Ganetespib (STA-9090)

Name: Ganetespib (STA-9090)
Brand: Selleck Chemicals
SKU: S1159
Rating: 5 (31 reviews)

For research use only.

Catalog No.S1159

31 publications

Ganetespib (STA-9090) Chemical Structure

Molecular Weight(MW): 364.4

Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.

Selleck's Ganetespib (STA-9090) has been cited by 31 publications

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

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 Discov, 2020, 10(5):674-687

PubMed: 32213539 ( click the link to review the publication )

Onco Targets Ther, 2020, 13:2997-3011

PubMed: 32308431 ( click the link to review the publication )

Nat Commun, 2019, 10(1):402

PubMed: 30679438 ( click the link to review the publication )

PLoS Biol, 2019, 17(3):e3000178

PubMed: 30865623 ( click the link to review the publication )

Theranostics, 2019, 9(2):554-572

PubMed: 30809293 ( click the link to review the publication )

Cell Death Dis, 2019, 10(12):911

PubMed: 31801945 ( click the link to review the publication )

Endocr Relat Cancer, 2019, 10.1530/ERC-18-0509

PubMed: 30730850 ( click the link to review the publication )

Food Chem Toxicol, 2019, 132:110645

PubMed: 31254591 ( click the link to review the publication )

Front Endocrinol (Lausanne), 2019, 10:487

PubMed: 31379752 ( click the link to review the publication )

Haematologica, 2019, 10.3324/haematol.2019.220871

PubMed: 31439673 ( click the link to review the publication )

ACS Chem Neurosci, 2019, 10(6):2890-2902

PubMed: 31017387 ( click the link to review the publication )

Hepatology, 2019, 69(2):573-586

PubMed: 29356025 ( click the link to review the publication )

Transl Lung Cancer Res, 2019, 8(4):340-351

PubMed: 31555510 ( click the link to review the publication )

Mol Cell, 2018, 69(4):594-609

PubMed: 29452639 ( click the link to review the publication )

Autophagy, 2018, 14(6):958-971

PubMed: 29561705 ( click the link to review the publication )

Mol Cancer Res, 2018, 10.1158/1541-7786

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

Oncotarget, 2018, 9(43-:27242-27255

PubMed: 29930762 ( click the link to review the publication )

Nat Commun, 2017, 8(1):422

PubMed: 28871086 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(9):1779-1790

PubMed: 28619753 ( click the link to review the publication )

Sci Rep, 2017, 7(1):1232

PubMed: 28450729 ( click the link to review the publication )
Toxicol Appl Pharmacol, 2017, 329:282-292

PubMed: 28624441 ( click the link to review the publication )

Oncotarget, 2017, 8(25):41294-41304

PubMed: 28476040 ( 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 )

Hum Mol Genet, 2015, 10.1093/hmg/ddv136

PubMed: 25877301 ( 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 )

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

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

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Description

Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.

Targets

HSP90 ^[1]
(OSA 8 cells)

