Ganetespib (STA-9090)

Catalog No.S1159

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.

Cited by 23 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 )

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

PubMed: 29356025 ( 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 )

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

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

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

PubMed: 31017387 ( 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 )

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 )

Sci Rep, 2017, 7(1):1232

PubMed: 28450729 ( 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	M1HEPWFxd3C2b4Ppd{BCe3OjeR?=	MX[zNE85OC9zNUCvNlUxKG6P	MlvLNlQwPDhxN{KgbC=>		MlHQbY5lfWOnczDkc5NmKGSncHXu[IFvfCCrbnT1Z5Rqd25ib3[gZZBweHSxc3nz	M3jSSVI2QDh{NUWw
MV411	NHTENWRCeG:ydH;zbZMhSXO\|YYm=	MYizNE85OC9zNUCvNlUxKG6P	MknyNlQwPDhxN{KgbC=>		M2\abIlv\HWlZYOg[I9{\SCmZYDlcoRidnRiaX7keYN1cW:wIH;mJIFxd3C2b4Ppdy=>	NGPUU5ozPTh6MkW1NC=>
MGC-803	NIPIOnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NXK0PFdQOC5zLUGwNFAhdk1?	NXrlcGhEPzJiaB?=		MYfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	NVe1U2M{OjV3OUC4NFU>
SGC-7901	MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	Mn20NE4yNTFyMECgcm0>	NWTmT29FPzJiaB?=		MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	MkHKNlU2QTB6MEW=
MKN-28	MmjGR4VtdCCYaXHibYxqfHliQYPzZZk>	M4POfFAvOS1zMECwJI5O	MlfjO\|IhcA>?		MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	NWPET5dGOjV3OUC4NFU>
MGC-803	MmXuSpVv[3Srb36gRZN{[Xl?	M2G2NFAvOS1zMECwJI5O	MX[yOEBp		NEXXOY9qdmS3Y3XzJGczN01iY3XscE1kgWOuZTDhdpJme3R?	MkjpNlU2QTB6MEW=
HCT-116	MXPGeY5kfGmxbjDBd5NigQ>?	MYe1NI5O	M4\HPVI1KGh?	NXPLbWVtTE2VTx?=	NHv6V\|hqdmS3Y3XkJGcxN0dzIHHydoV{fA>?	NEP0T5czPTJzMEe5OC=>
HT-29	Ml2xSpVv[3Srb36gRZN{[Xl?	NV21c\|B{PTCwTR?=	NHH0N20zPCCq	MWTEUXNQ	NHfaUY1qdmS3Y3XkJGcxN0dzIHHydoV{fA>?	NF3HcoszPTJzMEe5OC=>
SCC25	NV3VfpoxS3m2b4jpZ4l1gSCDc4PhfS=>	M3v3XlExNzVyIH7N	NYLhcFBLOjRiaB?=		NWD6VWpP\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdiCmb4PlJIRmeGWwZHXueIx6	M4Pz[lI2OjB3NEOw
FUDA	Mm\oR5l1d3irY3n0fUBCe3OjeR?=	MXWxNE82OCCwTR?=	M4fMTlI1KGh?		MXHk[YNz\WG\|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=	MUmyOVIxPTR\|MB?=
Detroit562	NYTJfnZyS3m2b4jpZ4l1gSCDc4PhfS=>	MlS5NVAwPTBibl2=	NYDpXpNHOjRiaB?=		MUjk[YNz\WG\|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=	M3S0dFI2OjB3NEOw
CAL27	NX60RnNPS3m2b4jpZ4l1gSCDc4PhfS=>	MUexNE82OCCwTR?=	MUWyOEBp		NEjrXnBl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk>	NFzLd3czPTJyNUSzNC=>
DSH1	NFjIVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MVXJR\|UxRTZibl2=	NVq0Vo1ZOjR5OES4N\|k>
SW-1710	MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NEDadnNKSzVyPU[gcm0>	NITHXZAzPDd6NEizPS=>
T24	NYLPVoVKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NHPMVpNKSzVyPUegcm0>	NVnPU4t6OjR5OES4N\|k>
RT112	MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYLJR\|UxRTlibl2=	NWjYdYtrOjR5OES4N\|k>
