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

大剂量询单有大折扣！

今日订购，明日送达，全国免运费！

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	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]

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 2018-11-16)

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。

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 2018-11-16)

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