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
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客户使用Selleck该产品发表文献8篇：

Nature, 2017, 10.1038/nature21064

PubMed: 28178232 ( click the link to review the publication )

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

PubMed: 28215707 ( click the link to review the publication )

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

PubMed: 25297628 ( click the link to review the publication )

Cell Death Dis, 2014, 6:e1595

PubMed: 25590805 ( click the link to review the publication )

Hum Mol Genet, 2015, 10.1093/hmg/ddv136

PubMed: 25877301 ( click the link to review the publication )

Mol Cancer Res, 2018, 10.1158/1541-7786

PubMed: 30002191 ( click the link to review the publication )

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

PubMed: 25205430 ( click the link to review the publication )

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

PubMed: ( click the link to review the publication )

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	NIPuOVVCeG:ydH;zbZMhSXO\|YYm=	NXvrR2EzOzBxOECvNVUxNzJ3MDDuUS=>	MkDaNlQwPDhxN{KgbC=>		NYrlTmh6cW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{	NF;HNpczPTh6MkW1NC=>
MV411	MnK2RZBweHSxc3nzJGF{e2G7	NWjoV2dxOzBxOECvNVUxNzJ3MDDuUS=>	MVWyOE81QC95MjDo		NXHacFNRcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{	MYKyOVg5OjV3MB?=
MGC-803	MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NXvBToVLOC5zLUGwNFAhdk1?	MVm3NkBp		Mo\WbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	MnfpNlU2QTB6MEW=
SGC-7901	M2\Pb2NmdGxiVnnhZoltcXS7IFHzd4F6	Ml7VNE4yNTFyMECgcm0>	MlXXO\|IhcA>?		NEHaXGdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	MmDNNlU2QTB6MEW=
MKN-28	MkjSR4VtdCCYaXHibYxqfHliQYPzZZk>	MXiwMlEuOTByMDDuUS=>	Mn;MO\|IhcA>?		M4\lcYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	NWDaZ\|NROjV3OUC4NFU>
MGC-803	MWHGeY5kfGmxbjDBd5NigQ>?	NXrBVXk5OC5zLUGwNFAhdk1?	MUCyOEBp		MWjpcoR2[2W\|IFeyM20h[2WubD3jfYNt\SCjcoLld5Q>	NWjTTGtwOjV3OUC4NFU>
HCT-116	M{TMVWZ2dmO2aX;uJGF{e2G7	MlHWOVBvVQ>?	NWXOUmVYOjRiaB?=	Mn3NSG1UVw>?	NHHxU45qdmS3Y3XkJGcxN0dzIHHydoV{fA>?	NXKyZpF1OjV{MUC3PVQ>
HT-29	MkLiSpVv[3Srb36gRZN{[Xl?	M3rkVFUxdk1?	MlvoNlQhcA>?	M{G2XWROW09?	NFH2fGtqdmS3Y3XkJGcxN0dzIHHydoV{fA>?	NH;kR4MzPTJzMEe5OC=>
SCC25	M3eyOmN6fG:6aXPpeJkhSXO\|YYm=	NVvkZXBOOTBxNUCgcm0>	MWOyOEBp		M33oeIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:\|ZTDk[ZBmdmSnboTsfS=>	NWTN[3prOjV{MEW0N\|A>
FUDA	NWPuT5F4S3m2b4jpZ4l1gSCDc4PhfS=>	MXmxNE82OCCwTR?=	M{T1dlI1KGh?		M{O4NoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:\|ZTDk[ZBmdmSnboTsfS=>	NYXQZlI2OjV{MEW0N\|A>
Detroit562	NULQW5ZNS3m2b4jpZ4l1gSCDc4PhfS=>	NV;1bVNROTBxNUCgcm0>	NYe4c5dPOjRiaB?=		MX7k[YNz\WG\|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=	M4P2[lI2OjB3NEOw
CAL27	MWTDfZRwgGmlaYT5JGF{e2G7	NI\QSFMyOC93MDDuUS=>	NFe3O3MzPCCq		M2XzOYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:\|ZTDk[ZBmdmSnboTsfS=>	NH;aeGczPTJyNUSzNC=>
DSH1	NFGxNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MV7JR\|UxRTZibl2=	M4fv[FI1Pzh2OEO5