639-V	Ml\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVjJR\|UxRTFyIH7N	M4W3XlI1Pzh2OEO5
SCaBER	NFrEelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NFTGfXRKSzVyPUGwJI5O	MnS3NlQ4QDR6M{m=
BFTC	NEe3fGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3zvbGlEPTB;MUegcm0>	NFjuZ2wzPDd6NEizPS=>
J82	MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NHL4XYlKSzVyPUG4JI5O	NVnHell6OjR5OES4N\|k>
HT-1376	NVXyeZZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NIS3TIhKSzVyPUKxJI5O	NH\xNlMzPDd6NEizPS=>
647-V	M3;BXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mn[xTWM2OD1{NzDuUS=>	MlLjNlQ4QDR6M{m=
UM-UC3	NF7uZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NF7mOXJKSzVyPUOzJI5O	NXy2fohCOjR5OES4N\|k>
LB831-BLC	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUTJR\|UxRTN2IH7N	M1XONVI1Pzh2OEO5
KU-19-19	M13PR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NH\PVnNKSzVyPUO2JI5O	MVqyOFc5PDh\|OR?=
35612	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4L1[WlEPTB;M{igcm0>	MXuyOFc5PDh\|OR?=
5637	M1LjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXHJR\|UxRTR2IH7N	Mn30NlQ4QDR6M{m=
HT-1197	MkDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M1XaW2lEPTB;NUOgcm0>	MlLiNlQ4QDR6M{m=
MGH-U3	NV\EZpVST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVXJR\|UxRTV\|IH7N	MoDxNlQ4QDR6M{m=
TCCSUP	Mn;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MojhTWM2OD1zNEKgcm0>	MX6yOFc5PDh\|OR?=
RT4	Mk[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NWfGUpRXUUN3ME2xO\|M{KG6P	NX;i[3ZpOjR5OES4N\|k>
SW780	NUfaXI9xT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NV24SodtUUN3ME2zOFUyKG6P	NYfVUXJDOjR5OES4N\|k>
RKO	NYDsU2huT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NFXmWYlKSzVyPUSgcm0>	Mo\CNlQ3QDJ5NEe=
LS-411 N	M4DPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NEnDWZFKSzVyPUWgcm0>	MYqyOFY5Ojd2Nx?=
SW620	Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M{C4fmlEPTB;ODDuUS=>	M2\NW\|I1Pjh{N{S3
HCT-15	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHf1To9KSzVyPUigcm0>	NUXPUHYyOjR4OEK3OFc>
HuTu-80	M2K5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MWjJR\|UxRTF\|IH7N	M3;CWlI1Pjh{N{S3
HCT 116	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NGjnPXhKSzVyPUG0JI5O	M4Tnc\|I1Pjh{N{S3
COLO-205	M3vlSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M4jtemlEPTB;MUSgcm0>	NETkT40zPDZ6Mke0Oy=>
NCI-H747	NXzQSI51T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NILlZXVKSzVyPUG3JI5O	MUeyOFY5Ojd2Nx?=
COLO-678	Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NFKwdHdKSzVyPUKxJI5O	MVuyOFY5Ojd2Nx?=
LoVo	M2jSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{LpWGlEPTB;MkKgcm0>	MYeyOFY5Ojd2Nx?=
LS-1034	M2TRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MkP5TWM2OD1\|MTDuUS=>	MmnvNlQ3QDJ5NEe=
SNU-C2B	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWHJR\|UxRTR3IH7N	NEHCXpkzPDZ6Mke0Oy=>
LS-123	NGfIOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MXXJR\|UxRTd\|IH7N	NH\XR2MzPDZ6Mke0Oy=>
