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 MYTBdI9xfG:|aYOgRZN{[Xl? MXezNE85OC9zNUCvNlUxKG6P NGXmXlQzPC92OD:3NkBp M4THVIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=> MoLoNlU5QDJ3NUC=
MV411 Mn3QRZBweHSxc3nzJGF{e2G7 NWHXd2h2OzBxOECvNVUxNzJ3MDDuUS=> NGnkTHEzPC92OD:3NkBp NX3JSJhQcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{ M4frfFI2QDh{NUWw
MGC-803 M4\rS2NmdGxiVnnhZoltcXS7IFHzd4F6 NVz4eZhkOC5zLUGwNFAhdk1? NVzTTFl1PzJiaB?= Mn3TbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVjZSIgyOjV3OUC4NFU>
SGC-7901 M{SzRWNmdGxiVnnhZoltcXS7IFHzd4F6 MkfXNE4yNTFyMECgcm0> MVi3NkBp MULpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NV\JWlc{OjV3OUC4NFU>
MKN-28 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkLVNE4yNTFyMECgcm0> NUPFSG5lPzJiaB?= M{HGeolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmHTNlU2QTB6MEW=
MGC-803 MoDVSpVv[3Srb36gRZN{[Xl? M3j6TVAvOS1zMECwJI5O NGDoNYczPCCq MWrpcoR2[2W|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q> MYqyOVU6ODhyNR?=
HCT-116 MYLGeY5kfGmxbjDBd5NigQ>? MmPEOVBvVQ>? NYrUVYd2OjRiaB?= MVfEUXNQ M1O1fYlv\HWlZXSgS|AwTzFiYYLy[ZN1 MnPxNlUzOTB5OUS=
HT-29 M3;GNGZ2dmO2aX;uJGF{e2G7 MVG1NI5O Mm\RNlQhcA>? NGXoenZFVVOR MYLpcoR2[2WmIFewM2cyKGG{cnXzeC=> M{TFeFI2OjFyN{m0
SCC25 MUjDfZRwgGmlaYT5JGF{e2G7 MmrtNVAwPTBibl2= MW[yOEBp MWDk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MWCyOVIxPTR|MB?=
FUDA NXXxN|FCS3m2b4jpZ4l1gSCDc4PhfS=> NF\zVYMyOC93MDDuUS=> MXeyOEBp M2nuWIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MUOyOVIxPTR|MB?=
Detroit562 NFHuenhEgXSxeHnjbZR6KEG|c3H5 MUGxNE82OCCwTR?= MlPPNlQhcA>? MmXq[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NIPycFAzPTJyNUSzNC=>
CAL27 NIXBTXREgXSxeHnjbZR6KEG|c3H5 MU[xNE82OCCwTR?= Ml31NlQhcA>? NX7Bdldr\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6 NXrTd3lrOjV{MEW0N|A>
DSH1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPOO2RKSzVyPU[gcm0> MoToNlQ4QDR6M{m=
SW-1710 NUXSfWdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPVTWM2OD14IH7N MmLXNlQ4QDR6M{m=
T24 NV7oeopxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTdibl2= NV7vPGpwOjR5OES4N|k>
RT112 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfIb4NDUUN3ME25JI5O NXnmSpVNOjR5OES4N|k>
639-V Mke3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXFTWM2OD1zMDDuUS=> Mk[yNlQ4QDR6M{m=
SCaBER MmXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7iTGdJUUN3ME2xNEBvVQ>? NWPDOVJIOjR5OES4N|k>
BFTC M4LJXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjwZYF[UUN3ME2xO{BvVQ>? NYjlPI9UOjR5OES4N|k>
J82 NHrMfppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDadYlMUUN3ME2xPEBvVQ>? MnGwNlQ4QDR6M{m=
HT-1376 NYP1SHN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jWXmlEPTB;MkGgcm0> NEjvfnkzPDd6NEizPS=>
647-V M1jhZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJ5IH7N MlK5NlQ4QDR6M{m=
UM-UC3 NIjofXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\UUY5xUUN3ME2zN{BvVQ>? MnLQNlQ4QDR6M{m=
LB831-BLC Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TmPGlEPTB;M{Sgcm0> M3zSbFI1Pzh2OEO5
KU-19-19 NIHIXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvDTGVTUUN3ME2zOkBvVQ>? NXPscXdjOjR5OES4N|k>
35612 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS4bmZ{UUN3ME2zPEBvVQ>? NHSzTIQzPDd6NEizPS=>
