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  
In DMSO 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23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 MUHBdI9xfG:|aYOgRZN{[Xl? MXyzNE85OC9zNUCvNlUxKG6P NIPQ[28zPC92OD:3NkBp MoPVbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz NWSwN4xJOjV6OEK1OVA>
MV411 MVvBdI9xfG:|aYOgRZN{[Xl? NXey[3BkOzBxOECvNVUxNzJ3MDDuUS=> NWG1OZdVOjRxNEivO|IhcA>? NEfVfWdqdmS3Y3XzJIRwe2ViZHXw[Y5l[W62IHnu[JVkfGmxbjDv[kBieG:ydH;zbZM> MkO5NlU5QDJ3NUC=
MGC-803 MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWqwMlEuOTByMDDuUS=> M2n0elczKGh? NGrkUWRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MWKyOVU6ODhyNR?=
SGC-7901 NF;K[lBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWqwMlEuOTByMDDuUS=> M2izTVczKGh? MnvtbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUKw[ItrOjV3OUC4NFU>
MKN-28 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXewMlEuOTByMDDuUS=> NGrpcFY4OiCq NHu3dGFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVS4XIJ4OjV3OUC4NFU>
MGC-803 NGOyS|RHfW6ldHnvckBCe3OjeR?= MojiNE4yNTFyMECgcm0> NXrobnBDOjRiaB?= NWDn[2Y{cW6mdXPld{BIOi:PIHPlcIwu[3mlbHWgZZJz\XO2 MX2yOVU6ODhyNR?=
HCT-116 NYfDNYY1TnWwY4Tpc44hSXO|YYm= Ml;VOVBvVQ>? NGXk[o0zPCCq M3ex[mROW09? M4LqZYlv\HWlZXSgS|AwTzFiYYLy[ZN1 MlfyNlUzOTB5OUS=
HT-29 NH32XIFHfW6ldHnvckBCe3OjeR?= NIXUdms2OG6P MmnxNlQhcA>? Mn\OSG1UVw>? MmjrbY5lfWOnZDDHNE9IOSCjcoLld5Q> NGfHcZozPTJzMEe5OC=>
SCC25 NIraUXREgXSxeHnjbZR6KEG|c3H5 M1ju[VExNzVyIH7N MnfONlQhcA>? MWTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MonjNlUzODV2M{C=
FUDA MULDfZRwgGmlaYT5JGF{e2G7 MVixNE82OCCwTR?= M1\KfFI1KGh? Ml3U[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NIDud20zPTJyNUSzNC=>
Detroit562 MYnDfZRwgGmlaYT5JGF{e2G7 M3zVOVExNzVyIH7N MVqyOEBp NFLib|Zl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MVmyOVIxPTR|MB?=
CAL27 MnP5R5l1d3irY3n0fUBCe3OjeR?= MV:xNE82OCCwTR?= NGL4VHczPCCq MXPk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MVSyOVIxPTR|MB?=
DSH1 M3;PPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV60TIdWUUN3ME22JI5O M17UUFI1Pzh2OEO5
SW-1710 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHuNItGUUN3ME22JI5O MofBNlQ4QDR6M{m=
T24 NEfUN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fMSGlEPTB;NzDuUS=> MVOyOFc5PDh|OR?=
RT112 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rVbWlEPTB;OTDuUS=> NUjUOVVJOjR5OES4N|k>
639-V Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFyIH7N MYOyOFc5PDh|OR?=
SCaBER NIXmeIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHqcGRKSzVyPUGwJI5O NFTUdYEzPDd6NEizPS=>
BFTC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLvcnhKSzVyPUG3JI5O NXXodXRYOjR5OES4N|k>
J82 NE\3VopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF6IH7N MWmyOFc5PDh|OR?=
HT-1376 M2LZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHFTWM2OD1{MTDuUS=> Ml;qNlQ4QDR6M{m=
647-V NXq0[Ix2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXBPHJKSzVyPUK3JI5O NXPZeXVvOjR5OES4N|k>
UM-UC3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnZUmtsUUN3ME2zN{BvVQ>? MVeyOFc5PDh|OR?=
LB831-BLC M2OySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTN2IH7N Mlr1NlQ4QDR6M{m=
