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 NYPWOlZvSXCxcITvd4l{KEG|c3H5 MXOzNE85OC9zNUCvNlUxKG6P Mn\sNlQwPDhxN{KgbC=> MWnpcoR2[2W|IHTvd4Uh\GWyZX7kZY51KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYO= NELYT3UzPTh6MkW1NC=>
MV411 NF7aRoRCeG:ydH;zbZMhSXO|YYm= MlTpN|AwQDBxMUWwM|I2OCCwTR?= M{C5W|I1NzR6L{eyJIg> M3jHNYlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> M3LSOlI2QDh{NUWw
MGC-803 NViydIV5S2WubDDWbYFjcWyrdImgRZN{[Xl? Ml;TNE4yNTFyMECgcm0> NHTFU|Q4OiCq M4rtPYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MXWyOVU6ODhyNR?=
SGC-7901 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Ml7ENE4yNTFyMECgcm0> NGPQeG04OiCq NXfSc492cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVnFdYNQOjV3OUC4NFU>
MKN-28 MkDnR4VtdCCYaXHibYxqfHliQYPzZZk> M1\CWVAvOS1zMECwJI5O NWXQeXFVPzJiaB?= NFPicpNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MWiyOVU6ODhyNR?=
MGC-803 M4XTXGZ2dmO2aX;uJGF{e2G7 MnLONE4yNTFyMECgcm0> NVrPbXZVOjRiaB?= NIDMUYJqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R? MX:yOVU6ODhyNR?=
HCT-116 Mk\QSpVv[3Srb36gRZN{[Xl? MWC1NI5O Ml\LNlQhcA>? NYHXUJFETE2VTx?= MYfpcoR2[2WmIFewM2cyKGG{cnXzeC=> NX7kNYsxOjV{MUC3PVQ>
HT-29 MoDZSpVv[3Srb36gRZN{[Xl? MkfOOVBvVQ>? MWCyOEBp M4rYdmROW09? NXexcWZYcW6mdXPl[EBIOC:JMTDhdpJme3R? MWmyOVIyODd7NB?=
SCC25 MYDDfZRwgGmlaYT5JGF{e2G7 NWHWelZkOTBxNUCgcm0> NWXLVpRCOjRiaB?= NIKwV2tl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MlWzNlUzODV2M{C=
FUDA M3KxUGN6fG:6aXPpeJkhSXO|YYm= NVuzS4FEOTBxNUCgcm0> M1i0XFI1KGh? NIOxbZVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MmnhNlUzODV2M{C=
Detroit562 MVnDfZRwgGmlaYT5JGF{e2G7 MoHkNVAwPTBibl2= M1fWOlI1KGh? NWHWeoc2\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NX6xO2xJOjV{MEW0N|A>
CAL27 M3PNVGN6fG:6aXPpeJkhSXO|YYm= MV[xNE82OCCwTR?= M4PzRlI1KGh? M3W3SYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NIHkU2EzPTJyNUSzNC=>
DSH1 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e2eGlEPTB;NjDuUS=> Mn;ZNlQ4QDR6M{m=
SW-1710 NFX4b|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnHTWM2OD14IH7N MXSyOFc5PDh|OR?=
T24 MoPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zCV2lEPTB;NzDuUS=> NH;qZ2QzPDd6NEizPS=>
RT112 NHj4VldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDvbFhrUUN3ME25JI5O MWmyOFc5PDh|OR?=
639-V NWrGWpN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DuVmlEPTB;MUCgcm0> MkG3NlQ4QDR6M{m=
SCaBER M{SxcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFyIH7N Mn3oNlQ4QDR6M{m=
BFTC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfxb5RKSzVyPUG3JI5O M4HNTFI1Pzh2OEO5
J82 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLVV2QxUUN3ME2xPEBvVQ>? MnfsNlQ4QDR6M{m=
HT-1376 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH5[HRKSzVyPUKxJI5O M{D3TlI1Pzh2OEO5
647-V M2nYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP2fnRKSzVyPUK3JI5O MY[yOFc5PDh|OR?=
UM-UC3 NGnaTmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLBTWM2OD1|MzDuUS=> NWX3bHI3OjR5OES4N|k>
LB831-BLC MnfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33IS2lEPTB;M{Sgcm0> NXX0cXlIOjR5OES4N|k>
KU-19-19 MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nSe2lEPTB;M{[gcm0> MnXQNlQ4QDR6M{m=
35612 NH\Zb3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN6IH7N NH3ac5IzPDd6NEizPS=>
5637 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml21TWM2OD12NDDuUS=> NVr5U|NtOjR5OES4N|k>