5637 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4qxXGlEPTB;NESgcm0> MVqyOFc5PDh|OR?=
HT-1197 NHXaUIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInr[GZKSzVyPUWzJI5O MX2yOFc5PDh|OR?=
MGH-U3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjIO4xYUUN3ME21N{BvVQ>? NUnLfY46OjR5OES4N|k>
TCCSUP NYfGXpBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDYTWM2OD1zNEKgcm0> NYK1Z|BkOjR5OES4N|k>
RT4 M{HpdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\jRWlEPTB;MUezN{BvVQ>? NVXzTHRrOjR5OES4N|k>
SW780 MofKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN2NUGgcm0> Mo\qNlQ4QDR6M{m=
RKO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjUTHBKSzVyPUSgcm0> MV6yOFY5Ojd2Nx?=
LS-411 N NFzjNmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTVibl2= NX\VS|BUOjR4OEK3OFc>
SW620 M{nwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRThibl2= NF;NOW8zPDZ6Mke0Oy=>
HCT-15 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHTTWM2OD16IH7N M1SxPVI1Pjh{N{S3
HuTu-80 NVzTdoFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LtUGlEPTB;MUOgcm0> Mn[4NlQ3QDJ5NEe=
HCT 116 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfXTWM2OD1zNDDuUS=> Ml3iNlQ3QDJ5NEe=
COLO-205 Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF2IH7N NF72[VczPDZ6Mke0Oy=>
NCI-H747 M2n5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jaOGlEPTB;MUegcm0> NHnKfmEzPDZ6Mke0Oy=>
COLO-678 NID4PIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEW3V4tKSzVyPUKxJI5O MmHYNlQ3QDJ5NEe=
LoVo MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr0fnFEUUN3ME2yNkBvVQ>? M3PC[FI1Pjh{N{S3
LS-1034 NX:1ZXk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3STWM2OD1|MTDuUS=> NUi3Xmt5OjR4OEK3OFc>
SNU-C2B NU\vOINpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfUNFh3UUN3ME20OUBvVQ>? MmTCNlQ3QDJ5NEe=
LS-123 NYrXR4NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPwZWNuUUN3ME23N{BvVQ>? NUKwOpBqOjR4OEK3OFc>
SK-CO-1 NHnwPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{T6cmlEPTB;OEGgcm0> Ml7BNlQ3QDJ5NEe=
HCC2998 NYLDcFdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXpd2VKSzVyPUGyPEBvVQ>? MnTnNlQ3QDJ5NEe=
MDA-MB-231 NGrWWnlHfW6ldHnvckBCe3OjeR?= MX6xNFAhdk1? Mo[3N|AhdWmw MX;pcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>? MVKyOFI1QDJ4NR?=
MDA-MB-435 M{P1PGZ2dmO2aX;uJGF{e2G7 NUHS[HM5OTByIH7N NHHWR44{OCCvaX6= MkewbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y|rF? MojnNlQzPDh{NkW=
BT-20  NYPqS4N5TnWwY4Tpc44hSXO|YYm= Mmm1NVAxNzJ3MDDuUS=> NU[wbXFIOjRiaB?= NX;DT3l6emW|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI MkeyNlQyPzN3NEG=
MDA-MB-231 M4TrW2Z2dmO2aX;uJGF{e2G7 MUSxNFAhdk1? NGqzeY4zPCCq M2\3O4lvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG|aY\lJINieGGlaYT5xsA> NGDXRpAzPDF5M{W0NS=>
H82 NULyO|E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H1PGlEPTB;M{CuNlchdk1? M3jLNFI1OTZ4NUC1
GLC4 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fsWWlEPTB;MkCuOFchdk1? NIDRWXczPDF4NkWwOS=>
H69 Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTh|LkO2JI5O MWSyOFE3PjVyNR?=
H128 M4nNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DnUmlEPTB;NkmuOVUhdk1? Ml;sNlQyPjZ3MEW=
H146 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJ6LkWxJI5O MWSyOFE3PjVyNR?=
