Ganetespib (STA-9090)

目录号：S1159

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

10mM (in 1mL DMSO)	RMB 2472.01	现货
5mg	RMB 2187.96	现货
10mg	RMB 3025.86	现货
大包装	有超大折扣

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全国免费电话：400-668-6834 | Email：info@selleck.cn

客户购买Selleck的此次产品后发表的文献8篇：

Nature, 2017, 10.1038/nature21064

PubMed: 28178232

Cell, 2017, 168(5):856-866

PubMed: 28215707

Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1017

PubMed: 25297628

Cell Death Dis, 2014, 6:e1595

PubMed: 25590805

Hum Mol Genet, 2015, 10.1093/hmg/ddv136

PubMed: 25877301

Mol Cancer Res, 2018, 10.1158/1541-7786

PubMed: 30002191

Cancer Chemoth Pharm, 2014, 74(5):1015-22

PubMed: 25205430

Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7

PubMed:

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]

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)

参考文献

[4] Lin TY, et al. Exp Hematol. 2008, 36(10), 1266-1277.

+ 展开

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 Download Ganetespib (STA-9090) SDF

分子量	364.4
化学式	C₂₀H₂₀N₄O₃
CAS号	888216-25-9
稳定性	3 years -20°C powder
稳定性	2 years -80°C in solvent
别名	N/A

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2018-09-11)

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。

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

选择性强的HSP90抑制剂

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
活性最高的HSP90抑制剂

KW-2478 ： HSP90, IC50=3.8 nM.
用于临床的HSP90抑制剂

17-AAG (Tanespimycin) ： Phase III for Gastrointestinal Stromal Tumors.
最新的HSP90抑制剂

XL888 ： ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

研究领域

产品类型

Ganetespib (STA-9090)

客户购买Selleck的此次产品后发表的文献8篇：

客户使用该产品的3个实验数据：

产品安全说明书

HSP (e.g. HSP90)抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Ganetespib (STA-9090) SDF

计算器

摩尔浓度计算器

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

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2018-09-11)

技术支持

常见问题及建议解决方法

HSP (e.g. HSP90) Signaling Pathway Map

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

相关HSP (e.g. HSP90)产品