4 nM

In vitro

The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. ^[1] Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. ^[1] Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. ^[2] Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. ^[3] Ganetespib treatment rapidly caused the degradation of known Hsp90 client proteins, exhibits superior potency to the ansamycin inhibitor 17-AAG, and shows sustained activity even with short exposure times.^[3] In anohter study, Ganetespib induces apoptosis of malignant canine mast cell lines. Ganetespib is active at significantly lower concentrations for C2 and BR canine malignant mast cells with IC50 of 19 and 4 nM, respectively, while 17-AAG inhibits C2 and BR canine malignant mast cells with IC50 of 958 and 44 nM, respectively. ^[4] Both the expression of WT and mutant Kit are downregulated by 100 nM Ganetespib after 24 hours in all lines treated including C2 and BMCMCs cells. However, no effects on PI3K or HSP90 expression are observed following treatment with Ganetespib.^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HL60	MXLBdI9xfG:\|aYOgRZN{[Xl?	MYGzNE85OC9zNUCvNlUxKG6P	NVXXOJloOjRxNEivO\|IhcA>?		NVX3ZYgxcW6mdXPld{Bld3OnIHTldIVv\GGwdDDpcoR2[3Srb36gc4Yh[XCxcITvd4l{	MXuyOVg5OjV3MB?=
MV411	NWrIcGY4SXCxcITvd4l{KEG\|c3H5	Mn3nN\|AwQDBxMUWwM\|I2OCCwTR?=	NUftXYpQOjRxNEivO\|IhcA>?		M4TldIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=>	M2C5WVI2QDh{NUWw
MGC-803	NXrQe2VwS2WubDDWbYFjcWyrdImgRZN{[Xl?	M1jnd\|AvOS1zMECwJI5O	MUO3NkBp		MWrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	NFrKflczPTV7MEiwOS=>
SGC-7901	Mlr3R4VtdCCYaXHibYxqfHliQYPzZZk>	M1XWclAvOS1zMECwJI5O	NYXXNIV{PzJiaB?=		Mk[zbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	M2jZdlI2PTlyOEC1
MKN-28	Ml23R4VtdCCYaXHibYxqfHliQYPzZZk>	NVPpcZF[OC5zLUGwNFAhdk1?	NVjxVWY5PzJiaB?=		NXe5RYNJcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	NXLmZ4prOjV3OUC4NFU>
MGC-803	MULGeY5kfGmxbjDBd5NigQ>?	NV62Z3VsOC5zLUGwNFAhdk1?	MUGyOEBp		NHrOTVdqdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R?	MUCyOVU6ODhyNR?=
HCT-116	MYrGeY5kfGmxbjDBd5NigQ>?	MlzrOVBvVQ>?	NInOO5EzPCCq	M{\mVmROW09?	NELYfopqdmS3Y3XkJGcxN0dzIHHydoV{fA>?	NFnXc3gzPTJzMEe5OC=>
HT-29	NVO2XGp5TnWwY4Tpc44hSXO\|YYm=	NE\DXYU2OG6P	Ml;SNlQhcA>?	NG\pXZVFVVOR	NHjDW\|RqdmS3Y3XkJGcxN0dzIHHydoV{fA>?	MYKyOVIyODd7NB?=
SCC25	Mny5R5l1d3irY3n0fUBCe3OjeR?=	NHfCTHgyOC93MDDuUS=>	M2OxTVI1KGh?		Ml3k[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5	NV;N[nFTOjV{MEW0N\|A>
FUDA	NHfhOGtEgXSxeHnjbZR6KEG\|c3H5	NHvjfG0yOC93MDDuUS=>	NEK0dZMzPCCq		NIfWdFVl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk>	MXuyOVIxPTR\|MB?=
Detroit562	M321fGN6fG:6aXPpeJkhSXO\|YYm=	MVOxNE82OCCwTR?=	MoXmNlQhcA>?		M1nvPYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:\|ZTDk[ZBmdmSnboTsfS=>	MlzRNlUzODV2M{C=
CAL27	NELS[YhEgXSxeHnjbZR6KEG\|c3H5	NEL6WYgyOC93MDDuUS=>	Mm[xNlQhcA>?		NYm1OlZQ\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6	M1;iXlI2OjB3NEOw
DSH1	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NX3ibHNWUUN3ME22JI5O	M1;NUFI1Pzh2OEO5
SW-1710	NXTDfXZbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NV\hS2VrUUN3ME22JI5O	NHK1SZgzPDd6NEizPS=>
T24	M{XPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXvJR\|UxRTdibl2=	MYOyOFc5PDh\|OR?=
RT112	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVvJR\|UxRTlibl2=	NIC4W4wzPDd6NEizPS=>
639-V	NX\aTI9CT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M33nZ2lEPTB;MUCgcm0>	NYDiOpA1OjR5OES4N\|k>