HT-1197 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HkV2lEPTB;NUOgcm0> MXmyOFc5PDh|OR?=
MGH-U3 MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTV|IH7N M1TDXVI1Pzh2OEO5
TCCSUP MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LaSGlEPTB;MUSyJI5O MoDiNlQ4QDR6M{m=
RT4 NV\y[Fh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr5cVZEUUN3ME2xO|M{KG6P NVzRVHA3OjR5OES4N|k>
SW780 NV;0O5RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TuZ2lEPTB;M{S1NUBvVQ>? MU[yOFc5PDh|OR?=
RKO MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfCTWM2OD12IH7N MYKyOFY5Ojd2Nx?=
LS-411 N NHz2bnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPjZm0yUUN3ME21JI5O NWLES2I1OjR4OEK3OFc>
SW620 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLEV|FKSzVyPUigcm0> MVeyOFY5Ojd2Nx?=
HCT-15 M{TqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRThibl2= NGrmeoszPDZ6Mke0Oy=>
HuTu-80 NF7uOoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHmdppKSzVyPUGzJI5O MmjKNlQ3QDJ5NEe=
HCT 116 NH;CbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDXOlRKSzVyPUG0JI5O MorsNlQ3QDJ5NEe=
COLO-205 Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHKTWM2OD1zNDDuUS=> NVnyUGVDOjR4OEK3OFc>
NCI-H747 NWDnSpBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXyfolKSzVyPUG3JI5O MWWyOFY5Ojd2Nx?=
COLO-678 NFLtbJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e5ZWlEPTB;MkGgcm0> MoPGNlQ3QDJ5NEe=
LoVo NULyepYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXRc45oUUN3ME2yNkBvVQ>? MWSyOFY5Ojd2Nx?=
LS-1034 MoDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID4eYlKSzVyPUOxJI5O NGLsNXEzPDZ6Mke0Oy=>
SNU-C2B M2LRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR3IH7N M13vS|I1Pjh{N{S3
LS-123 M2HHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:4W3B5UUN3ME23N{BvVQ>? NHPSbZozPDZ6Mke0Oy=>
SK-CO-1 MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRThzIH7N M3qwRVI1Pjh{N{S3
HCC2998 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jSemlEPTB;MUK4JI5O NYrSOJdjOjR4OEK3OFc>
MDA-MB-231 NIPwTIFHfW6ldHnvckBCe3OjeR?= MoLWNVAxKG6P Ml3KN|AhdWmw NILUXmtqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?= NUPoUlVZOjR{NEiyOlU>
MDA-MB-435 MkmxSpVv[3Srb36gRZN{[Xl? NXnNcWJzOTByIH7N MYqzNEBucW5? NX\0cWM3cW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NIDleJkzPDJ2OEK2OS=>
BT-20  MVfGeY5kfGmxbjDBd5NigQ>? M3fGPVExOC9{NUCgcm0> NHnvelAzPCCq NGrKfHdz\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ? M2jyU|I1OTd|NUSx
MDA-MB-231 NFyxUIFHfW6ldHnvckBCe3OjeR?= Mn\YNVAxKG6P M1S3SFI1KGh? MlPQbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=> NHXqfnUzPDF5M{W0NS=>
H82 NVHuT255T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\xSIVKUUN3ME2zNE4zPyCwTR?= M3rvPVI1OTZ4NUC1
GLC4 MnPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHm1ZmVKSzVyPUKwMlQ4KG6P NH\2NmQzPDF4NkWwOS=>
H69 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXNbW51UUN3ME24N{4{PiCwTR?= MorsNlQyPjZ3MEW=
H128 NXzofZQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vZ[GlEPTB;NkmuOVUhdk1? NX;6T414OjRzNk[1NFU>
H146 MnrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjHUJgxUUN3ME2yPE42OSCwTR?= MYiyOFE3PjVyNR?=
H187 M2fNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInoPVdKSzVyPUK0Mlk6KG6P NUDwZYlVOjRzNk[1NFU>
H526 NUm5WpNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoO3TWM2OD1{MT62OEBvVQ>? MXqyOFE3PjVyNR?=