H187 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfve4NKSzVyPUK0Mlk6KG6P NYrLRY9COjRzNk[1NFU>
H526 Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJzLk[0JI5O NYjubpN7OjRzNk[1NFU>
N592 NWf4OZI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzNend[UUN3ME2xOE4yOiCwTR?= M2jCPVI1OTZ4NUC1
H620 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HCVWlEPTB;M{KuOlchdk1? NI\1cJEzPDF4NkWwOS=>
H792 NHi5e3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;sTWM2OD12NT6wO{BvVQ>? NXPycnBxOjRzNk[1NFU>
H1173 NFvpR3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTubJNKSzVyPUGyMlYzKG6P NWfvT4VwOjRzNk[1NFU>
AC3 M3vUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnSemNoUUN3ME2yOU46KG6P NV7qT4NuOjRzNk[1NFU>
H82 M2XoeWZ2dmO2aX;uJGF{e2G7 NH36[|A{OCCwTR?= MoLOO|IhcA>? M3jBVIlv\HWlZYOgdIVze2m|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=> MUOyOFE3PjVyNR?=
GLC4 MX3GeY5kfGmxbjDBd5NigQ>? NVrEOZRrOzBibl2= NFvoOZk4OiCq NYLNO3RRcW6mdXPld{Bx\XK|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1 NWnB[GhWOjRzNk[1NFU>
H146  NVzDZ4ZHTnWwY4Tpc44hSXO|YYm= M4\tWFMxKG6P NWrqcpRDPzJiaB?= MoWzbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0 M37uNVI1OTZ4NUC1
OVCAR-5 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV[wMVExODBibl2= MVq3NkBp MUDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWqyN|kxODF|Nh?=
OVCAR-8 NX;3ZmMyS2WubDDWbYFjcWyrdImgRZN{[Xl? M{i1c|AuOTByMDDuUS=> MkjuO|IhcA>? NInBO4xqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUHDPXhTOjN7MECxN|Y>
A1847 NFj3O4FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3\3ZVAuOTByMDDuUS=> NYDuO|ZuPzJiaB?= M4LNdYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHLKbYUzOzlyMEGzOi=>
SKOV-3 NILiUW5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHTSPWoxNTFyMECgcm0> NUflPGsyPzJiaB?= NIXjbFlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1HZUFI{QTByMUO2
OVCAR-5 MW\BdI9xfG:|aYOgRZN{[Xl? NI\x[VQyOC1zMECgcm0> M3XiOlI1NzR6L{eyJIg> NH;nVnFqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5 MXeyN|kxODF|Nh?=
OVCAR-8 M3jNSmFxd3C2b4Ppd{BCe3OjeR?= MVyxNE0yODBibl2= MXGyOE81QC95MjDo M4XLeYlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MUSyN|kxODF|Nh?=
A1847 NF\pfI5CeG:ydH;zbZMhSXO|YYm= MV2xNE0yODBibl2= M{WwdlI1NzR6L{eyJIg> M{HEXYlv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm= MYWyN|kxODF|Nh?=
H2228 M1q1bGNmdGxiVnnhZoltcXS7IFHzd4F6 M3PyTlAuOTByMDDuUS=> Mkj4O|IhcA>? MlXQTWM2OD1zMzDuUS=> M1HWVVI{PTN|Mk[1
H3122 NYfKT|RMS2WubDDWbYFjcWyrdImgRZN{[Xl? M2i1V|AuOTByMDDuUS=> MYS3NkBp M1PrfWlEPTB;MUCgcm0> Mn:1NlM2OzN{NkW=
K008 M1\wT2NmdGxiVnnhZoltcXS7IFHzd4F6 MVPJR|UxRTZyIH7N MYWyN|QyQDV{Mx?=
K028 NVXaPWN7S2WubDDWbYFjcWyrdImgRZN{[Xl? NH\hemNKSzVyPUi0JI5O M3z1b|I{PDF6NUKz
K029 NGfGPIlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVTUSIQ1UUN3ME20OkBvVQ>? MU[yN|QyQDV{Mx?=
M23 MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH3YXpFKSzVyPUO3MlUhdk1? Mm\CNlM1OTh3MkO=
K033 NF7LVotE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWDJR|UxRTd3LkWgcm0> MlnTNlM1OTh3MkO=
K008 MmLTSpVv[3Srb36gRZN{[Xl? M2rDTVI2OCCwTR?= M4G3O|I1KGh? MX3pcoR2[2W|IFeyJIFzemW|dB?= MmG0NlM1OTh3MkO=
K028 NUnlTGdZTnWwY4Tpc44hSXO|YYm= NHSxdVUzPTBibl2= NV\nb2ViOjRiaB?= NXjIT3ZDcW6mdXPld{BIOiCjcoLld5Q> NV7WcWxjOjN2MUi1NlM>
