Ganetespib (STA-9090)

Catalog No.S1159

Ganetespib 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.

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Ganetespib (STA-9090) Chemical Structure

Ganetespib (STA-9090) Chemical Structure
Molecular Weight: 364.4

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Ganetespib (STA-9090) is available in the following compound libraries:

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  • Most Potent HSP90 Inhibitor

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  • Inhibitor in Clinical Trial

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  • Newest HSP90 Inhibitor

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Product Information

  • Compare HSP (e.g. HSP90) Inhibitors
    Compare HSP (e.g. HSP90) Inhibitors
  • Research Area

Product Description

Biological Activity

Description Ganetespib 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.
Targets HSP90
IC50 4 nM [1]
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]
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]
Features

Protocol(Only for Reference)

Cell Assay: [1]

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.

Animal Study: [4]

Animal Models Female severe combined immune-deficient (SCID) mice
Dosages 25 mg/kg/day for 3 days
Administration Tail vein injection
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01562015 Recruiting Non Small Cell Lung Cancer Synta Pharmaceuticals Corp. 2012-04 Phase 2
NCT01579994 Recruiting Advanced Lung Cancer Memorial Sloan-Kettering Cancer Center 2012-04 Phase 1|Phase 2
NCT01677455 Recruiting Breast Cancer|HER-2 Positive Breast Cancer|Triple Negative Breast Cancer Synta Pharmaceuticals Corp. 2012-07 Phase 2
NCT01590160 Not yet recruiting Lung Cancer - Malignant Pleural Mesothelioma University College, London|Cancer Research UK 2012-09 Phase 1|Phase 2
NCT01798485 Recruiting Non-Small-Cell Lung Adenocarcinoma|Non-small Cell Lung Cancer Stage IIIB|Non-small Cell Lung Cancer Stage IV|Non-small Cell Lung Cancer Metastatic Synta Pharmaceuticals Corp. 2013-03 Phase 3

Chemical Information

Download Ganetespib (STA-9090) SDF
Molecular Weight (MW) 364.4
Formula

C20H20N4O3

CAS No. 888216-25-9
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 40 mg/mL (109 mM)
Water <1 mg/mL (<1 mM)
Ethanol 9 mg/mL (24 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.3644 3.644 7.288 10.932

Research Area

Tech Support & FAQs

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.

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  • Ganetespib (STA-9090)

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