SW-1710	M1PnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NH\KTZZKSzVyPU[gcm0>	MnTQNlQ4QDR6M{m=
T24	MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4Kx[2lEPTB;NzDuUS=>	NWKybZFEOjR5OES4N\|k>
RT112	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NFLmOmNKSzVyPUmgcm0>	MW[yOFc5PDh\|OR?=
639-V	NWHNU3lrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M1jNSWlEPTB;MUCgcm0>	MYmyOFc5PDh\|OR?=
SCaBER	NIm3d5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3nWe2lEPTB;MUCgcm0>	M3fxUlI1Pzh2OEO5
BFTC	M{TIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NEX5fYJKSzVyPUG3JI5O	M3;LblI1Pzh2OEO5
J82	M2DKc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MWDJR\|UxRTF6IH7N	MnXSNlQ4QDR6M{m=
HT-1376	MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M3K5XWlEPTB;MkGgcm0>	MUeyOFc5PDh\|OR?=
647-V	NXfsSph2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MW\JR\|UxRTJ5IH7N	NFntNVUzPDd6NEizPS=>
UM-UC3	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MlfhTWM2OD1\|MzDuUS=>	NILH[VIzPDd6NEizPS=>
LB831-BLC	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUXJR\|UxRTN2IH7N	NVnofpdCOjR5OES4N\|k>
KU-19-19	MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NIDm[nFKSzVyPUO2JI5O	MXuyOFc5PDh\|OR?=
35612	M2HMNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M3:yb2lEPTB;M{igcm0>	NUjDOWtmOjR5OES4N\|k>
5637	MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnPkTWM2OD12NDDuUS=>	M1rhNFI1Pzh2OEO5
HT-1197	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUHJR\|UxRTV\|IH7N	M3LyV\|I1Pzh2OEO5
MGH-U3	Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M3;vcGlEPTB;NUOgcm0>	NX\obnBVOjR5OES4N\|k>
TCCSUP	NFfCendIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				Mk\rTWM2OD1zNEKgcm0>	NVn0bIFFOjR5OES4N\|k>
RT4	MnG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWDJR\|UxRTF5M{Ogcm0>	M4nke\|I1Pzh2OEO5
SW780	NEnPe3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NIHweGRKSzVyPUO0OVEhdk1?	NIP2[VAzPDd6NEizPS=>
RKO	NVrqcXByT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3W3SWlEPTB;NDDuUS=>	NE\kO2QzPDZ6Mke0Oy=>
LS-411 N	NXjXe\|BQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MWnJR\|UxRTVibl2=	M2e4TlI1Pjh{N{S3
SW620	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUHJR\|UxRThibl2=	MmPyNlQ3QDJ5NEe=
HCT-15	MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4H4NmlEPTB;ODDuUS=>	MViyOFY5Ojd2Nx?=
HuTu-80	NX3CT41MT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NX;XOm5UUUN3ME2xN{BvVQ>?	NED4NlczPDZ6Mke0Oy=>
HCT 116	NVPQVmVkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M2\kZmlEPTB;MUSgcm0>	NXOxUmN6OjR4OEK3OFc>
COLO-205	NWrYUGZNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NHqzOmdKSzVyPUG0JI5O	M{H5[FI1Pjh{N{S3
NCI-H747	MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NGDmXW5KSzVyPUG3JI5O	MXuyOFY5Ojd2Nx?=
COLO-678	MlT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYjwe5Q3UUN3ME2yNUBvVQ>?	MoX4NlQ3QDJ5NEe=
LoVo	MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NF\SR2dKSzVyPUKyJI5O	NGi4fJMzPDZ6Mke0Oy=>