SK-CO-1	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NWnYcoJSUUN3ME24NUBvVQ>?	NFXhb\|MzPDZ6Mke0Oy=>
HCC2998	Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVnJR\|UxRTF{ODDuUS=>	MWqyOFY5Ojd2Nx?=
MDA-MB-231	NX3sTnIxTnWwY4Tpc44hSXO\|YYm=	NXO5RZhQOTByIH7N	MUWzNEBucW5?		M1HrSIlvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z	NYjHfll4OjR{NEiyOlU>
MDA-MB-435	NHTjO4hHfW6ldHnvckBCe3OjeR?=	MWWxNFAhdk1?	NVfVdGxGOzBibXnu		M2fqV4lvcGmkaYTzJIFk[3WvdXzheIlwdiCxZjDITWYuOc7z	NUHi[4Z6OjR{NEiyOlU>
BT-20	Mlr0SpVv[3Srb36gRZN{[Xl?	M{TR[VExOC9{NUCgcm0>	NYWwZlRyOjRiaB?=		Ml7WdoV{fWy2ZXSgbY4h[SCmb4PlMYRmeGWwZHXueEBl\XO2YXLpcIl7[XSrb36gc4YhTUeIUjygTWdHNUmULDDNSXQtKGGwZDDDVmFH	M1ThOFI1OTd\|NUSx
MDA-MB-231	M4HobmZ2dmO2aX;uJGF{e2G7	NX7TdW9iOTByIH7N	NH7KRVczPCCq		M1LMXYlvcGmkaYTzJJRp\SCvaXfyZZRwenliYX7kJIlvfmG\|aY\lJINieGGlaYT5xsA>	MlfFNlQyPzN3NEG=
H82	M3fwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MV3JR\|UxRTNyLkK3JI5O	NWH2WWNIOjRzNk[1NFU>
GLC4	NHnQbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3H5PGlEPTB;MkCuOFchdk1?	NXvWeJA6OjRzNk[1NFU>
H69	M1PVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NW\kfoR7UUN3ME24N{4{PiCwTR?=	MWSyOFE3PjVyNR?=
H128	M2DZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYTJR\|UxRTZ7LkW1JI5O	NUXqe216OjRzNk[1NFU>
H146	M{LGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MmXzTWM2OD1{OD61NUBvVQ>?	M2L1U\|I1OTZ4NUC1
H187	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NVjCTopUUUN3ME2yOE46QSCwTR?=	MYmyOFE3PjVyNR?=
H526	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NUfPRWZIUUN3ME2yNU43PCCwTR?=	MofNNlQyPjZ3MEW=
N592	NUHmfYxLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmjTTWM2OD1zND6xNkBvVQ>?	MlLrNlQyPjZ3MEW=
H620	M1LzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MX;JR\|UxRTN{Lk[3JI5O	M3;Vc\|I1OTZ4NUC1
H792	NYHP[VlVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NXG4e5liUUN3ME20OU4xPyCwTR?=	NF7O[5QzPDF4NkWwOS=>
H1173	Mn:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MkfDTWM2OD1zMj62NkBvVQ>?	MkK3NlQyPjZ3MEW=
AC3	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MXzJR\|UxRTJ3Lkmgcm0>	MmDlNlQyPjZ3MEW=
H82	M3\sOGZ2dmO2aX;uJGF{e2G7	NFLxXmc{OCCwTR?=	NFnsOIY4OiCq		NWXCenFYcW6mdXPld{Bx\XK\|aYP0[Y51KEd{L12gdIhie2ViYYLy[ZN1	NH;RTngzPDF4NkWwOS=>
GLC4	NHHEZ3VHfW6ldHnvckBCe3OjeR?=	NVrIfGJROzBibl2=	NGG2Omo4OiCq		MYPpcoR2[2W\|IIDldpNqe3SnboSgS\|IwVSCyaHHz[UBienKnc4S=	MWqyOFE3PjVyNR?=
H146	NEHE[3lHfW6ldHnvckBCe3OjeR?=	MVKzNEBvVQ>?	MmDOO\|IhcA>?		NIrhU2tqdmS3Y3XzJJBmenOrc4TlcpQhTzJxTTDwbIF{\SCjcoLld5Q>	NYPXOJZyOjRzNk[1NFU>
OVCAR-5	MnfNR4VtdCCYaXHibYxqfHliQYPzZZk>	MofSNE0yODByIH7N	M2DpS\|czKGh?		M4TXNYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	NEm5NlczOzlyMEGzOi=>
OVCAR-8	M4K3UmNmdGxiVnnhZoltcXS7IFHzd4F6	NEXCTmwxNTFyMECgcm0>	MnzqO\|IhcA>?		M{jN[olvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	M{LRNlI{QTByMUO2
A1847	MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MWmwMVExODBibl2=	MVO3NkBp		M2LzTIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	M2PkZ\|I{QTByMUO2