K029 NWHpbVR6TnWwY4Tpc44hSXO|YYm= M1WzW|I2OCCwTR?= NEDMUFgzPCCq MWrpcoR2[2W|IFexJIFzemW|dB?= MVuyN|QyQDV{Mx?=
M23 NXnpfmlvTnWwY4Tpc44hSXO|YYm= NFTTeYczPTBibl2= NUPGN5hTOjRiaB?= NIXvcZhqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=> MoPnNlM1OTh3MkO=
K033 MlrWSpVv[3Srb36gRZN{[Xl? NGG2fGUzPTBibl2= NX3Ub2ptOjRiaB?= MUjpcoR2[2W|IHGgcY9l\XO2IHnuZ5Jm[XOnIHnuJGcyKHCxcIXsZZRqd25? NE\qbWMzOzRzOEWyNy=>
K008 MXrBdI9xfG:|aYOgRZN{[Xl? NWjZVYY5OTByIH7N NX\aPVJ6PzJiaB?= Morzd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NV\GT45DOjN2MUi1NlM>
K028 MWrBdI9xfG:|aYOgRZN{[Xl? Mn70NVAxKG6P NXHOe3RDPzJiaB?= M2fRbpNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? MWmyN|QyQDV{Mx?=
K029 NG\adJNCeG:ydH;zbZMhSXO|YYm= NV7GVIY3OTByIH7N MUS3NkBp M1G4eZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN? NWrv[YZqOjN2MUi1NlM>
M23 MUXBdI9xfG:|aYOgRZN{[Xl? M1LTN|ExOCCwTR?= NHfESoU4OiCq MVnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{ Ml\NNlM1OTh3MkO=
K033 NYPN[GRISXCxcITvd4l{KEG|c3H5 MXGxNFAhdk1? M2jPdlczKGh? MonYd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>? NH3LSXYzOzRzOEWyNy=>
RD M{TmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRThibl2= MXqyN|MxOzd2MR?=
Rh41 NV61SmJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\vT|dHUUN3ME2xNE41KG6P NIPyblYzOzNyM{e0NS=>
Rh18 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly0TWM2OD14LkKgcm0> NVrGSJZOOjN|MEO3OFE>
Rh30 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn32TWM2OD13Lk[gcm0> MoL5NlM{ODN5NEG=
BT-12 NYX0XmRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rLdmlEPTB;MUSuN{BvVQ>? M3PoOFI{OzB|N{Sx
CHLA-266 NFrl[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ewd2lEPTB;MkeuNUBvVQ>? Moj4NlM{ODN5NEG=
TC-71 NWPFcnJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLI[YtKSzVyPUSuOUBvVQ>? Mn3lNlM{ODN5NEG=
CHLA-9 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrFTWM2OD12Lk[gcm0> MnXNNlM{ODN5NEG=
CHLA-10 NGDhXllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6xe|NoUUN3ME21Mlchdk1? NHGycXozOzNyM{e0NS=>
CHLA-258 NVXNTVFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLVSolJUUN3ME22MlQhdk1? M1ixUFI{OzB|N{Sx
SJ-GBM2 NVLwbXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF{Lkmgcm0> NYXOcpFCOjN|MEO3OFE>
NB-1643 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTdwNDDuUS=> NUXRc2tNOjN|MEO3OFE>
NB-EBc1 NXnyfXFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LWeGlEPTB;MU[uPEBvVQ>? NU[2OpdXOjN|MEO3OFE>
CHLA-90 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme1TWM2OD1{Mj6zJI5O NFPEbnczOzNyM{e0NS=>
CHLA-136 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e3cmlEPTB;MkOuNkBvVQ>? NE\NToUzOzNyM{e0NS=>
NALM-6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjrTWM2OD1zMT63JI5O Mn7NNlM{ODN5NEG=
COG-LL-317 NYDzOXFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTRwNDDuUS=> M4jVPFI{OzB|N{Sx
RS4;11 M{TqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS0NFhKSzVyPUGzMlUhdk1? NYXreXhlOjN|MEO3OFE>
MOLT-4 NX;CO5RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HLcWlEPTB;MUCuOkBvVQ>? NXPHUppCOjN|MEO3OFE>
CCRF-CEM (1) MnLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\MTWM2OD1zMj61JI5O M321NFI{OzB|N{Sx
