVI1OjR6Mk[1
MDA-MB-435 MlvySpVv[3Srb36gRZN{[Xl? MV:xNFAhdk1? NXzxZ5JwOzBibXnu MnHDbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? NF:wUm0zPDJ2OEK2OS=>
BT-20  Mn\PSpVv[3Srb36gRZN{[Xl? M3TEfFExOC9{NUCgcm0> M{TjOFI1KGh? NYWyc2lxemW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI M3;MNVI1OTd|NUSx
MDA-MB-231 M4r4TmZ2dmO2aX;uJGF{e2G7 NX\CPVY5OTByIH7N NFLWNm8zPCCq NGXCdYZqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh NH2zTIMzPDF5M{W0NS=>
H82 NXj2OmlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDjTWM2OD1|MD6yO{BvVQ>? Mn7GNlQyPjZ3MEW=
GLC4 NEPMTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJyLkS3JI5O NWnBPYdpOjRzNk[1NFU>
H69 NGjOWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jycmlEPTB;OEOuN|Yhdk1? NHnBWFgzPDF4NkWwOS=>
H128 Ml7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7qWZlKSzVyPU[5MlU2KG6P M4DicFI1OTZ4NUC1
H146 M{TrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;oTWM2OD1{OD61NUBvVQ>? M1HkUFI1OTZ4NUC1
H187 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOxXotkUUN3ME2yOE46QSCwTR?= MVyyOFE3PjVyNR?=
H526 NVTFfYlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTXTWM2OD1{MT62OEBvVQ>? MoD6NlQyPjZ3MEW=
N592 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDPV|M1UUN3ME2xOE4yOiCwTR?= NVKxOnU2OjRzNk[1NFU>
H620 MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\rTWM2OD1|Mj62O{BvVQ>? M3\5U|I1OTZ4NUC1
H792 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7pfnNKSzVyPUS1MlA4KG6P MoXYNlQyPjZ3MEW=
H1173 MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDDVJdKSzVyPUGyMlYzKG6P M2q1WFI1OTZ4NUC1
AC3 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\VVmtKSzVyPUK1Mlkhdk1? Mk\NNlQyPjZ3MEW=
H82 NUDye2pGTnWwY4Tpc44hSXO|YYm= NYWzc5A2OzBibl2= NYOw[G0zPzJiaB?= NIDqXZFqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> NGjUUngzPDF4NkWwOS=>
GLC4 MmLOSpVv[3Srb36gRZN{[Xl? MYSzNEBvVQ>? M1LjNVczKGh? M{nUZ4lv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MX:yOFE3PjVyNR?=
H146  MXnGeY5kfGmxbjDBd5NigQ>? NVrWRWJ5OzBibl2= NGnrd4s4OiCq MoXGbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 NUTDeJp{OjRzNk[1NFU>
OVCAR-5 NFHVZoFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXPGToNMOC1zMECwJI5O MUW3NkBp MkTybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXmyN|kxODF|Nh?=
OVCAR-8 MlLzR4VtdCCYaXHibYxqfHliQYPzZZk> NXWxSopQOC1zMECwJI5O M4j0NlczKGh? NWrmd4ZbcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4HoNlI{QTByMUO2
A1847 M4rQfWNmdGxiVnnhZoltcXS7IFHzd4F6 M{X3SlAuOTByMDDuUS=> NYnDOlV7PzJiaB?= MUTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUiyN|kxODF|Nh?=
SKOV-3 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3XPZ|AuOTByMDDuUS=> MYS3NkBp NEjUcJBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1G3WlI{QTByMUO2
OVCAR-5 MmnNRZBweHSxc3nzJGF{e2G7 MVGxNE0yODBibl2= NWDOOop4OjRxNEivO|IhcA>? NHTwd2JqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NYPjOXM1OjN7MECxN|Y>
OVCAR-8 NH\CWGFCeG:ydH;zbZMhSXO|YYm= MlLENVAuOTByIH7N MmexNlQwPDhxN{KgbC=> NEHq[GZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 NVv1XXdTOjN7MECxN|Y>
A1847 MXrBdI9xfG:|aYOgRZN{[Xl? NHHKOnoyOC1zMECgcm0> M17idlI1NzR6L{eyJIg> Mn;CbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= NVXYbFJjOjN7MECxN|Y>
H2228 MkLTR4VtdCCYaXHibYxqfHliQYPzZZk> NVWzWJBxOC1zMECwJI5O NV7EXWhQPzJiaB?= NVnIVGJRUUN3ME2xN{BvVQ>? NInGS5YzOzV|M{K2OS=>
H3122 NIe0PIRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2XEWlAuOTByMDDuUS=> NVzjbZViPzJiaB?= MWrJR|UxRTFyIH7N MV:yN|U{OzJ4NR?=
K008 M4C1N2NmdGxiVnnhZoltcXS7IFHzd4F6 MVzJR|UxRTZyIH7N NFK3c2czOzRzOEWyNy=>