SCaBER	NXjwZVhOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NV3Fd5ZUUUN3ME2xNEBvVQ>?	M3n5RlI1Pzh2OEO5
BFTC	NXXjfZZCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NUXHV2NGUUN3ME2xO{BvVQ>?	NFy0W3kzPDd6NEizPS=>
J82	MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlOyTWM2OD1zODDuUS=>	MV[yOFc5PDh\|OR?=
HT-1376	MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnXVTWM2OD1{MTDuUS=>	NYPSdXY2OjR5OES4N\|k>
647-V	NWHDUHlNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MlzDTWM2OD1{NzDuUS=>	NFjpNIEzPDd6NEizPS=>
UM-UC3	MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mo\STWM2OD1\|MzDuUS=>	NGnuNWkzPDd6NEizPS=>
LB831-BLC	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MV3JR\|UxRTN2IH7N	MXeyOFc5PDh\|OR?=
KU-19-19	M4rVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MkHTTWM2OD1\|NjDuUS=>	M2LhcVI1Pzh2OEO5
35612	MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYDJR\|UxRTN6IH7N	NHrXb4IzPDd6NEizPS=>
5637	Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mn\ZTWM2OD12NDDuUS=>	M4K2cVI1Pzh2OEO5
HT-1197	M3;0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MorqTWM2OD13MzDuUS=>	M371UVI1Pzh2OEO5
MGH-U3	NITwXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NVTWRnlPUUN3ME21N{BvVQ>?	MVyyOFc5PDh\|OR?=
TCCSUP	M1PJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M3rFUGlEPTB;MUSyJI5O	NHvFcWozPDd6NEizPS=>
RT4	MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlHZTWM2OD1zN{OzJI5O	NFjaUlczPDd6NEizPS=>
SW780	M{LRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MnniTWM2OD1\|NEWxJI5O	MV[yOFc5PDh\|OR?=
RKO	M1u1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NXK2ZW14UUN3ME20JI5O	NWPYcFlSOjR4OEK3OFc>
LS-411 N	MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M2CzN2lEPTB;NTDuUS=>	NYflZmh2OjR4OEK3OFc>
SW620	NVPyZoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MUPJR\|UxRThibl2=	NHzxNHEzPDZ6Mke0Oy=>
HCT-15	NHHBbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M17LbGlEPTB;ODDuUS=>	MlLYNlQ3QDJ5NEe=
HuTu-80	NHXpdZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M4P0UmlEPTB;MUOgcm0>	NWS0eodKOjR4OEK3OFc>
HCT 116	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUjJR\|UxRTF2IH7N	NWLuZ2U6OjR4OEK3OFc>
COLO-205	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NXfvOplIUUN3ME2xOEBvVQ>?	M{\4UFI1Pjh{N{S3
NCI-H747	NGH4TWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MUHJR\|UxRTF5IH7N	MlS5NlQ3QDJ5NEe=
COLO-678	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUHJR\|UxRTJzIH7N	MViyOFY5Ojd2Nx?=
LoVo	NEm2VGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3XvUWlEPTB;MkKgcm0>	M1\HblI1Pjh{N{S3
LS-1034	NVK1eIwxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NEDmOmdKSzVyPUOxJI5O	MVKyOFY5Ojd2Nx?=
SNU-C2B	NYWzWoZzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmntTWM2OD12NTDuUS=>	NUDQNHk4OjR4OEK3OFc>
LS-123	NYLNUHpVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MX\JR\|UxRTd\|IH7N	M{XXWlI1Pjh{N{S3
SK-CO-1	M2ewWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MVjJR\|UxRThzIH7N	NIO2OFkzPDZ6Mke0Oy=>
HCC2998	MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M{jHVGlEPTB;MUK4JI5O	NWfGXVN[OjR4OEK3OFc>
MDA-MB-231	NUTzc3I6TnWwY4Tpc44hSXO\|YYm=	NEO4bXMyODBibl2=	MWqzNEBucW5?		M1;2R4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z	MoWwNlQzPDh{NkW=
MDA-MB-435	M3jRZ2Z2dmO2aX;uJGF{e2G7	NIrVUpQyODBibl2=	NGjSb4c{OCCvaX6=		NILZZolqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?=	MUSyOFI1QDJ4NR?=