LS-1034	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4S0eGlEPTB;M{Ggcm0>	MmHkNlQ3QDJ5NEe=
SNU-C2B	M{DSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{HDbWlEPTB;NEWgcm0>	NWTnPItuOjR4OEK3OFc>
LS-123	M17GOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{L1fmlEPTB;N{Ogcm0>	NH7p[ZgzPDZ6Mke0Oy=>
SK-CO-1	M{e2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NYG2bWNmUUN3ME24NUBvVQ>?	MUGyOFY5Ojd2Nx?=
HCC2998	MorRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NUnKUVMyUUN3ME2xNlghdk1?	M1XSeFI1Pjh{N{S3
MDA-MB-231	MVzGeY5kfGmxbjDBd5NigQ>?	NGrjPZAyODBibl2=	NVjrb2N2OzBibXnu		NWX5OJpYcW6qaXLpeJMh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG=	M1HYZVI1OjR6Mk[1
MDA-MB-435	MlvySpVv[3Srb36gRZN{[Xl?	MV:xNFAhdk1?	NXzxZ5JwOzBibXnu		MnHDbY5pcWKrdIOgZYNkfW23bHH0bY9vKG:oIFjJSk0y\|rF?	NF:wUm0zPDJ2OEK2OS=>
BT-20	Mn\PSpVv[3Srb36gRZN{[Xl?	M3TEfFExOC9{NUCgcm0>	M{TjOFI1KGh?		NYWyc2lxemW\|dXz0[YQhcW5iYTDkc5NmNWSncHXu[IVvfCCmZYP0ZYJqdGm8YYTpc44hd2ZiRVfGVkwhUUeILVnSMEBOTVRuIHHu[EBEWkGI	M3;MNVI1OTd\|NUSx
MDA-MB-231	M4r4TmZ2dmO2aX;uJGF{e2G7	NX\CPVY5OTByIH7N	NFLWNm8zPCCq		NGXCdYZqdmirYnn0d{B1cGVibXnndoF1d3K7IHHu[EBqdn[jc3n2[UBk[XCjY3n0feKh	NH2zTIMzPDF5M{W0NS=>
H82	NXj2OmlHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MkDjTWM2OD1\|MD6yO{BvVQ>?	Mn7GNlQyPjZ3MEW=
GLC4	NEPMTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYHJR\|UxRTJyLkS3JI5O	NWnBPYdpOjRzNk[1NFU>
H69	NGjOWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3jycmlEPTB;OEOuN\|Yhdk1?	NHnBWFgzPDF4NkWwOS=>
H128	Ml7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NH7qWZlKSzVyPU[5MlU2KG6P	M4DicFI1OTZ4NUC1
H146	M{TrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Ml;oTWM2OD1{OD61NUBvVQ>?	M1HkUFI1OTZ4NUC1
H187	MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NUOxXotkUUN3ME2yOE46QSCwTR?=	MVyyOFE3PjVyNR?=
H526	NVTFfYlrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmTXTWM2OD1{MT62OEBvVQ>?	MoD6NlQyPjZ3MEW=
N592	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NYDPV\|M1UUN3ME2xOE4yOiCwTR?=	NVKxOnU2OjRzNk[1NFU>
H620	MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mm\rTWM2OD1\|Mj62O{BvVQ>?	M3\5U\|I1OTZ4NUC1
H792	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NF7pfnNKSzVyPUS1MlA4KG6P	MoXYNlQyPjZ3MEW=
H1173	MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NEDDVJdKSzVyPUGyMlYzKG6P	M2q1WFI1OTZ4NUC1
AC3	Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NF\VVmtKSzVyPUK1Mlkhdk1?	Mk\NNlQyPjZ3MEW=
H82	NUDye2pGTnWwY4Tpc44hSXO\|YYm=	NYWzc5A2OzBibl2=	NYOw[G0zPzJiaB?=		NIDqXZFqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q>	NGjUUngzPDF4NkWwOS=>
GLC4	MmLOSpVv[3Srb36gRZN{[Xl?	MYSzNEBvVQ>?	M1LjNVczKGh?		M{nUZ4lv\HWlZYOgdIVze2m\|dHXueEBIOi:PIIDoZZNmKGG{cnXzeC=>	MX:yOFE3PjVyNR?=
H146	MXnGeY5kfGmxbjDBd5NigQ>?	NVrWRWJ5OzBibl2=	NGnrd4s4OiCq		MoXGbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0	NUTDeJp{OjRzNk[1NFU>
OVCAR-5	NFHVZoFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NXPGToNMOC1zMECwJI5O	MUW3NkBp		MkTybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	MXmyN\|kxODF\|Nh?=