N592 M1LKdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:2R2lEPTB;MUSuNVIhdk1? MWeyOFE3PjVyNR?=
H620 NEO1WHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLBPI1QUUN3ME2zNk43PyCwTR?= M3vqfFI1OTZ4NUC1
H792 M1rzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{KxeGlEPTB;NEWuNFchdk1? NF\zOFYzPDF4NkWwOS=>
H1173 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnkbZRKSzVyPUGyMlYzKG6P Mlu0NlQyPjZ3MEW=
AC3 M1GxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ3Lkmgcm0> NGXoW3MzPDF4NkWwOS=>
H82 NIL6b5RHfW6ldHnvckBCe3OjeR?= MkC4N|Ahdk1? NGXhUVA4OiCq NHHoNZNqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> M{f0cFI1OTZ4NUC1
GLC4 M1G1VGZ2dmO2aX;uJGF{e2G7 MlXYN|Ahdk1? NVjLO4R{PzJiaB?= NIfibXRqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q> MlrXNlQyPjZ3MEW=
H146  MYDGeY5kfGmxbjDBd5NigQ>? MkfHN|Ahdk1? NIXkTWk4OiCq NXvBS3FvcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 M12xeVI1OTZ4NUC1
OVCAR-5 NGLESo1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEfHfIIxNTFyMECgcm0> MoXHO|IhcA>? MWXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmTENlM6ODBzM{[=
OVCAR-8 NE\BUlBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXiwMVExODBibl2= Mke1O|IhcA>? MmH6bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVLiRlFxOjN7MECxN|Y>
A1847 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUWwMVExODBibl2= NWLOcXFHPzJiaB?= NF3F[WJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NI\NTWMzOzlyMEGzOi=>
SKOV-3 NXmzeGJDS2WubDDWbYFjcWyrdImgRZN{[Xl? MWWwMVExODBibl2= M{P5OVczKGh? MWPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4\ZXFI{QTByMUO2
OVCAR-5 M{H4SGFxd3C2b4Ppd{BCe3OjeR?= NYfjeI5nOTBvMUCwJI5O NF;YNm8zPC92OD:3NkBp MkLFbY5lfWOnczDhdI9xfG:|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?= Mn76NlM6ODBzM{[=
OVCAR-8 NYfm[pk5SXCxcITvd4l{KEG|c3H5 NVnVO2djOTBvMUCwJI5O NH;HZ5AzPC92OD:3NkBp MWrpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 MWCyN|kxODF|Nh?=
A1847 M2m1d2Fxd3C2b4Ppd{BCe3OjeR?= NHfmb2IyOC1zMECgcm0> MY[yOE81QC95MjDo MXzpcoR2[2W|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7 M3vibFI{QTByMUO2
H2228 M3XvTWNmdGxiVnnhZoltcXS7IFHzd4F6 MoLxNE0yODByIH7N MV63NkBp MoDoTWM2OD1zMzDuUS=> NHTjZ4QzOzV|M{K2OS=>
H3122 MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn\FNE0yODByIH7N NVTrcpN3PzJiaB?= NF3Qfo9KSzVyPUGwJI5O MXiyN|U{OzJ4NR?=
K008 NXT3NYJVS2WubDDWbYFjcWyrdImgRZN{[Xl? MUnJR|UxRTZyIH7N NGPiXHIzOzRzOEWyNy=>
K028 MoTwR4VtdCCYaXHibYxqfHliQYPzZZk> NGnyfpNKSzVyPUi0JI5O MmnDNlM1OTh3MkO=
K029 NVe5[HdHS2WubDDWbYFjcWyrdImgRZN{[Xl? NWmx[Y82UUN3ME20OkBvVQ>? M2nJT|I{PDF6NUKz
M23 NIrpRphE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3jp[WlEPTB;M{euOUBvVQ>? M1jqNFI{PDF6NUKz
K033 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVHIZWFzUUN3ME23OU42KG6P NUjN[nRKOjN2MUi1NlM>
K008 MkHsSpVv[3Srb36gRZN{[Xl? NVHjSphvOjVyIH7N Mlq4NlQhcA>? NIrxNpdqdmS3Y3XzJGczKGG{cnXzeC=> MWSyN|QyQDV{Mx?=
K028 MXnGeY5kfGmxbjDBd5NigQ>? MYSyOVAhdk1? NUjCNFNxOjRiaB?= MkL1bY5lfWOnczDHNkBienKnc4S= MWKyN|QyQDV{Mx?=
K029 NXXyOZhlTnWwY4Tpc44hSXO|YYm= MnPRNlUxKG6P MnnmNlQhcA>? NEL2fYJqdmS3Y3XzJGcyKGG{cnXzeC=> MljhNlM1OTh3MkO=
M23 M1fDT2Z2dmO2aX;uJGF{e2G7 MoHsNlUxKG6P MkLVNlQhcA>? MXnpcoR2[2W|IFexJIFv\CCJMj;NJIFzemW|dB?= M{[0SFI{PDF6NUKz
K033 M1;sWGZ2dmO2aX;uJGF{e2G7 MWGyOVAhdk1? NIDwbogzPCCq M1jqfYlv\HWlZYOgZUBud2Snc4SgbY5kemWjc3WgbY4hTzFicH;weYxifGmxbh?= MWiyN|QyQDV{Mx?=