KU-19-19 NHzl[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zTTGlEPTB;M{[gcm0> NYjpOGxCOjR5OES4N|k>
35612 NXntSXN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTN6IH7N MUmyOFc5PDh|OR?=
5637 NHzmUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ZTWM2OD12NDDuUS=> M3fKZlI1Pzh2OEO5
HT-1197 M17VUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWxS5ViUUN3ME21N{BvVQ>? NH;Qc20zPDd6NEizPS=>
MGH-U3 MmrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnVTWM2OD13MzDuUS=> Mm\ENlQ4QDR6M{m=
TCCSUP MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW5XJBKSzVyPUG0NkBvVQ>? NXHMXFJTOjR5OES4N|k>
RT4 M2TGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHxTWM2OD1zN{OzJI5O MmSzNlQ4QDR6M{m=
SW780 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPJfIRKSzVyPUO0OVEhdk1? NVTFS4pXOjR5OES4N|k>
RKO NHLF[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\JfmlEPTB;NDDuUS=> NXX2ZphqOjR4OEK3OFc>
LS-411 N MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDqTWM2OD13IH7N M1\zTlI1Pjh{N{S3
SW620 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknETWM2OD16IH7N MXqyOFY5Ojd2Nx?=
HCT-15 NHT3SWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfzTWM2OD16IH7N NWXWV25sOjR4OEK3OFc>
HuTu-80 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6zVoRKSzVyPUGzJI5O NHz3VFczPDZ6Mke0Oy=>
HCT 116 NWrqfmFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF2IH7N M4TCNVI1Pjh{N{S3
COLO-205 NGG1dVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS3TWM2OD1zNDDuUS=> NYXXXItGOjR4OEK3OFc>
NCI-H747 NEXUOmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDhW3JKSzVyPUG3JI5O M3nmdlI1Pjh{N{S3
COLO-678 M{LOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJzIH7N NXHuTVk6OjR4OEK3OFc>
LoVo MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHHW4RDUUN3ME2yNkBvVQ>? NYG2OJlQOjR4OEK3OFc>
LS-1034 NVXWOJBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHqzeZpKSzVyPUOxJI5O NGHyUlczPDZ6Mke0Oy=>
SNU-C2B Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HQe2lEPTB;NEWgcm0> MXqyOFY5Ojd2Nx?=
LS-123 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zLeGlEPTB;N{Ogcm0> MoLiNlQ3QDJ5NEe=
SK-CO-1 NFfnPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\QTmlEPTB;OEGgcm0> NXWwbWw{OjR4OEK3OFc>
HCC2998 MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF{ODDuUS=> M1rDXlI1Pjh{N{S3
MDA-MB-231 MX7GeY5kfGmxbjDBd5NigQ>? MYGxNFAhdk1? M4rWW|MxKG2rbh?= MUHpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? NUe5Omk6OjR{NEiyOlU>
MDA-MB-435 MY\GeY5kfGmxbjDBd5NigQ>? MljrNVAxKG6P M4XZOlMxKG2rbh?= Mk[wbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MXKyOFI1QDJ4NR?=
BT-20  NFvWcI9HfW6ldHnvckBCe3OjeR?= MXyxNFAwOjVyIH7N NVLzcHdpOjRiaB?= M17PVJJme3WudHXkJIlvKGFiZH;z[U1l\XCnbnTlcpQh\GW|dHHibYxqgmG2aX;uJI9nKEWJRmKsJGlITi2LUjygUWVVNCCjbnSgR3JCTg>? NFjpcXQzPDF5M{W0NS=>
MDA-MB-231 MoWzSpVv[3Srb36gRZN{[Xl? MYCxNFAhdk1? NUfkTGJlOjRiaB?= MUnpcohq[mm2czD0bIUhdWmpcnH0c5J6KGGwZDDpcpZie2m4ZTDjZZBi[2m2edMg NYDmTXRUOjRzN{O1OFE>
H82 M2fxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTQTWM2OD1|MD6yO{BvVQ>? M2PRcVI1OTZ4NUC1
GLC4 NFz2Zo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK1eodKSzVyPUKwMlQ4KG6P MnT4NlQyPjZ3MEW=
H69 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnvZZpKSzVyPUizMlM3KG6P M{fKRlI1OTZ4NUC1