BT-20	M3nGTmZ2dmO2aX;uJGF{e2G7	NXi1VIY{OTByL{K1NEBvVQ>?	M3LEVVI1KGh?		NFr3Xm9z\XO3bITl[EBqdiCjIHTvd4Uu\GWyZX7k[Y51KGSnc4ThZoltcXqjdHnvckBw\iCHR1\SMEBKT0ZvSWKsJG1GXCxiYX7kJGNTSUZ?	MUSyOFE4OzV2MR?=
MDA-MB-231	NWTOdIo5TnWwY4Tpc44hSXO\|YYm=	M2DUXVExOCCwTR?=	NXX6c4p5OjRiaB?=		MnjDbY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=>	M3fTd\|I1OTd\|NUSx
H82	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHrtNlZKSzVyPUOwMlI4KG6P	MnPRNlQyPjZ3MEW=
GLC4	M4fuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXHJR\|UxRTJyLkS3JI5O	MnPMNlQyPjZ3MEW=
H69	NEfF[YJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXmxR5hPUUN3ME24N{4{PiCwTR?=	NGLs[GozPDF4NkWwOS=>
H128	M3OzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NYrneHl[UUN3ME22PU42PSCwTR?=	M1:wVFI1OTZ4NUC1
H146	M{GzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NX3nZZZPUUN3ME2yPE42OSCwTR?=	M{\xe\|I1OTZ4NUC1
H187	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MlywTWM2OD1{ND65PUBvVQ>?	NXG4N5RJOjRzNk[1NFU>
H526	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWTJR\|UxRTJzLk[0JI5O	MXmyOFE3PjVyNR?=
N592	Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MknkTWM2OD1zND6xNkBvVQ>?	M4XsTlI1OTZ4NUC1
H620	NIHmVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MofKTWM2OD1\|Mj62O{BvVQ>?	NUDR[YZiOjRzNk[1NFU>
H792	MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NGPJd4RKSzVyPUS1MlA4KG6P	MUCyOFE3PjVyNR?=
H1173	NYn2VZhpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NF:zfWFKSzVyPUGyMlYzKG6P	NXraPXg1OjRzNk[1NFU>
AC3	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NFuwVJRKSzVyPUK1Mlkhdk1?	MXeyOFE3PjVyNR?=
H82	MWXGeY5kfGmxbjDBd5NigQ>?	M3LTdFMxKG6P	NYLDSm1bPzJiaB?=		NWPMOXFTcW6mdXPld{Bx\XK\|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1	M1\UeFI1OTZ4NUC1
GLC4	MonGSpVv[3Srb36gRZN{[Xl?	NFGzS2o{OCCwTR?=	M3z0[lczKGh?		MlvjbY5lfWOnczDw[ZJ{cXO2ZX70JGczN01icHjhd4Uh[XK{ZYP0	MnrTNlQyPjZ3MEW=
H146	M2DG[GZ2dmO2aX;uJGF{e2G7	NH\FflA{OCCwTR?=	NXLINlhRPzJiaB?=		NUXN[YNzcW6mdXPld{Bx\XK\|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1	NHrw[\|kzPDF4NkWwOS=>
OVCAR-5	MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NUnjXo0yOC1zMECwJI5O	NHr6bpc4OiCq		NI\0XGtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	NYDLOlRYOjN7MECxN\|Y>
OVCAR-8	NXPrdGNTS2WubDDWbYFjcWyrdImgRZN{[Xl?	Ml[yNE0yODByIH7N	Ml3vO\|IhcA>?		NX[1VHl{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	MmOwNlM6ODBzM{[=
A1847	MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NUTBZ2QzOC1zMECwJI5O	NHzoNnM4OiCq		MWnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	Mn7wNlM6ODBzM{[=
SKOV-3	NV\PRZZqS2WubDDWbYFjcWyrdImgRZN{[Xl?	MXSwMVExODBibl2=	MnPqO\|IhcA>?		MX3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	MnPBNlM6ODBzM{[=
OVCAR-5	NXe4WHhKSXCxcITvd4l{KEG\|c3H5	M4q1c\|ExNTFyMDDuUS=>	MlvENlQwPDhxN{KgbC=>		MWnpcoR2[2W\|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7	MlzLNlM6ODBzM{[=
OVCAR-8	NX3IW\|lKSXCxcITvd4l{KEG\|c3H5	NWnzOZNPOTBvMUCwJI5O	NEP4dGYzPC92OD:3NkBp		NGfsdWNqdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5	NWnBW2VkOjN7MECxN\|Y>
A1847	Mne3RZBweHSxc3nzJGF{e2G7	M4DjRVExNTFyMDDuUS=>	NW\veWFTOjRxNEivO\|IhcA>?		MXfpcoR2[2W\|IHHwc5B1d3OrczD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfGy7	NWPrU21wOjN7MECxN\|Y>
H2228	NFf5bm5E\WyuIG\pZYJqdGm2eTDBd5NigQ>?	M1q3TlAuOTByMDDuUS=>	MXi3NkBp		MlrkTWM2OD1zMzDuUS=>	NYXhSZVFOjN3M{OyOlU>
H3122	M1XHS2NmdGxiVnnhZoltcXS7IFHzd4F6	MmTENE0yODByIH7N	NHK1Uow4OiCq		M3;rZmlEPTB;MUCgcm0>	NVPPNZZPOjN3M{OyOlU>
