Ganetespib (STA-9090)

Name: Ganetespib (STA-9090)
Brand: Selleck Chemicals
SKU: S1159
Rating: 5 (37 reviews)

For research use only.

Catalog No.S1159

37 publications

Ganetespib (STA-9090) Chemical Structure

CAS No. 888216-25-9

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 37 publications

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

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 )

Cell Death Dis, 2021, 12(1):126

PubMed: 33500390 ( click the link to review the publication )

Sci China Life Sci, 2021, 10.1007/s11427-020-1860-2

PubMed: 33439458 ( 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 )

Theranostics, 2020, 10(18):8415-8429

PubMed: 32724478 ( 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 Syst Biol, 2018, 14(7):e8071

PubMed: 29997244 ( 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,

PubMed: 29599910 ( 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 (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
NCI-H1975	NFvpclFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mn;1O\|IhcA>?		MmnnTWM2OD16IH7N	NHTocmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG0OFY3PSd-MkKxOFQ3PjV:L3G+
NCI-H1975	M33zcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NH\qZlc1QCCq		MnPuTWM2OD1zNjDuUS=>	MlvvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNES2OlUoRjJ{MUS0OlY2RC:jPh?=
Calu-6	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NIfVVXZKSzVyPU[0JI5O	MoG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ\|MEGyNlQ5RC:jPh?=
Calu-1	NGTXOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M4\wRmlEPTB;NUigcm0>	M33selxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
H2122	M4DseGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NInEcYpKSzVyPUWzJI5O	NXXhRXZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
A549	Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYPJR\|UxRTR\|IH7N	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
H358	M3vj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYTJR\|UxRTJ7IH7N	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
H1734	NX3DNlNRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MX7JR\|UxRTJ6IH7N	MnnkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ\|MEGyNlQ5RC:jPh?=
H727	M1yzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXjJR\|UxRTJ6IH7N	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
COR-L23	NYXCcld1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NH\PPFhKSzVyPUKyJI5O	M1qz[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
H1792	NIfqSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NGX5[Y1KSzVyPUKwJI5O	NVjtXXpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H2009	NFPhfmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MnjpTWM2OD1zOTDuUS=>	NYPOfGpwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
SK-LU-1	NHLqPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXvlVWcxUUN3ME2xPEBvVQ>?	NVK4T4J1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H2212	M1jRTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{\4UWlEPTB;MUegcm0>	MkjMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ\|MEGyNlQ5RC:jPh?=
H441	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MlHXTWM2OD1zNDDuUS=>	MoDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUKyOFgoRjJ\|MEGyNlQ5RC:jPh?=
H2030	NEjUUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MX;JR\|UxRTF{IH7N	M3zBcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
H23	MonMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MXjJR\|UxRTFzIH7N	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
HOP-62	MnrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MXjJR\|UxRTFzIH7N	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzMkK0PEc,OjNyMUKyOFg9N2F-
IA-LM	Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVXCXlNIUUN3ME2xNEBvVQ>?	NFXUfYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{CxNlI1QCd-MkOwNVIzPDh:L3G+
H460	M1KyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mn7LTWM2OD16IH7N	NXzEVXNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwNVIzPDhpPkKzNFEzOjR6PD;hQi=>
H157	NGX0Z2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NWfyZWQ{UUN3ME23JI5O	M{XDWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
H1355	NFK3bIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MXzJR\|UxRTVibl2=	M3TlN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MEGyNlQ5Lz5{M{CxNlI1QDxxYU6=
VCaP	M1nxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mlr2TWM2OD15IH7N	Mn:2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNUKwNFQoRjJ\|MUWyNFA1RC:jPh?=
LNCaP	NIP3VZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NUHneIE2UUN3ME24JI5O	MoG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNUKwNFQoRjJ\|MUWyNFA1RC:jPh?=
Ramos-RA1	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWPJR\|UxRTdwNDDuUS=>	NGnNelc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwN\|c1OSd-MkOzNFM4PDF:L3G+
Karpas-299	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MoTtTWM2OD17Lk[gcm0>	M{O0VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{CzO\|QyLz5{M{OwN\|c1OTxxYU6=
Kasumi-1	M2LJcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MnjyTWM2OD13Lkigcm0>	MnPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
CCRF-CEM (2)	M33x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M3Psd2lEPTB;Nz6yJI5O	M13sSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{CzO\|QyLz5{M{OwN\|c1OTxxYU6=
CCRF-CEM (1)	M13ybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXrJR\|UxRTF{LkWgcm0>	NXfxXVR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFM4PDFpPkKzN\|A{PzRzPD;hQi=>
MOLT-4	MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NFLC[pJKSzVyPUGwMlYhdk1?	NEP2NY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwN\|c1OSd-MkOzNFM4PDF:L3G+
RS4;11	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVnJR\|UxRTF\|LkWgcm0>	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyM{e0NUc,OjN\|MEO3OFE9N2F-
COG-LL-317	MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M2XVUWlEPTB;ND60JI5O	MmjhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
NALM-6	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NVnLXmJRUUN3ME2xNU44KG6P	MkjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
CHLA-136	M1vWSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MoH0TWM2OD1{Mz6yJI5O	NGr6ZZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwN\|c1OSd-MkOzNFM4PDF:L3G+