OVCAR-8	MlLzR4VtdCCYaXHibYxqfHliQYPzZZk>	NXWxSopQOC1zMECwJI5O	M4j0NlczKGh?		NWrmd4ZbcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	M4HoNlI{QTByMUO2
A1847	M4rQfWNmdGxiVnnhZoltcXS7IFHzd4F6	M{X3SlAuOTByMDDuUS=>	NYnDOlV7PzJiaB?=		MUTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	MUiyN\|kxODF\|Nh?=
SKOV-3	MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	M3XPZ\|AuOTByMDDuUS=>	MYS3NkBp		NEjUcJBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	M1G3WlI{QTByMUO2
OVCAR-5	MmnNRZBweHSxc3nzJGF{e2G7	MVGxNE0yODBibl2=	NWDOOop4OjRxNEivO\|IhcA>?		NHTwd2JqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5	NYPjOXM1OjN7MECxN\|Y>
OVCAR-8	NH\CWGFCeG:ydH;zbZMhSXO\|YYm=	MlLENVAuOTByIH7N	MmexNlQwPDhxN{KgbC=>		NEHq[GZqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5	NVv1XXdTOjN7MECxN\|Y>
A1847	MXrBdI9xfG:\|aYOgRZN{[Xl?	NHHKOnoyOC1zMECgcm0>	M17idlI1NzR6L{eyJIg>		Mn;CbY5lfWOnczDhdI9xfG:\|aYOgeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnSueR?=	NVXYbFJjOjN7MECxN\|Y>
H2228	MkLTR4VtdCCYaXHibYxqfHliQYPzZZk>	NVWzWJBxOC1zMECwJI5O	NV7EXWhQPzJiaB?=		NVnIVGJRUUN3ME2xN{BvVQ>?	NInGS5YzOzV\|M{K2OS=>
H3122	NIe0PIRE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	M2XEWlAuOTByMDDuUS=>	NVzjbZViPzJiaB?=		MWrJR\|UxRTFyIH7N	MV:yN\|U{OzJ4NR?=
K008	M4C1N2NmdGxiVnnhZoltcXS7IFHzd4F6				MVzJR\|UxRTZyIH7N	NFK3c2czOzRzOEWyNy=>
K028	NUjtb\|hUS2WubDDWbYFjcWyrdImgRZN{[Xl?				M4rIXmlEPTB;OESgcm0>	MkXBNlM1OTh3MkO=
K029	MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>				NXLBdJh2UUN3ME20OkBvVQ>?	NHGzN40zOzRzOEWyNy=>
M23	M{PodWNmdGxiVnnhZoltcXS7IFHzd4F6				NIHJU\|VKSzVyPUO3MlUhdk1?	NIW1O4UzOzRzOEWyNy=>
K033	M4Phe2NmdGxiVnnhZoltcXS7IFHzd4F6				NF7GOllKSzVyPUe1MlUhdk1?	NYj1ZWF1OjN2MUi1NlM>
K008	M2G1fWZ2dmO2aX;uJGF{e2G7	MXiyOVAhdk1?	NFHuPHQzPCCq		MXXpcoR2[2W\|IFeyJIFzemW\|dB?=	MUmyN\|QyQDV{Mx?=
K028	M1H5cmZ2dmO2aX;uJGF{e2G7	Ml7YNlUxKG6P	Mlr1NlQhcA>?		Mny5bY5lfWOnczDHNkBienKnc4S=	MViyN\|QyQDV{Mx?=
K029	M2HjbmZ2dmO2aX;uJGF{e2G7	M3TjO\|I2OCCwTR?=	MUKyOEBp		NFf6[JhqdmS3Y3XzJGcyKGG{cnXzeC=>	MXeyN\|QyQDV{Mx?=
M23	MX;GeY5kfGmxbjDBd5NigQ>?	NV61VYhoOjVyIH7N	MXSyOEBp		NHjCemZqdmS3Y3XzJGcyKGGwZDDHNk9OKGG{cnXzeC=>	NV7EXmF3OjN2MUi1NlM>
K033	NGjiOpdHfW6ldHnvckBCe3OjeR?=	MX2yOVAhdk1?	MWGyOEBp		NYjPTYVScW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u	NFfmXGYzOzRzOEWyNy=>
K008	MVPBdI9xfG:\|aYOgRZN{[Xl?	NFvFPW0yODBibl2=	M1\rd\|czKGh?		MVjzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{	MnHNNlM1OTh3MkO=
K028	NULydGtjSXCxcITvd4l{KEG\|c3H5	NHH4[lcyODBibl2=	Mor3O\|IhcA>?		NITsUJB{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m\|	M1n0elI{PDF6NUKz
K029	Mn\ZRZBweHSxc3nzJGF{e2G7	NWnEeJRxOTByIH7N	MnzFO\|IhcA>?		Ml;nd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>?	NIr3W4YzOzRzOEWyNy=>
M23	M1fRfWFxd3C2b4Ppd{BCe3OjeR?=	M1TE[VExOCCwTR?=	MYq3NkBp		MWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{	NVX1WJVYOjN2MUi1NlM>