H128 NWDjXHRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPiTWM2OD14OT61OUBvVQ>? MWWyOFE3PjVyNR?=
H146 M2C1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ6LkWxJI5O M2TyTVI1OTZ4NUC1
H187 NGC0cFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTJ2Lkm5JI5O M3v2XVI1OTZ4NUC1
H526 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjxfHFKSzVyPUKxMlY1KG6P MXuyOFE3PjVyNR?=
N592 NHTUUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2OzfGlEPTB;MUSuNVIhdk1? M3u4SVI1OTZ4NUC1
H620 M1vZNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzwOWNKSzVyPUOyMlY4KG6P NYqyTZhROjRzNk[1NFU>
H792 NH7mfmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW4[mxKSzVyPUS1MlA4KG6P M2\BUVI1OTZ4NUC1
H1173 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\nTWM2OD1zMj62NkBvVQ>? MmPhNlQyPjZ3MEW=
AC3 NEjCU5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLzXXdKSzVyPUK1Mlkhdk1? NGT4ZYEzPDF4NkWwOS=>
H82 NWrPdoRtTnWwY4Tpc44hSXO|YYm= M1zlXlMxKG6P MlPCO|IhcA>? NIC0fHhqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M1TXXFI1OTZ4NUC1
GLC4 NHjkd45HfW6ldHnvckBCe3OjeR?= MVKzNEBvVQ>? M{fXOFczKGh? MXrpcoR2[2W|IIDldpNqe3SnboSgS|IwVSCyaHHz[UBienKnc4S= NET3bmEzPDF4NkWwOS=>
H146  M4jM[2Z2dmO2aX;uJGF{e2G7 MXmzNEBvVQ>? NWPWepd4PzJiaB?= M1u0eYlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> M133XFI1OTZ4NUC1
OVCAR-5 NXO1c2NiS2WubDDWbYFjcWyrdImgRZN{[Xl? MUiwMVExODBibl2= M1\GVFczKGh? NUfEUm9ncW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MkXoNlM6ODBzM{[=
OVCAR-8 NVfydXh5S2WubDDWbYFjcWyrdImgRZN{[Xl? MnvTNE0yODByIH7N MlT1O|IhcA>? M3HGPYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MWWyN|kxODF|Nh?=
A1847 Mn7rR4VtdCCYaXHibYxqfHliQYPzZZk> NU\OU3FLOC1zMECwJI5O NInVN284OiCq M3PuVolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NFvGTXczOzlyMEGzOi=>
SKOV-3 MmjxR4VtdCCYaXHibYxqfHliQYPzZZk> Mkj1NE0yODByIH7N NX6xcWtSPzJiaB?= M1G1NIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHLVeWEzOzlyMEGzOi=>
OVCAR-5 NHTrTJFCeG:ydH;zbZMhSXO|YYm= NI\BcVgyOC1zMECgcm0> M4jUUFI1NzR6L{eyJIg> NI\6emhqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MVeyN|kxODF|Nh?=
OVCAR-8 NGXVflRCeG:ydH;zbZMhSXO|YYm= NFXUS|AyOC1zMECgcm0> NXSyN414OjRxNEivO|IhcA>? MYLpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MlzmNlM6ODBzM{[=
A1847 NHTJT|dCeG:ydH;zbZMhSXO|YYm= MVKxNE0yODBibl2= NXi0R|hqOjRxNEivO|IhcA>? MXzpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MkLiNlM6ODBzM{[=
H2228 M1PX[2NmdGxiVnnhZoltcXS7IFHzd4F6 NEP5NlMxNTFyMECgcm0> MlTBO|IhcA>? MXXJR|UxRTF|IH7N M4jKNVI{PTN|Mk[1
H3122 M2DmTmNmdGxiVnnhZoltcXS7IFHzd4F6 MWSwMVExODBibl2= MYi3NkBp MkD1TWM2OD1zMDDuUS=> Mkn1NlM2OzN{NkW=
K008 NHG0[4VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYPJR|UxRTZyIH7N Mn;HNlM1OTh3MkO=
K028 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1rvWmlEPTB;OESgcm0> MV6yN|QyQDV{Mx?=
K029 MlfmR4VtdCCYaXHibYxqfHliQYPzZZk> MYTJR|UxRTR4IH7N NXeySJJROjN2MUi1NlM>
M23 NX[zeHRsS2WubDDWbYFjcWyrdImgRZN{[Xl? NILrVJlKSzVyPUO3MlUhdk1? NWqxNYZzOjN2MUi1NlM>
K033 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXix[HNQUUN3ME23OU42KG6P M2\qUFI{PDF6NUKz
K008 M{niS2Z2dmO2aX;uJGF{e2G7 MWKyOVAhdk1? NHjxTIMzPCCq MWnpcoR2[2W|IFeyJIFzemW|dB?= NIPQUHYzOzRzOEWyNy=>