CHLA-90	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVTJR\|UxRTJ{LkOgcm0>	NYGxWVZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNFM4PDFpPkKzN\|A{PzRzPD;hQi=>
NB-EBc1	M1jKO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NIGwZWNKSzVyPUG2Mlghdk1?	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyM{e0NUc,OjN\|MEO3OFE9N2F-
NB-1643	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4PyWmlEPTB;Nz60JI5O	Ml2yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
SJ-GBM2	M3Tncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M4\GXGlEPTB;MUKuPUBvVQ>?	M2jnVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{CzO\|QyLz5{M{OwN\|c1OTxxYU6=
CHLA-258	NV7rN3Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M1K5emlEPTB;Nj60JI5O	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNyM{e0NUc,OjN\|MEO3OFE9N2F-
CHLA-10	NF20VmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M2HORWlEPTB;NT63JI5O	MonFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
CHLA-9	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NVezR4xbUUN3ME20MlYhdk1?	Mlj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
TC-71	NGLBcIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MlfJTWM2OD12LkWgcm0>	Mk\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|MEO3OFEoRjJ\|M{CzO\|QyRC:jPh?=
CHLA-266	NUfCUGJUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NHG2c2JKSzVyPUK3MlEhdk1?	M4PDO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|M{CzO\|QyLz5{M{OwN\|c1OTxxYU6=
BT-12	MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MW\JR\|UxRTF2LkOgcm0>	NGLLUJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OwN\|c1OSd-MkOzNFM4PDF:L3G+
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MDA-MB-231	MX3GeY5kfGmxbjDBd5NigQ>?	NXnLfVlTOTByIH7N	NGjLcYczPCCq		Mm[5bY5pcWKrdIOgeIhmKG2rZ4LheI9zgSCjbnSgbY53[XOrdnWgZ4Fx[WOrdIpCpC=>	MlrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzN{O1OFEoRjJ2MUezOVQyRC:jPh?=
BT-20	MnrUSpVv[3Srb36gRZN{[Xl?	MY[xNFAwOjVyIH7N	MX2yOEBp		MUPy[ZN2dHSnZDDpckBiKGSxc3Wt[IVx\W6mZX70JIRme3SjYnnsbZpifGmxbjDv[kBGT0[ULDDJS2YuUVJuIF3FWEwh[W6mIFPSRWY>	M37NR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUezOVQyLz5{NEG3N\|U1OTxxYU6=
MDA-MB-435	M{\KVWZ2dmO2aX;uJGF{e2G7	MmH1NVAxKG6P	MVyzNEBucW5?		NIn0OoFqdmirYnn0d{Bi[2O3bYXsZZRqd25ib3[gTGlHNTIQsR?=	NYPVSW1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFgzPjVpPkK0NlQ5OjZ3PD;hQi=>
MDA-MB-231	Mn3ZSpVv[3Srb36gRZN{[Xl?	MlHiNVAxKG6P	Mmf2N\|AhdWmw		MXHpcohq[mm2czDhZ4N2dXWuYYTpc44hd2ZiSFnGMVHPuQ>?	Mn3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NEiyOlUoRjJ2MkS4NlY2RC:jPh?=
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RD	MWDxTHRUKGG\|c3H5				Mo\QdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{	NGnXcHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-SH	M3j2cpFJXFNiYYPzZZk>				M2njNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz	NVzaNIJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	MkHVdWhVWyCjc4PhfS=>				MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	Ml\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	MYrxTHRUKGG\|c3H5				M1rjbJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO=	NFXJSGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	MmrldWhVWyCjc4PhfS=>				M{XSOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq	M1X6RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	MXTxTHRUKGG\|c3H5				M2rRZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz	M{T1WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	MXfxTHRUKGG\|c3H5				Mon2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	MlKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	M{HHTZFJXFNiYYPzZZk>				MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?=	NUn2e3hqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5	MlXldWhVWyCjc4PhfS=>				NX3jeZhHeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz	M{nXPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18	M1q0PJFJXFNiYYPzZZk>				NIOycWxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?=	MmDJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

... 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]

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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]

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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.

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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 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)O)O

In vivo Formulation Calculator (Clear solution)

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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 μL 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)

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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)

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
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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

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

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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)
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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

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 (HSP90) Signaling Pathway Map

HSP (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 (HSP90) Products

PU-H71 ^New

PU-H71 (NSC 750424) 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

VER155008 (C07) 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Tanespimycin (17-AAG)

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 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. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

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

Luminespib (AUY-922, NVP-AUY922, VER-52296) 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. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Alvespimycin (17-DMAG) HCl

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) 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 (NSC 122750) is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
HSP990 (NVP-HSP990)

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

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.

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Ganetespib (STA-9090)