K008 NFnZNG1CeG:ydH;zbZMhSXO|YYm= MWWxNFAhdk1? NFvCVY84OiCq MV\zbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ MWGyN|QyQDV{Mx?=
K028 MmPoRZBweHSxc3nzJGF{e2G7 MVSxNFAhdk1? MYC3NkBp M1jEOJNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NWrkemRbOjN2MUi1NlM>
K029 MlnsRZBweHSxc3nzJGF{e2G7 M4HNUVExOCCwTR?= MYm3NkBp NIj1UFl{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m| MlLnNlM1OTh3MkO=
M23 MmjPRZBweHSxc3nzJGF{e2G7 MkHTNVAxKG6P MmDUO|IhcA>? M2DMRpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? M1vyO|I{PDF6NUKz
K033 NUf5[GdoSXCxcITvd4l{KEG|c3H5 NVjPXItKOTByIH7N M1PLeFczKGh? NWXBN5pve2mpbnnmbYNidnSueTDpcoR2[2W|IHHwc5B1d3Orcx?= NXXoXVdyOjN2MUi1NlM>
RD MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH21N|hKSzVyPUigcm0> M4nkRVI{OzB|N{Sx
Rh41 NITLXmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFyLkSgcm0> NXrqeoJzOjN|MEO3OFE>
Rh18 MlfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;PcHJlUUN3ME22MlIhdk1? MV2yN|MxOzd2MR?=
Rh30 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Pld2lEPTB;NT62JI5O NEKx[pQzOzNyM{e0NS=>
BT-12 NF3MZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXPfItGUUN3ME2xOE4{KG6P M3rtOlI{OzB|N{Sx
CHLA-266 M136c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ5LkGgcm0> MVyyN|MxOzd2MR?=
TC-71 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTuTWM2OD12LkWgcm0> MYOyN|MxOzd2MR?=
CHLA-9 NYHnT|l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzVO4l7UUN3ME20MlYhdk1? NVi3clE6OjN|MEO3OFE>
CHLA-10 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXvcVdFUUN3ME21Mlchdk1? NUnBUoVPOjN|MEO3OFE>
CHLA-258 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLlUWdKSzVyPU[uOEBvVQ>? NIW5O3AzOzNyM{e0NS=>
SJ-GBM2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF{Lkmgcm0> NIjWcWozOzNyM{e0NS=>
NB-1643 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXXPFhIUUN3ME23MlQhdk1? M4nGe|I{OzB|N{Sx
NB-EBc1 NIO0cnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjoU2FKSzVyPUG2Mlghdk1? NW[xbnF[OjN|MEO3OFE>
CHLA-90 NVLCdlFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ{LkOgcm0> MXeyN|MxOzd2MR?=
CHLA-136 NGWyNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoT0TWM2OD1{Mz6yJI5O M4Xib|I{OzB|N{Sx
NALM-6 M2myTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7pTXl3UUN3ME2xNU44KG6P MYmyN|MxOzd2MR?=
COG-LL-317 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\zTZVKSzVyPUSuOEBvVQ>? NF7vTHgzOzNyM{e0NS=>
RS4;11 M2fuO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnOTWM2OD1zMz61JI5O NVTPSpJVOjN|MEO3OFE>
MOLT-4 MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTqbmRKSzVyPUGwMlYhdk1? MWeyN|MxOzd2MR?=
CCRF-CEM (1) MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfjTWM2OD1zMj61JI5O NIHOSZMzOzNyM{e0NS=>
CCRF-CEM (2) MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3T[mtZUUN3ME23MlIhdk1? Mmr0NlM{ODN5NEG=
Kasumi-1 NYfjdlhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYniWnIzUUN3ME21Mlghdk1? M3X3S|I{OzB|N{Sx
Karpas-299 MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\6W2lEPTB;OT62JI5O NU\LcYZrOjN|MEO3OFE>
Ramos-RA1 MlnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXYUZRKSzVyPUeuOEBvVQ>? NXOyPYEzOjN|MEO3OFE>
LNCaP M3;TTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHhRoVKSzVyPUigcm0> NFjEO|EzOzF3MkCwOC=>
VCaP MlvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTdibl2= NGHTb44zOzF3MkCwOC=>
H1355 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rlRmlEPTB;NTDuUS=> NELRWW4zOzBzMkK0PC=>