K028 M{KwT2Z2dmO2aX;uJGF{e2G7 MYWyOVAhdk1? M3LLRlI1KGh? NYKzfnRScW6mdXPld{BIOiCjcoLld5Q> NVjuPIZnOjN2MUi1NlM>
K029 NEH3N3hHfW6ldHnvckBCe3OjeR?= M2PTW|I2OCCwTR?= NGDwTnkzPCCq MknYbY5lfWOnczDHNUBienKnc4S= MVmyN|QyQDV{Mx?=
M23 MmWwSpVv[3Srb36gRZN{[Xl? NXLQbYZqOjVyIH7N M3\OXVI1KGh? NEH1VmlqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> MkC0NlM1OTh3MkO=
K033 M1G1N2Z2dmO2aX;uJGF{e2G7 NHe0eWQzPTBibl2= M1jOclI1KGh? MX7pcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? NX\aXIl2OjN2MUi1NlM>
K008 MX;BdI9xfG:|aYOgRZN{[Xl? MYixNFAhdk1? MX23NkBp Momyd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? M{i3VVI{PDF6NUKz
K028 MXPBdI9xfG:|aYOgRZN{[Xl? NFzoXoQyODBibl2= MWW3NkBp NFfLTo9{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| NIPlco4zOzRzOEWyNy=>
K029 NUjQeYx{SXCxcITvd4l{KEG|c3H5 M1rhblExOCCwTR?= NUjDUGtmPzJiaB?= NUHIUodIe2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= M1S3WFI{PDF6NUKz
M23 NH\U[YNCeG:ydH;zbZMhSXO|YYm= MYmxNFAhdk1? NI\HWoU4OiCq M1\wR5Nq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MYiyN|QyQDV{Mx?=
K033 MWXBdI9xfG:|aYOgRZN{[Xl? M4nYZlExOCCwTR?= M3frd|czKGh? NGXiVpB{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MVOyN|QyQDV{Mx?=
RD MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvvTWM2OD16IH7N MoWxNlM{ODN5NEG=
Rh41 NWfwfmtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX5TWM2OD1zMD60JI5O NUfUNXVSOjN|MEO3OFE>
Rh18 NVXPeHZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTZwMjDuUS=> MYiyN|MxOzd2MR?=
Rh30 M3X0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HJ[mlEPTB;NT62JI5O M2e2XVI{OzB|N{Sx
BT-12 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[5TWM2OD1zND6zJI5O MUSyN|MxOzd2MR?=
CHLA-266 Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\tWIVKSzVyPUK3MlEhdk1? NGHieoUzOzNyM{e0NS=>
TC-71 M3j2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljOTWM2OD12LkWgcm0> NIPsXoUzOzNyM{e0NS=>
CHLA-9 MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTRwNjDuUS=> NXTKNlJSOjN|MEO3OFE>
CHLA-10 MlvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HwNWlEPTB;NT63JI5O M3XSNlI{OzB|N{Sx
CHLA-258 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTZwNDDuUS=> MWeyN|MxOzd2MR?=
SJ-GBM2 NF2xdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2GyfWlEPTB;MUKuPUBvVQ>? M4jVWlI{OzB|N{Sx
NB-1643 NFPZSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnsU3FKSzVyPUeuOEBvVQ>? NFnQUmszOzNyM{e0NS=>
NB-EBc1 M{nRWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\TTWM2OD1zNj64JI5O MVuyN|MxOzd2MR?=
CHLA-90 NEmwV5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqwWJBKSzVyPUKyMlMhdk1? M3X0[lI{OzB|N{Sx
CHLA-136 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTJ|LkKgcm0> NXj0TJZYOjN|MEO3OFE>
NALM-6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfPRWNKSzVyPUGxMlchdk1? MlfvNlM{ODN5NEG=
COG-LL-317 MkLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fsbGlEPTB;ND60JI5O MlrvNlM{ODN5NEG=
RS4;11 NV34U2hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHkTWM2OD1zMz61JI5O NV\C[HJwOjN|MEO3OFE>
MOLT-4 NIW2bo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3j0XGlEPTB;MUCuOkBvVQ>? NUDnd457OjN|MEO3OFE>
CCRF-CEM (1) M{SzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPZdHlpUUN3ME2xNk42KG6P M3Xj[VI{OzB|N{Sx