K033	M2PqOWFxd3C2b4Ppd{BCe3OjeR?=	NYXBNlVIOTByIH7N	NHjUNG04OiCq		NH7tU3h{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m\|	NUXNW3U2OjN2MUi1NlM>
RD	M2nxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NWPLcWk{UUN3ME24JI5O	MkHuNlM{ODN5NEG=
Rh41	MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NHv5enVKSzVyPUGwMlQhdk1?	MljZNlM{ODN5NEG=
Rh18	M3vrTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NWLVO4RyUUN3ME22MlIhdk1?	M1vXN\|I{OzB\|N{Sx
Rh30	NV\5eIl6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NFLVcpdKSzVyPUWuOkBvVQ>?	NXLLVZRMOjN\|MEO3OFE>
BT-12	M{\PT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M13sXmlEPTB;MUSuN{BvVQ>?	NUDSdXlOOjN\|MEO3OFE>
CHLA-266	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVrJR\|UxRTJ5LkGgcm0>	MnvqNlM{ODN5NEG=
TC-71	NF7Fb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXzGRW9tUUN3ME20MlUhdk1?	MlvnNlM{ODN5NEG=
CHLA-9	NITR[HlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NHTVNGJKSzVyPUSuOkBvVQ>?	MXOyN\|MxOzd2MR?=
CHLA-10	M1vwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NYT1TI9EUUN3ME21Mlchdk1?	NYTpcHBOOjN\|MEO3OFE>
CHLA-258	NH7GTW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NX6wXJpFUUN3ME22MlQhdk1?	MlnlNlM{ODN5NEG=
SJ-GBM2	NHPwV5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MVLJR\|UxRTF{Lkmgcm0>	M{ezZ\|I{OzB\|N{Sx
NB-1643	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHzoWWlKSzVyPUeuOEBvVQ>?	NIS3cmMzOzNyM{e0NS=>
NB-EBc1	M4XoN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MX3JR\|UxRTF4Lkigcm0>	NXH4XJhFOjN\|MEO3OFE>
CHLA-90	Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYP1UHpLUUN3ME2yNk4{KG6P	NH\vVpMzOzNyM{e0NS=>
CHLA-136	NUS5VVN7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M{PyPGlEPTB;MkOuNkBvVQ>?	M{XPOVI{OzB\|N{Sx
NALM-6	NUPlbZp{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M4fKZmlEPTB;MUGuO{BvVQ>?	MnvJNlM{ODN5NEG=
COG-LL-317	NFK0[YlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MkiwTWM2OD12LkSgcm0>	M2HJcVI{OzB\|N{Sx
RS4;11	NX\SRZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVfJR\|UxRTF\|LkWgcm0>	NUfYOYpJOjN\|MEO3OFE>
MOLT-4	NXezXWl7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmPaTWM2OD1zMD62JI5O	NX\XPGJZOjN\|MEO3OFE>
CCRF-CEM (1)	NHHyWllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MWrJR\|UxRTF{LkWgcm0>	MkLoNlM{ODN5NEG=
CCRF-CEM (2)	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M2HVRmlEPTB;Nz6yJI5O	Moe4NlM{ODN5NEG=
Kasumi-1	NU\ZSWZXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M4e1Z2lEPTB;NT64JI5O	NI\Ld\|YzOzNyM{e0NS=>
Karpas-299	NFvNfHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MV3JR\|UxRTlwNjDuUS=>	MoLBNlM{ODN5NEG=
Ramos-RA1	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NVjSVow4UUN3ME23MlQhdk1?	NXXCWFlOOjN\|MEO3OFE>
LNCaP	M4DQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXnJR\|UxRThibl2=	MXeyN\|E2OjByNB?=
VCaP	NUHFe4FlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmrJTWM2OD15IH7N	NXn5TGNuOjNzNUKwNFQ>
H1355	NE\5Wo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NWrEXZNLUUN3ME21JI5O	NE\jboYzOzBzMkK0PC=>