K008	NUDGUIRSS2WubDDWbYFjcWyrdImgRZN{[Xl?				M3Hyc2lEPTB;NkCgcm0>	NGDqdW4zOzRzOEWyNy=>
K028	MlnPR4VtdCCYaXHibYxqfHliQYPzZZk>				M3XQR2lEPTB;OESgcm0>	M1fGWlI{PDF6NUKz
K029	NELlUmdE\WyuIG\pZYJqdGm2eTDBd5NigQ>?				MorZTWM2OD12NjDuUS=>	NUXnSFV6OjN2MUi1NlM>
M23	M{jGO2NmdGxiVnnhZoltcXS7IFHzd4F6				NWfZco1iUUN3ME2zO{42KG6P	MVeyN\|QyQDV{Mx?=
K033	MmPDR4VtdCCYaXHibYxqfHliQYPzZZk>				M1;veGlEPTB;N{WuOUBvVQ>?	NIS3bnYzOzRzOEWyNy=>
K008	MY\GeY5kfGmxbjDBd5NigQ>?	MYeyOVAhdk1?	MkLwNlQhcA>?		MUnpcoR2[2W\|IFeyJIFzemW\|dB?=	M2Dkc\|I{PDF6NUKz
K028	MYjGeY5kfGmxbjDBd5NigQ>?	M4fJTVI2OCCwTR?=	M1PJ[FI1KGh?		NU\XPWdscW6mdXPld{BIOiCjcoLld5Q>	MWOyN\|QyQDV{Mx?=
K029	Mle3SpVv[3Srb36gRZN{[Xl?	MXyyOVAhdk1?	M1joW\|I1KGh?		Ml:5bY5lfWOnczDHNUBienKnc4S=	MVqyN\|QyQDV{Mx?=
M23	NHTER3BHfW6ldHnvckBCe3OjeR?=	NVvUNJhHOjVyIH7N	NWLuNmN4OjRiaB?=		MVnpcoR2[2W\|IFexJIFv\CCJMj;NJIFzemW\|dB?=	MYqyN\|QyQDV{Mx?=
K033	MonHSpVv[3Srb36gRZN{[Xl?	MYiyOVAhdk1?	MVuyOEBp		NWiybIRYcW6mdXPld{BiKG2xZHXzeEBqdmO{ZXHz[UBqdiCJMTDwc5B2dGG2aX;u	NEfQNJEzOzRzOEWyNy=>
K008	MWPBdI9xfG:\|aYOgRZN{[Xl?	NEHp[ngyODBibl2=	MWS3NkBp		MWLzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{	NWnXZ\|BkOjN2MUi1NlM>
K028	NYK1SGJSSXCxcITvd4l{KEG\|c3H5	Mo\MNVAxKG6P	M4\FWVczKGh?		MoTod4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>?	M3PkWVI{PDF6NUKz
K029	MYrBdI9xfG:\|aYOgRZN{[Xl?	M1nqR\|ExOCCwTR?=	NEXLOFE4OiCq		Ml;Zd4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>?	MX6yN\|QyQDV{Mx?=
M23	MVnBdI9xfG:\|aYOgRZN{[Xl?	M1\GbVExOCCwTR?=	NVjP[WhPPzJiaB?=		M{i4PZNq\26rZnnjZY51dHliaX7keYNmeyCjcH;weI9{cXN?	M1eyTVI{PDF6NUKz
K033	NUn1[3d7SXCxcITvd4l{KEG\|c3H5	M1fzeFExOCCwTR?=	MYW3NkBp		MmTod4lodmmoaXPhcpRtgSCrbnT1Z4V{KGGyb4D0c5Nqew>?	MUSyN\|QyQDV{Mx?=
RD	M3voT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFjwSXZKSzVyPUigcm0>	NIX6NHAzOzNyM{e0NS=>
Rh41	NY\BfXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NUjsb5VGUUN3ME2xNE41KG6P	M3vIb\|I{OzB\|N{Sx
Rh18	NVnDSpRVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M{PEemlEPTB;Nj6yJI5O	NUL1fpBWOjN\|MEO3OFE>
Rh30	M{OyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NIPYcYdKSzVyPUWuOkBvVQ>?	MkHINlM{ODN5NEG=
BT-12	NVnCcpgxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NEnLPJdKSzVyPUG0MlMhdk1?	M1\vPFI{OzB\|N{Sx
CHLA-266	NEPQ[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NWHBSGJqUUN3ME2yO{4yKG6P	NIHKbnkzOzNyM{e0NS=>
TC-71	MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MXnJR\|UxRTRwNTDuUS=>	NIPPN5QzOzNyM{e0NS=>
CHLA-9	NYXxfVVzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NVfIR21JUUN3ME20MlYhdk1?	MWKyN\|MxOzd2MR?=
CHLA-10	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M1KxeWlEPTB;NT63JI5O	NG\nboczOzNyM{e0NS=>
CHLA-258	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MXvJR\|UxRTZwNDDuUS=>	MX[yN\|MxOzd2MR?=
SJ-GBM2	M3Tyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MUfJR\|UxRTF{Lkmgcm0>	M3:3VlI{OzB\|N{Sx
NB-1643	M1u4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NETxcYpKSzVyPUeuOEBvVQ>?	NIDSe4wzOzNyM{e0NS=>
NB-EBc1	NVnrSYFET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MXTJR\|UxRTF4Lkigcm0>	NH3HdogzOzNyM{e0NS=>
CHLA-90	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MXvJR\|UxRTJ{LkOgcm0>	M{GyfVI{OzB\|N{Sx
CHLA-136	NUDEc3Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmXRTWM2OD1{Mz6yJI5O	NFK0dZUzOzNyM{e0NS=>
NALM-6	NGrwdYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NFewdnJKSzVyPUGxMlchdk1?	NY\0Nmc{OjN\|MEO3OFE>