H157 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHW1dZRKSzVyPUegcm0> NFzNdWIzOzBzMkK0PC=>
H460 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRThibl2= NXXER4p3OjNyMUKyOFg>
IA-LM M1\zU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP3TWM2OD1zMDDuUS=> MYOyN|AyOjJ2OB?=
HOP-62 M3TzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzQemd6UUN3ME2xNUBvVQ>? NUXVVG5TOjNyMUKyOFg>
H23 M3S5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fsbWlEPTB;MUGgcm0> M2rvdFI{ODF{MkS4
H2030 MkXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PiSWlEPTB;MUKgcm0> NXK1T2M{OjNyMUKyOFg>
H441 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF2IH7N M3;0dVI{ODF{MkS4
H2212 M2S5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XQPWlEPTB;MUegcm0> NV;F[VFtOjNyMUKyOFg>
SK-LU-1 NI\hd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHKSWxKSzVyPUG4JI5O MYmyN|AyOjJ2OB?=
H2009 NGPYbm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF7IH7N M3LoV|I{ODF{MkS4
H1792 NGLRb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu0fHdxUUN3ME2yNEBvVQ>? MXyyN|AyOjJ2OB?=
COR-L23 M3\PWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ{IH7N MXGyN|AyOjJ2OB?=
H727 M1nCUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ6IH7N NHHme20zOzBzMkK0PC=>
H1734 NVfofIJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ6IH7N M4rQWVI{ODF{MkS4
H358 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TEOGlEPTB;Mkmgcm0> M2fqV|I{ODF{MkS4
A549 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjqcmhLUUN3ME20N{BvVQ>? MWCyN|AyOjJ2OB?=
H2122 M4rKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TqWWlEPTB;NUOgcm0> NGL2NZgzOzBzMkK0PC=>
Calu-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnyOGJyUUN3ME21PEBvVQ>? MW[yN|AyOjJ2OB?=
Calu-6 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInJbldKSzVyPU[0JI5O NH3l[|MzOzBzMkK0PC=>
NCI-H1975 M3zGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWna[4FqPDhiaB?= NWLPTHNVUUN3ME2xOkBvVQ>? MljCNlIyPDR4NkW=
NCI-H1975 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\3b4dkPzJiaB?= NXHJWGc4UUN3ME24JI5O M{exT|IzOTR2Nk[1

... 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
NCT01962948 Active not recruiting Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer Fox Chase Cancer Center|National Cancer Institute (NCI) October 9 2013 Phase 1|Phase 2
NCT02012192 Terminated Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Medical University Innsbruck|European Commission July 4 2014 Phase 1|Phase 2
NCT01173523 Completed Small Cell Lung Cancer David M. Jackman MD|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp.|Dana-Farber Cancer Institute July 28 2010 Phase 2
NCT02637375 Withdrawn Breast Cancer University of Chicago May 2016 Not Applicable
NCT02389751 Active not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. April 2015 Phase 1
NCT02334319 Terminated Stage I Hypopharyngeal Squamous Cell Carcinoma|Stage I Laryngeal Squamous Cell Carcinoma|Stage I Oral Cavity Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma|Stage II Hypopharyngeal Squamous Cell Carcinoma|Stage II Laryngeal Squamous Cell Carcinoma|Stage II Oral Cavity Squamous Cell Carcinoma|Stage II Oropharyngeal Squamous Cell Carcinoma|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma Emory University|Synta Pharmaceuticals Corp. December 2014 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