CCRF-CEM (2) NEfpV|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LHe2lEPTB;Nz6yJI5O MUGyN|MxOzd2MR?=
Kasumi-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD3TWM2OD13Lkigcm0> NX3vTI1{OjN|MEO3OFE>
Karpas-299 NXfpVGNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTlwNjDuUS=> MWKyN|MxOzd2MR?=
Ramos-RA1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTdwNDDuUS=> NVLlWG1MOjN|MEO3OFE>
LNCaP MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRThibl2= MlvTNlMyPTJyMES=
VCaP MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;aXZZKSzVyPUegcm0> MXWyN|E2OjByNB?=
H1355 NXzSe5R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP0TWM2OD13IH7N NH61UoYzOzBzMkK0PC=>
H157 M3jKU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonETWM2OD15IH7N MkexNlMxOTJ{NEi=
H460 NY\LeodYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnaZZBSUUN3ME24JI5O NVrp[WtXOjNyMUKyOFg>
IA-LM M1z4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFyIH7N MWWyN|AyOjJ2OB?=
HOP-62 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuzTWM2OD1zMTDuUS=> M4q0T|I{ODF{MkS4
H23 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H1WWlEPTB;MUGgcm0> M{\oUVI{ODF{MkS4
H2030 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF{IH7N M3G0WlI{ODF{MkS4
H441 NYXXW4xNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvSTWM2OD1zNDDuUS=> NVP4[nJyOjNyMUKyOFg>
H2212 M3;sb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LjcWlEPTB;MUegcm0> NEDRSXEzOzBzMkK0PC=>
SK-LU-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;mPWlEPTB;MUigcm0> NUiyfWV3OjNyMUKyOFg>
H2009 M3HmXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jLN2lEPTB;MUmgcm0> M4LXUVI{ODF{MkS4
H1792 M37YWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFryU4VKSzVyPUKwJI5O M{DvSFI{ODF{MkS4
COR-L23 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rOZWlEPTB;MkKgcm0> NVfxRW0yOjNyMUKyOFg>
H727 M2T0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ6IH7N Ml\HNlMxOTJ{NEi=
H1734 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnSXJpKSzVyPUK4JI5O NYfaXFNiOjNyMUKyOFg>
H358 M3;tXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ7IH7N MUWyN|AyOjJ2OB?=
A549 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIju[|FKSzVyPUSzJI5O NG[0RYozOzBzMkK0PC=>
H2122 Mn;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzyTWM2OD13MzDuUS=> Mn\JNlMxOTJ{NEi=
Calu-1 M2[zfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDK[JdKSzVyPUW4JI5O M4rNdVI{ODF{MkS4
Calu-6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M125ZWlEPTB;NkSgcm0> NHfJZ2szOzBzMkK0PC=>
NCI-H1975 NH7GeVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX33W|lNPDhiaB?= M{[3ZWlEPTB;MU[gcm0> NV;EZnJ{OjJzNES2OlU>
NCI-H1975 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK3UHk4OiCq M3nTSmlEPTB;ODDuUS=> NIHvSXYzOjF2NE[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
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
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
NCT02192541 Terminated Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 2 2014 Phase 1
NCT02261805 Terminated Cancer|Small Cell Lung Cancer Georgetown University|Synta Pharmaceuticals Corp. October 2014 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

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