COG-LL-317	NEX5OIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NX61OHA6UUN3ME20MlQhdk1?	M3Tjb\|I{OzB\|N{Sx
RS4;11	NYT2XppzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NFTZdXlKSzVyPUGzMlUhdk1?	MnjRNlM{ODN5NEG=
MOLT-4	NUT3dlg4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MlPQTWM2OD1zMD62JI5O	NYLuXnl5OjN\|MEO3OFE>
CCRF-CEM (1)	NULq[2pqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVHJR\|UxRTF{LkWgcm0>	NX3neHlkOjN\|MEO3OFE>
CCRF-CEM (2)	M{\DXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M1K4ZmlEPTB;Nz6yJI5O	NX3OZVF3OjN\|MEO3OFE>
Kasumi-1	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NGjTNGtKSzVyPUWuPEBvVQ>?	NVnSRYVTOjN\|MEO3OFE>
Karpas-299	NXv3PWo2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NG\ZZVhKSzVyPUmuOkBvVQ>?	NHX0XYkzOzNyM{e0NS=>
Ramos-RA1	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NX3tcnZFUUN3ME23MlQhdk1?	M2\zXVI{OzB\|N{Sx
LNCaP	M3K4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFXYbHNKSzVyPUigcm0>	Moe0NlMyPTJyMES=
VCaP	NFjwbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M4C0bGlEPTB;NzDuUS=>	NFHzTHMzOzF3MkCwOC=>
H1355	NI\MbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NHmySYZKSzVyPUWgcm0>	M1vPXlI{ODF{MkS4
H157	M1f3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MUDJR\|UxRTdibl2=	MXKyN\|AyOjJ2OB?=
H460	MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYfodmp4UUN3ME24JI5O	NULPdFlEOjNyMUKyOFg>
IA-LM	NFjDNZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M13Ob2lEPTB;MUCgcm0>	NXLIflVvOjNyMUKyOFg>
HOP-62	NGH3WmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NVXHTFNjUUN3ME2xNUBvVQ>?	MmHJNlMxOTJ{NEi=
H23	NInKZ\|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MmLzTWM2OD1zMTDuUS=>	NV3VNpdWOjNyMUKyOFg>
H2030	M1W0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYfJR\|UxRTF{IH7N	NX3sPVJGOjNyMUKyOFg>
H441	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NWT6WY1oUUN3ME2xOEBvVQ>?	NX\OUYdJOjNyMUKyOFg>
H2212	MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MkH3TWM2OD1zNzDuUS=>	NFfX[oYzOzBzMkK0PC=>
SK-LU-1	NVvGZZN2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NWDhTlI1UUN3ME2xPEBvVQ>?	NVPqWIkyOjNyMUKyOFg>
H2009	MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXPRN29ZUUN3ME2xPUBvVQ>?	NHHOPGMzOzBzMkK0PC=>
H1792	Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MkTsTWM2OD1{MDDuUS=>	Mn32NlMxOTJ{NEi=
COR-L23	NXfRV4FsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NUPvXlc3UUN3ME2yNkBvVQ>?	MXuyN\|AyOjJ2OB?=
H727	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWXJR\|UxRTJ6IH7N	Mn\rNlMxOTJ{NEi=
H1734	M3HVXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NETCOZNKSzVyPUK4JI5O	MXmyN\|AyOjJ2OB?=
H358	NECx[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXG0b3ZVUUN3ME2yPUBvVQ>?	MojmNlMxOTJ{NEi=
A549	M3\EVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M1rIOWlEPTB;NEOgcm0>	MkLvNlMxOTJ{NEi=
H2122	M3TrU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MnTnTWM2OD13MzDuUS=>	MkXUNlMxOTJ{NEi=
Calu-1	M2\BWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NHrTVmdKSzVyPUW4JI5O	MVeyN\|AyOjJ2OB?=
Calu-6	M1vt[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFHoXHJKSzVyPU[0JI5O	M2PRXFI{ODF{MkS4
NCI-H1975	M3SzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVLLSJh1PDhiaB?=		M1:1cmlEPTB;MU[gcm0>	M2O5[VIzOTR2Nk[1
NCI-H1975	M2DDN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVjD[XVFPzJiaB?=		Mn3OTWM2OD16IH7N	M3\6e\|IzOTR2Nk[1