SKOV-3	MkjsR4VtdCCYaXHibYxqfHliQYPzZZk>	M4flfFAuOTByMDDuUS=>	NUnQ[3ZTPzJiaB?=		MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	NEDLPXEzOzlyMEGzOi=>
OVCAR-5	MX7BdI9xfG:\|aYOgRZN{[Xl?	NWnmPY5mOTBvMUCwJI5O	MWOyOE81QC95MjDo		NHu5fo5qdmS3Y3XzJIFxd3C2b4Ppd{B1cW2nIHHu[EBld3OnIHTldIVv\GWwdHz5	NHGxZXczOzlyMEGzOi=>
OVCAR-8	NHzZcWVCeG:ydH;zbZMhSXO\|YYm=	NHfDOGsyOC1zMECgcm0>	NIXSRZUzPC92OD:3NkBp		M4rSS4lv\HWlZYOgZZBweHSxc3nzJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62bIm=	MnzLNlM6ODBzM{[=
A1847	NGr5O2ZCeG:ydH;zbZMhSXO\|YYm=	NFP0bnkyOC1zMECgcm0>	MnLRNlQwPDhxN{KgbC=>		NWDaSIZucW6mdXPld{BieG:ydH;zbZMhfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboTsfS=>	NIWwOoczOzlyMEGzOi=>
H2228	MnrnR4VtdCCYaXHibYxqfHliQYPzZZk>	NGTqRmIxNTFyMECgcm0>	MnuxO\|IhcA>?		M1XNVGlEPTB;MUOgcm0>	NWO0V5NEOjN3M{OyOlU>
H3122	NYn3cmhnS2WubDDWbYFjcWyrdImgRZN{[Xl?	NYX3UFVmOC1zMECwJI5O	NXH4XJgzPzJiaB?=		NG\penZKSzVyPUGwJI5O	M3XlW\|I{PTN\|Mk[1
K008	MorPR4VtdCCYaXHibYxqfHliQYPzZZk>				NX;OVG5wUUN3ME22NEBvVQ>?	MYOyN\|QyQDV{Mx?=
K028	NH;ITWxE\WyuIG\pZYJqdGm2eTDBd5NigQ>?				NEj0WmtKSzVyPUi0JI5O	NV3KcotnOjN2MUi1NlM>
K029	NUHwVo1FS2WubDDWbYFjcWyrdImgRZN{[Xl?				Mni0TWM2OD12NjDuUS=>	MkD6NlM1OTh3MkO=
M23	Mnz5R4VtdCCYaXHibYxqfHliQYPzZZk>				NXS1T4FmUUN3ME2zO{42KG6P	M{KxclI{PDF6NUKz
K033	NVriUYZ3S2WubDDWbYFjcWyrdImgRZN{[Xl?				NIXYfZlKSzVyPUe1MlUhdk1?	MkDDNlM1OTh3MkO=
K008	MUnGeY5kfGmxbjDBd5NigQ>?	NG\zfo4zPTBibl2=	MXeyOEBp		NVO3N4lKcW6mdXPld{BIOiCjcoLld5Q>	MojQNlM1OTh3MkO=
K028	MXLGeY5kfGmxbjDBd5NigQ>?	MonmNlUxKG6P	NIDvb24zPCCq		MVzpcoR2[2W\|IFeyJIFzemW\|dB?=	MoD0NlM1OTh3MkO=
K029	M17MfmZ2dmO2aX;uJGF{e2G7	NWL6foxuOjVyIH7N	NX;VXVB1OjRiaB?=		MVfpcoR2[2W\|IFexJIFzemW\|dB?=	NUHhVJpPOjN2MUi1NlM>
M23	MV3GeY5kfGmxbjDBd5NigQ>?	NXK2XHRQOjVyIH7N	M1rYWVI1KGh?		NXHaeWlycW6mdXPld{BIOSCjbnSgS\|IwVSCjcoLld5Q>	M3;EOlI{PDF6NUKz
K033	M4nib2Z2dmO2aX;uJGF{e2G7	NFrHZlgzPTBibl2=	Ml7LNlQhcA>?		NITzcHpqdmS3Y3XzJIEhdW:mZYP0JIlv[3KnYYPlJIlvKEdzIIDvdJVt[XSrb36=	MYOyN\|QyQDV{Mx?=
K008	MmXzRZBweHSxc3nzJGF{e2G7	M2mwZVExOCCwTR?=	Mmr6O\|IhcA>?		NXjsXGVne2mpbnnmbYNidnSueTDpcoR2[2W\|IHHwc5B1d3Orcx?=	NGHqOWszOzRzOEWyNy=>
K028	MXHBdI9xfG:\|aYOgRZN{[Xl?	NU\tRmpVOTByIH7N	M1HLb\|czKGh?		NF;MWHh{cWewaX\pZ4FvfGy7IHnu[JVk\XNiYYDvdJRwe2m\|	Ml3oNlM1OTh3MkO=
K029	NXnCeXFFSXCxcITvd4l{KEG\|c3H5	MWqxNFAhdk1?	MUS3NkBp		NWexcGxTe2mpbnnmbYNidnSueTDpcoR2[2W\|IHHwc5B1d3Orcx?=	MnmzNlM1OTh3MkO=
M23	NVWyOXQ4SXCxcITvd4l{KEG\|c3H5	NV3nbIM{OTByIH7N	M1L6bVczKGh?		MXfzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{	M{DhdVI{PDF6NUKz
K033	NV;XXm05SXCxcITvd4l{KEG\|c3H5	NE\6WmUyODBibl2=	M1rwVVczKGh?		MUnzbYdvcW[rY3HueIx6KGmwZIXj[ZMh[XCxcITvd4l{	MXKyN\|QyQDV{Mx?=
RD	M33wWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGC0VXRKSzVyPUigcm0>	NV;OS29mOjN\|MEO3OFE>
Rh41	MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MonJTWM2OD1zMD60JI5O	NYLSUHhwOjN\|MEO3OFE>
Rh18	M1nQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MWDJR\|UxRTZwMjDuUS=>	NVzFNYJ6OjN\|MEO3OFE>
Rh30	M{[2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGPJbJNKSzVyPUWuOkBvVQ>?	NV7ETnJSOjN\|MEO3OFE>