K028 NUjtb|hUS2WubDDWbYFjcWyrdImgRZN{[Xl? M4rIXmlEPTB;OESgcm0> MkXBNlM1OTh3MkO=
K029 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXLBdJh2UUN3ME20OkBvVQ>? NHGzN40zOzRzOEWyNy=>
M23 M{PodWNmdGxiVnnhZoltcXS7IFHzd4F6 NIHJU|VKSzVyPUO3MlUhdk1? NIW1O4UzOzRzOEWyNy=>
K033 M4Phe2NmdGxiVnnhZoltcXS7IFHzd4F6 NF7GOllKSzVyPUe1MlUhdk1? NYj1ZWF1OjN2MUi1NlM>
K008 M2G1fWZ2dmO2aX;uJGF{e2G7 MXiyOVAhdk1? NFHuPHQzPCCq MXXpcoR2[2W|IFeyJIFzemW|dB?= MUmyN|QyQDV{Mx?=
K028 M1H5cmZ2dmO2aX;uJGF{e2G7 Ml7YNlUxKG6P Mlr1NlQhcA>? Mny5bY5lfWOnczDHNkBienKnc4S= MViyN|QyQDV{Mx?=
K029 M2HjbmZ2dmO2aX;uJGF{e2G7 M3TjO|I2OCCwTR?= MUKyOEBp NFf6[JhqdmS3Y3XzJGcyKGG{cnXzeC=> MXeyN|QyQDV{Mx?=
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M23 M1fRfWFxd3C2b4Ppd{BCe3OjeR?= M1TE[VExOCCwTR?= MYq3NkBp MWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ NVX1WJVYOjN2MUi1NlM>
K033 M2PqOWFxd3C2b4Ppd{BCe3OjeR?= NYXBNlVIOTByIH7N NHjUNG04OiCq NH7tU3h{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NUXNW3U2OjN2MUi1NlM>
RD M2nxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPLcWk{UUN3ME24JI5O MkHuNlM{ODN5NEG=
Rh41 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHv5enVKSzVyPUGwMlQhdk1? MljZNlM{ODN5NEG=
Rh18 M3vrTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLVO4RyUUN3ME22MlIhdk1? M1vXN|I{OzB|N{Sx
Rh30 NV\5eIl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLVcpdKSzVyPUWuOkBvVQ>? NXLLVZRMOjN|MEO3OFE>
BT-12 M{\PT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13sXmlEPTB;MUSuN{BvVQ>? NUDSdXlOOjN|MEO3OFE>
CHLA-266 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJ5LkGgcm0> MnvqNlM{ODN5NEG=
TC-71 NF7Fb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzGRW9tUUN3ME20MlUhdk1? MlvnNlM{ODN5NEG=
CHLA-9 NITR[HlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTVNGJKSzVyPUSuOkBvVQ>? MXOyN|MxOzd2MR?=
CHLA-10 M1vwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT1TI9EUUN3ME21Mlchdk1? NYTpcHBOOjN|MEO3OFE>
CHLA-258 NH7GTW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6wXJpFUUN3ME22MlQhdk1? MlnlNlM{ODN5NEG=
SJ-GBM2 NHPwV5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTF{Lkmgcm0> M{ezZ|I{OzB|N{Sx
NB-1643 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzoWWlKSzVyPUeuOEBvVQ>? NIS3cmMzOzNyM{e0NS=>
NB-EBc1 M4XoN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF4Lkigcm0> NXH4XJhFOjN|MEO3OFE>
CHLA-90 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP1UHpLUUN3ME2yNk4{KG6P NH\vVpMzOzNyM{e0NS=>
CHLA-136 NUS5VVN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PyPGlEPTB;MkOuNkBvVQ>? M{XPOVI{OzB|N{Sx
NALM-6 NUPlbZp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fKZmlEPTB;MUGuO{BvVQ>? MnvJNlM{ODN5NEG=
COG-LL-317 NFK0[YlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkiwTWM2OD12LkSgcm0> M2HJcVI{OzB|N{Sx
RS4;11 NX\SRZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF|LkWgcm0> NUfYOYpJOjN|MEO3OFE>
MOLT-4 NXezXWl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPaTWM2OD1zMD62JI5O NX\XPGJZOjN|MEO3OFE>
CCRF-CEM (1) NHHyWllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTF{LkWgcm0> MkLoNlM{ODN5NEG=
CCRF-CEM (2) MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HVRmlEPTB;Nz6yJI5O Moe4NlM{ODN5NEG=
Kasumi-1 NU\ZSWZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e1Z2lEPTB;NT64JI5O NI\Ld|YzOzNyM{e0NS=>
Karpas-299 NFvNfHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTlwNjDuUS=> MoLBNlM{ODN5NEG=
Ramos-RA1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjSVow4UUN3ME23MlQhdk1? NXXCWFlOOjN|MEO3OFE>
LNCaP M4DQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRThibl2= MXeyN|E2OjByNB?=