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK; PubMed: 23418523 PLoS One Downregulation of multiple signaling pathways by ganetespib in melanoma cells.A. Cells were treated with indicated amounts of ganetespib for 24 h. B-RAF and N-RAS mutational status of each cell line is indicated. p27(Kip1) / p21 (Cip1) / Cyclin D1 / Cyclin E / Cyclin B1 / CDK1 / CDK2 / CDK4; PubMed: 23418523 PLoS One Alterations in expression of multiple cell cycle regulating proteins induced by ganetespib. Cells were treated with indicated amounts of ganetespib for 48 h and analyzed by Western blot analysis. Relative expression levels of proteins (treated vs. control䲧疝Ỵ疞㧀疜膉痘  Survivin / Bcl-2 / Bcl-xl / Mcl-1; PubMed: 23418523 PLoS One Effect of ganetespib on the expression of antiapoptotic proteins. Cells were treated with ganetespib for 48 h and analyzed using Western blot analysis. Relative expression levels of proteins are indicated. B-RAF / C-RAF / N-RAS ; PubMed: 23418523 PLoS One Effect of ganetespib on B-RAF, C-RAF and N-RAS expression in melanoma cells.Cells were treated with indicated amounts of ganetespib for 48 h and subjected to Western blot analysis. HER2 / p-STAT3 / BIM ; PubMed: 25077897 Target Oncol NCI-H1975 cells were incubated with the indicated concentrations of ganetespib for 24 h. Cell lysates were analyzed by Western blotting. CDK1 / Cyclin D1 / Cyclin B1 / p27; PubMed: 29717218 Sci Rep Cropped Western blot images of the indicated cell cycle regulators are shown in ganetespib-treated (0–300 nM for 16 hours) BT474 and SKBR3 cells. c-PARP / c-caspase 3 / caspase 8 / c-caspase 8 / caspase 9 / c-caspase 9; PubMed: 29717218 Sci Rep Cropped images of Western blots at the target molecular weights for the indicated apoptotic markers are shown in ganetespib-treated (0, 10, 30, 100, 300 nM for 16 hours) BT474 and SKBR3 cells. ErbB2 / pErbB2 / Src / pSrc / mTOR / pmTOR / Bad / pBad / GSK3 / pGSK3; PubMed: 29717218 Sci Rep Ganetespib inhibits RTK signaling in ErbB2+ breast cancer cells. BT474 and SKBR3 cells were treated with ganetespib (0, 10, 30, 100, or 300 nM) for 16 hours, followed by Western blot analysis (cropped images) of the expression and activation/phosphorylati䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖 Wee1 / p-Wee1 / Chk1 / p-Chk1; PubMed: 27834954 Cell Death Differ Hsp90 inhibition degrades the G2/M checkpoint kinases Wee1 and Chk1. The cells were treated with 200 nM ganetespib and 75 μM carboplatin for 24 h followed by immunoblot analysis. Carboplatin treatment leads to the activation of Chk1, indicated by phospho—䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ	23418523 25077897 29717218 27834954
Growth inhibition assay	Cell viability ; PubMed: 23418523 PLoS One A. Ganetespib reduced viability. Cells were treated with varying amounts of ganetespib for 72 h and subjected to MTS assay. Data are expressed as mean±SD of three independent experiments. B. Mutational status and ganetespib IC50 of cell lines.	23418523