H157	M1SwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M17FeWlEPTB;NzDuUS=>	MnrINlMxOTJ{NEi=
H460	NHn4eGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NGjiVVJKSzVyPUigcm0>	MXmyN\|AyOjJ2OB?=
IA-LM	M3LqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MkXYTWM2OD1zMDDuUS=>	Ml7xNlMxOTJ{NEi=
HOP-62	NXnscJB2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NWXrUYNkUUN3ME2xNUBvVQ>?	M1;kcFI{ODF{MkS4
H23	MoXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Ml\DTWM2OD1zMTDuUS=>	MkixNlMxOTJ{NEi=
H2030	M{DWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MkK5TWM2OD1zMjDuUS=>	NGL6c3EzOzBzMkK0PC=>
H441	M1XTN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NEPWcWhKSzVyPUG0JI5O	NUTI[nNqOjNyMUKyOFg>
H2212	M3PG[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGHZU3JKSzVyPUG3JI5O	NEjNb2MzOzBzMkK0PC=>
SK-LU-1	NGPEdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MWnJR\|UxRTF6IH7N	NYX5WYJuOjNyMUKyOFg>
H2009	NIjhSJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MWDJR\|UxRTF7IH7N	NEPqV5QzOzBzMkK0PC=>
H1792	MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MmHUTWM2OD1{MDDuUS=>	MX[yN\|AyOjJ2OB?=
COR-L23	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NH7uR\|NKSzVyPUKyJI5O	MkizNlMxOTJ{NEi=
H727	M{nYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGjUeIxKSzVyPUK4JI5O	MkHONlMxOTJ{NEi=
H1734	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NFHiXVRKSzVyPUK4JI5O	NI\yVHIzOzBzMkK0PC=>
H358	M3Lv[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M1;OUWlEPTB;Mkmgcm0>	NXnCcGdXOjNyMUKyOFg>
A549	NIrjd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MnjITWM2OD12MzDuUS=>	MkC1NlMxOTJ{NEi=
H2122	NYDTUIlTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M4jkeWlEPTB;NUOgcm0>	M3f0V\|I{ODF{MkS4
Calu-1	M{D2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mn[5TWM2OD13ODDuUS=>	NXLXfIxnOjNyMUKyOFg>
Calu-6	NFTLeZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M1nBTmlEPTB;NkSgcm0>	NWG0NlBCOjNyMUKyOFg>
NCI-H1975	NEPnS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MWi0PEBp		MmXLTWM2OD1zNjDuUS=>	NWrtbm1wOjJzNES2OlU>
NCI-H1975	M3;iemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2TpRVczKGh?		MVzJR\|UxRThibl2=	NIXQZ5IzOjF2NE[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 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03783949	Recruiting	Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Carcinoma	Universitaire Ziekenhuizen Leuven\|European Commission	November 30 2018	Phase 2
NCT03783949	Recruiting	Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Carcinoma	Universitaire Ziekenhuizen Leuven\|European Commission	November 30 2018	Phase 2
NCT02637375	Withdrawn	Breast Cancer	University of Chicago	May 2016	Not Applicable
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
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

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)

客户使用Selleck该产品发表文献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 2019-03-27)

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