BT-12	NUX0e2E{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MoXmTWM2OD1zND6zJI5O	NWrGVXUxOjN\|MEO3OFE>
CHLA-266	M2faZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mmf2TWM2OD1{Nz6xJI5O	M4m5NlI{OzB\|N{Sx
TC-71	NFTvdGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M{T0VWlEPTB;ND61JI5O	MVKyN\|MxOzd2MR?=
CHLA-9	M1v3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M3m2UWlEPTB;ND62JI5O	NX:4OJl1OjN\|MEO3OFE>
CHLA-10	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NWXOflR{UUN3ME21Mlchdk1?	MoK2NlM{ODN5NEG=
CHLA-258	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MmjqTWM2OD14LkSgcm0>	MWqyN\|MxOzd2MR?=
SJ-GBM2	NIHDNWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M{LjbmlEPTB;MUKuPUBvVQ>?	NWDRTXJQOjN\|MEO3OFE>
NB-1643	M4XQXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MmG5TWM2OD15LkSgcm0>	M4LWSlI{OzB\|N{Sx
NB-EBc1	MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlL1TWM2OD1zNj64JI5O	Ml\TNlM{ODN5NEG=
CHLA-90	NED2cZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NGG2VWdKSzVyPUKyMlMhdk1?	Mn23NlM{ODN5NEG=
CHLA-136	NVT1dVZET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVTJR\|UxRTJ\|LkKgcm0>	M3u5blI{OzB\|N{Sx
NALM-6	MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NX7BRVJlUUN3ME2xNU44KG6P	MmDhNlM{ODN5NEG=
COG-LL-317	MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYj1cXF1UUN3ME20MlQhdk1?	MXKyN\|MxOzd2MR?=
RS4;11	M3fiXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2TuTGlEPTB;MUOuOUBvVQ>?	NX3nNolWOjN\|MEO3OFE>
MOLT-4	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NFXsfmhKSzVyPUGwMlYhdk1?	MUCyN\|MxOzd2MR?=
CCRF-CEM (1)	NVfuOVlGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NHPXOZdKSzVyPUGyMlUhdk1?	NV;UXJZuOjN\|MEO3OFE>
CCRF-CEM (2)	NFHR[2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MX3JR\|UxRTdwMjDuUS=>	M4\ON\|I{OzB\|N{Sx
Kasumi-1	NHuzc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MnXrTWM2OD13Lkigcm0>	MViyN\|MxOzd2MR?=
Karpas-299	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHLRUHNKSzVyPUmuOkBvVQ>?	NH32coIzOzNyM{e0NS=>
Ramos-RA1	Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXLRe\|ZvUUN3ME23MlQhdk1?	MmnGNlM{ODN5NEG=
LNCaP	NVTHN5BTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MojVTWM2OD16IH7N	M2[zc\|I{OTV{MEC0
VCaP	MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4HvSWlEPTB;NzDuUS=>	NUDQN4t4OjNzNUKwNFQ>
H1355	M1rWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NWW1[GFGUUN3ME21JI5O	MkKyNlMxOTJ{NEi=
H157	MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVLJR\|UxRTdibl2=	M3HwVVI{ODF{MkS4
H460	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NV;WOXdZUUN3ME24JI5O	NYL1SGZvOjNyMUKyOFg>
IA-LM	M2jmSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NVLIPFJuUUN3ME2xNEBvVQ>?	MkLoNlMxOTJ{NEi=
HOP-62	NFXuUpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYXJR\|UxRTFzIH7N	MmXCNlMxOTJ{NEi=
H23	NGmwbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NH24fGlKSzVyPUGxJI5O	NHvTRY8zOzBzMkK0PC=>
H2030	M{TKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NXH4cFdxUUN3ME2xNkBvVQ>?	MlTXNlMxOTJ{NEi=