In vivo

Administration of Ganetespib leads to significant tumor shrinkage in several tumor xenograft models in mice and appears to be less toxic. Furthermore Ganetespib demonstrated better tumor penetration compared with tanespimycin.^[2] Ganetespib inhibits in vivo tumor growth in both malignant mast cell and OSA xenograft models. Ganetespib significantly inhibits tumor growth when dosed with two repeating cycles of 25 mg/kg/day for 3 days, with a %T/C value of 18. Ganetespib is well-tolerated, with the vehicle and Ganetespib groups having average bodyweight changes relative to the start of the study of +0.3% and -8.1% on day 17, respectively.^[4]

Protocol

Cell Research:^[1]

- Collapse

Cell lines: OSA cells
Concentrations: 0.001-1μM
Incubation Time: 5 days
Method: A total of 1.5 × 10³ OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.
(Only for Reference)

Animal Research:^[4]

- Collapse

Animal Models: Female severe combined immune-deficient (SCID) mice
Dosages: 25 mg/kg/day for 3 days
Administration: Tail vein injection
(Only for Reference)

References

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

- Collapse

Solubility (25°C)

In vitro	DMSO	40 mg/mL (109.76 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+45% PEG 300+ddH2O For best results, use promptly after mixing.	11mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Ganetespib (STA-9090) SDF

Molecular Weight	364.4
Formula	C₂₀H₂₀N₄O₃
CAS No.	888216-25-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CC(C)C1=C(O)C=C(O)C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)[N](C)C=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

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):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02192541	Terminated	Drug: Ziv-Aflibercept\|Drug: Ganetespib	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	December 2 2014	Phase 1
NCT02008877	Completed	Drug: ganetespib\|Drug: Sirolimus	Malignant Peripheral Nerve Sheath Tumors (MPNST)\|Sarcoma	Sarcoma Alliance for Research through Collaboration\|Synta Pharmaceuticals Corp.\|United States Department of Defense	December 2013	Phase 1\|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Does this inhibitor inhibit both isoforms of HSP90?
Answer:
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

Selective HSP90 Inhibitor

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
Most Potent HSP90 Inhibitor

KW-2478 : HSP90, IC50=3.8 nM.
HSP90 Inhibitor in Clinical Trial

17-AAG (Tanespimycin) : Phase III for Gastrointestinal Stromal Tumors.
Newest HSP90 Inhibitor

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

Related HSP (e.g. HSP90) Products

PU-H71 ^New

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
KNK437 ^New

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
VER155008 ^New

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.
Tanespimycin (17-AAG)

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2.

Features:Displays very low toxicity toward normal cells.
Luminespib (NVP-AUY922)

Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.
Alvespimycin (17-DMAG) HCl

Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.
Geldanamycin

Geldanamycin is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
HSP990 (NVP-HSP990)

NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM.

Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.
Elesclomol (STA-4783)

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
Onalespib (AT13387)

Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

Choose Your Country or Region

By Signaling Pathways

By product type

Ganetespib (STA-9090)