CCRF-CEM (2) NFX4VI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[0TWM2OD15LkKgcm0> M13RU|I{OzB|N{Sx
Kasumi-1 M1vHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTXW|dKSzVyPUWuPEBvVQ>? NVSxOVNmOjN|MEO3OFE>
Karpas-299 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rJdmlEPTB;OT62JI5O M3KyVFI{OzB|N{Sx
Ramos-RA1 M4TiWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17ieWlEPTB;Nz60JI5O NIrBSnQzOzNyM{e0NS=>
LNCaP NU\LNnZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XkeGlEPTB;ODDuUS=> MV:yN|E2OjByNB?=
VCaP M1L2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTdibl2= M{DxOFI{OTV{MEC0
H1355 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PPcWlEPTB;NTDuUS=> M3n0flI{ODF{MkS4
H157 NVvwcZdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KyPGlEPTB;NzDuUS=> M4fNdlI{ODF{MkS4
H460 M1XHNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj0WnpKSzVyPUigcm0> M1\lR|I{ODF{MkS4
IA-LM M3nuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;0UJB2UUN3ME2xNEBvVQ>? NGXPemkzOzBzMkK0PC=>
HOP-62 NF;FepRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HVW2lEPTB;MUGgcm0> M2SydFI{ODF{MkS4
H23 NUjsb|gzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7SSYNtUUN3ME2xNUBvVQ>? M4\TXVI{ODF{MkS4
H2030 M3LO[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnicmREUUN3ME2xNkBvVQ>? NVrCTo5NOjNyMUKyOFg>
H441 NWXhPGV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M373WWlEPTB;MUSgcm0> M2nMRlI{ODF{MkS4
H2212 NILPR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnzTWM2OD1zNzDuUS=> NWG1XZJ7OjNyMUKyOFg>
SK-LU-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHGTWM2OD1zODDuUS=> MnvsNlMxOTJ{NEi=
H2009 NXW4UJY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorjTWM2OD1zOTDuUS=> M4DJcVI{ODF{MkS4
H1792 NFv6TZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LrdGlEPTB;MkCgcm0> NXzScG1yOjNyMUKyOFg>
COR-L23 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iyTGlEPTB;MkKgcm0> Mmq3NlMxOTJ{NEi=
H727 NULoXnp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ6IH7N MUOyN|AyOjJ2OB?=
H1734 M2jVbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrXbllKSzVyPUK4JI5O MWiyN|AyOjJ2OB?=
H358 M1HnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ7IH7N M1z1dFI{ODF{MkS4
A549 M3zacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL2TWM2OD12MzDuUS=> MmT3NlMxOTJ{NEi=
H2122 NFjFeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlv5TWM2OD13MzDuUS=> NY\rWpI5OjNyMUKyOFg>
Calu-1 MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HFSmlEPTB;NUigcm0> NIe2c44zOzBzMkK0PC=>
Calu-6 M1LI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTZ2IH7N MmXrNlMxOTJ{NEi=
NCI-H1975 NV3RcopbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TTU|Q5KGh? M1XsTWlEPTB;MU[gcm0> NILxOGozOjF2NE[2OS=>
NCI-H1975 NFfZeHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTSO|IhcA>? MXTJR|UxRThibl2= MXqyNlE1PDZ4NR?=

... 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
  • 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
储存条件 粉状
溶于溶剂
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 (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 (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