H441	NX;T[Hl{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYjTVWJLUUN3ME2xOEBvVQ>?	NGjSbVEzOzBzMkK0PC=>
H2212	M{PKT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXzJR\|UxRTF5IH7N	NW\BZnFoOjNyMUKyOFg>
SK-LU-1	NFfzToxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3z2NWlEPTB;MUigcm0>	MlnDNlMxOTJ{NEi=
H2009	NUixTZFtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MX7JR\|UxRTF7IH7N	M33NOFI{ODF{MkS4
H1792	MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXWzemFKUUN3ME2yNEBvVQ>?	NFrBfmgzOzBzMkK0PC=>
COR-L23	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NX;GUnBzUUN3ME2yNkBvVQ>?	M4n6eVI{ODF{MkS4
H727	MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlTOTWM2OD1{ODDuUS=>	MViyN\|AyOjJ2OB?=
H1734	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MoTZTWM2OD1{ODDuUS=>	NEPxS2wzOzBzMkK0PC=>
H358	NEjRfIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MoX0TWM2OD1{OTDuUS=>	NWfzdJg2OjNyMUKyOFg>
A549	NEO1OJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MmDqTWM2OD12MzDuUS=>	NFPKdYszOzBzMkK0PC=>
H2122	MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Ml[xTWM2OD13MzDuUS=>	NHv3RpkzOzBzMkK0PC=>
Calu-1	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NWCzTGNkUUN3ME21PEBvVQ>?	M{jFeVI{ODF{MkS4
Calu-6	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHLqVIdKSzVyPU[0JI5O	MYiyN\|AyOjJ2OB?=
NCI-H1975	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mo\iOFghcA>?		NGP4eZVKSzVyPUG2JI5O	NEHvSVIzOjF2NE[2OS=>
NCI-H1975	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MoPsO\|IhcA>?		M37ZNGlEPTB;ODDuUS=>	MkTyNlIyPDR4NkW=

... 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 Formulation: In DMSO and diluted 1:10 with 20% Cremophor RH 40 Dosages: 25 mg/kg/day for 3 days Administration: Tail vein injection (Only for Reference)

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
Formulation: In DMSO and diluted 1:10 with 20% Cremophor RH 40
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

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 2019-10-14)

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 (AUY-922, 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)

Cited by 23 Publications

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Ganetespib (STA-9090) SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

Tech Support

Frequently Asked Questions

HSP (e.g. HSP90) Signaling Pathway Map

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

Related HSP (e.g. HSP90) Products

Choose Your Country or Region

By Signaling Pathways

By product type

Ganetespib (STA-9090)

Cited by 23 Publications

Purity & Quality Control

Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Ganetespib (STA-9090) SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

Tech Support

Frequently Asked Questions

HSP (e.g. HSP90) Signaling Pathway Map

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

Related HSP (e.g. HSP90) Products

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