VCaP NUHFe4FlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrJTWM2OD15IH7N NXn5TGNuOjNzNUKwNFQ>
H1355 NE\5Wo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrEXZNLUUN3ME21JI5O NE\jboYzOzBzMkK0PC=>
H157 M1SwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17FeWlEPTB;NzDuUS=> MnrINlMxOTJ{NEi=
H460 NHn4eGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjiVVJKSzVyPUigcm0> MXmyN|AyOjJ2OB?=
IA-LM M3LqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXYTWM2OD1zMDDuUS=> Ml7xNlMxOTJ{NEi=
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H23 MoXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\DTWM2OD1zMTDuUS=> MkixNlMxOTJ{NEi=
H2030 M{DWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK5TWM2OD1zMjDuUS=> NGL6c3EzOzBzMkK0PC=>
H441 M1XTN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPWcWhKSzVyPUG0JI5O NUTI[nNqOjNyMUKyOFg>
H2212 M3PG[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHZU3JKSzVyPUG3JI5O NEjNb2MzOzBzMkK0PC=>
SK-LU-1 NGPEdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF6IH7N NYX5WYJuOjNyMUKyOFg>
H2009 NIjhSJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF7IH7N NEPqV5QzOzBzMkK0PC=>
H1792 MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHUTWM2OD1{MDDuUS=> MX[yN|AyOjJ2OB?=
COR-L23 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7uR|NKSzVyPUKyJI5O MkizNlMxOTJ{NEi=
H727 M{nYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjUeIxKSzVyPUK4JI5O MkHONlMxOTJ{NEi=
H1734 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHiXVRKSzVyPUK4JI5O NI\yVHIzOzBzMkK0PC=>
H358 M3Lv[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;OUWlEPTB;Mkmgcm0> NXnCcGdXOjNyMUKyOFg>
A549 NIrjd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjITWM2OD12MzDuUS=> MkC1NlMxOTJ{NEi=
H2122 NYDTUIlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jkeWlEPTB;NUOgcm0> M3f0V|I{ODF{MkS4
Calu-1 M{D2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[5TWM2OD13ODDuUS=> NXLXfIxnOjNyMUKyOFg>
Calu-6 NFTLeZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nBTmlEPTB;NkSgcm0> NWG0NlBCOjNyMUKyOFg>
NCI-H1975 NEPnS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi0PEBp MmXLTWM2OD1zNjDuUS=> NWrtbm1wOjJzNES2OlU>
NCI-H1975 M3;iemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TpRVczKGh? MVzJR|UxRThibl2= NIXQZ5IzOjF2NE[2OS=>

... Click to View More Cell Line Experimental Data

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]
+ 展开
  • 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]
+ 展开
  • Animal Models: 雌性严重的联合免疫缺陷(SCID)小鼠
  • Formulation: 在DMSO中用20% Cremophor RH 40以1:10稀释
  • 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
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT03783949 Recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Universitaire Ziekenhuizen Leuven|European Commission November 30 2018 Phase 2
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1
NCT02389751 Active not recruiting Gastroesophageal Junction Adenocarcinoma|Malignant Neoplasm of the Cervical Esophagus|Malignant Neoplasm of the Thoracic Esophagus|Stage IIA Esophageal Cancer AJCC v7|Stage IIB Esophageal Cancer AJCC v7|Stage IIIA Esophageal Cancer AJCC v7|Stage IIIB Esophageal Cancer AJCC v7|Stage IIIC Esophageal Cancer AJCC v7 M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 10 2015 Phase 1

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 (e.g. HSP90) Signaling Pathway Map

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

相关HSP (e.g. HSP90)产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID