1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP

Ganetespib (Synonyms: STA-9090)

Cat. No.: HY-15205 Purity: 99.56%
Data Sheet SDS Handling Instructions

Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with IC50 of 4 nM in OSA 8 cells.

For research use only. We do not sell to patients.
Ganetespib Chemical Structure

Ganetespib Chemical Structure

CAS No. : 888216-25-9

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Customer Review

    Ganetespib purchased from MCE. Usage Cited in: Sci Rep. 2015 Aug 3;5:12728.

    Ganetespib decreases the DYRK1A protein level. 293T cells are transiently transfected with an expression vector for 3xFLAG-DYRK1A. At 24 h after transfection, the cells are treated with Ganetespib (100 nM) and collected 0 and 8 h after treatment. Total cell lysates are subjected to SDS-PAGE followed by Western blot analysis using antibodies against FLAG and GAPDH. In the control group (DMSO), expression of 3xFLAG-DYRK1A increases at 8 h compared to 0 h, and Ganetespib suppresses this increase of

    Ganetespib purchased from MCE. Usage Cited in: ACS Chem Biol. 2016 Jan 15;11(1):200-10.

    Protein level by immunoblotting for HSR target proteins.

    Ganetespib purchased from MCE. Usage Cited in: Oncotarget. 2015 Nov 24;6(37):39821-38.

    J82 cells are treated with 1 μM STA9090 and 50 μM VER155008 as mono or dual therapy for the time indicated. Lysates are prepared and Western blots probed for cell cycle markers.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with IC50 of 4 nM in OSA 8 cells.

    In Vitro

    Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 values ranging 2-30 nM in genomically-defined NSCLC cell lines. Ganetespib is also approximately 20-fold more potent in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants[1]. Ganetespib exhibits potent in vitro cytotoxicity in a range of solid and hematologic tumor cell lines, induces the degradation of known Hsp90 client proteins, displays superior potency to the ansamycin inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG)[2]. Ganetespib is a potent HSP90 inhibitor, and shown to kill canine tumor cell lines in vitro[3]. Ganetespib possesses superior JAK/STAT inhibitory activity to both P6 and 17-AAG in terms of potency or duration of response in the HEL92.1.7 cells[4].

    In Vivo

    Ganetespib (125 mg/kg, i.v.) accumulates in tumors relative to normal tissues and displays greater in vivo efficacy than 17-AAG without increased toxicity and inhibits proliferation and induces apoptosis in parallel with EGFR depletion in NCI-H1975 xenografts[1]. Ganetespib (100, 125, 150 mg/kg, i.v.) shows potent antitumor efficacy in solid and hematologic xenograft models of oncogene addiction, as evidenced by significant growth inhibition and/or regressions[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01554969 Emory University|Synta Pharmaceuticals Corp. Rectal Cancer May 2012 Phase 1
    NCT01485835 Emory University|Multiple Myeloma Research Consortium|Synta Pharmaceuticals Corp. Multiple Myeloma January 2012 Phase 1
    NCT02008877 Sarcoma Alliance for Research through Collaboration|Synta Pharmaceuticals Corp.|United States Department of Defense Malignant Peripheral Nerve Sheath Tumors (MPNST)|Sarcoma December 2013 Phase 1|Phase 2
    NCT01560416 Dana-Farber Cancer Institute Breast Cancer May 2012 Phase 2
    NCT01562015 Synta Pharmaceuticals Corp. Non Small Cell Lung Cancer April 2012 Phase 2
    NCT02261805 Georgetown University|Synta Pharmaceuticals Corp. Cancer|Small Cell Lung Cancer October 2014 Phase 1|Phase 2
    NCT01798485 Synta Pharmaceuticals Corp. 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 April 2013 Phase 3
    NCT01039519 Synta Pharmaceuticals Corp. Gastrointestinal Stromal Tumor January 2010 Phase 2
    NCT01579994 Memorial Sloan Kettering Cancer Center Advanced Lung Cancer April 2012 Phase 1
    NCT02334319 Emory University|Synta Pharmaceuticals Corp. Stage I Hypopharyngeal Squamous Cell Carcinoma|Stage I Laryngeal Squamous Cell Carcinoma|Stage I Oral Cavity Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma|Stage II Hypopharyngeal Squamous Cell Carcinoma|Stage II Laryngeal Squamous Cell Carcinoma|Stage II Oral Cavity Squamous Cell Carcinoma|Stage II Oropharyngeal Squamous Cell Carcinoma|Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma December 2014 Phase 1
    NCT01962948 Fox Chase Cancer Center|National Cancer Institute (NCI) Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer October 9, 2013 Phase 1|Phase 2
    NCT02389751 M.D. Anderson Cancer Center|Synta Pharmaceuticals Corp. Esophageal Cancer April 2015 Phase 1
    NCT02060253 Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI)|Synta Pharmaceuticals Corp.|New York University Cancer Institute HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer April 2014 Phase 1
    NCT01183364 Synta Pharmaceuticals Corp. Solid Tumor Malignancies July 2010 Phase 1
    NCT00688116 Synta Pharmaceuticals Corp. Solid Tumors October 2007 Phase 1
    NCT01677455 Synta Pharmaceuticals Corp. Breast Cancer|HER-2 Positive Breast Cancer|Triple Negative Breast Cancer|ER/Progressive Response (PR) + Refractory to Prior Hormonal Treatment July 2012 Phase 2
    NCT01590160 University College, London|Cancer Research UK Lung Cancer - Malignant Pleural Mesothelioma August 2013 Phase 1|Phase 2
    NCT02012192 Medical University Innsbruck|European Commission Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer June 2014 Phase 1|Phase 2
    NCT01348126 Synta Pharmaceuticals Corp. Non-small Cell Lung Cancer Stage IIIB|Non-small Cell Lung Cancer Stage IV|Non-small Cell Lung Cancer Metastatic May 2011 Phase 2|Phase 3
    NCT00858572 Synta Pharmaceuticals Corp. AML|CML|MDS|Myeloproliferative Disorders March 2009 Phase 1
    NCT02192541 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neoplasms July 9, 2014 Phase 1
    NCT01236144 Cardiff University|Leukaemia & Lymphoma Research Group|Experimental Cancer Medicine Centre Network Acute Myeloid Leukaemia|High Risk Myelodysplastic Syndrome April 2011 Phase 1|Phase 2
    NCT00964873 Synta Pharmaceuticals Corp. Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Blast-phase Chronic Myelogenous Leukemia|AML|ALL|CML August 2009 Phase 1
    NCT02637375 University of Chicago Breast Cancer May 2016
    NCT02272478 Cardiff University|Cancer Research UK Acute Myeloid Leukaemia|Myelodysplastic Syndrome October 2014 Phase 3
    NCT01042379 QuantumLeap Healthcare Collaborative Breast Neoplasms|Breast Cancer|Breast Tumors March 2010 Phase 2
    NCT01031225 Synta Pharmaceuticals Corp. Non Small Cell Lung Cancer November 2009 Phase 2
    NCT01167114 Massachusetts General Hospital|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp. Esophagogastric Cancer August 2010 Phase 2
    NCT01665937 Massachusetts General Hospital|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp. Hepatocellular Carcinoma August 2010 Phase 1
    NCT01273896 Memorial Sloan Kettering Cancer Center|Synta Pharmaceuticals Corp. Breast Cancer January 2011 Phase 2
    NCT01111838 Memorial Sloan Kettering Cancer Center|Synta Pharmaceuticals Corp. Colon Cancer|Rectal Cancer April 2010 Phase 2
    NCT00687934 Synta Pharmaceuticals Corp. Solid Tumors October 2007 Phase 1
    NCT01173523 David M. Jackman, MD|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Synta Pharmaceuticals Corp.|Dana-Farber Cancer Institute Small Cell Lung Cancer July 28, 2010 Phase 2
    NCT01551693 Dana-Farber Cancer Institute|Synta Pharmaceuticals Corp. Melanoma September 2011 Phase 2
    NCT01200238 Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|Brigham and Women's Hospital|Synta Pharmaceuticals Corp. Ocular Melanoma June 2010 Phase 2
    NCT01270880 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer January 2011 Phase 2
    NCT01227018 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer December 2010 Phase 2
    NCT01368003 Toni Choueiri, MD|Dana-Farber Cancer Institute Adenocarcinoma of the Prostate April 2011 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.7442 mL 13.7212 mL 27.4424 mL
    5 mM 0.5488 mL 2.7442 mL 5.4885 mL
    10 mM 0.2744 mL 1.3721 mL 2.7442 mL
    Kinase Assay
    [1]

    Exponentially growing cells are processed in lysis buffer (20 mM HEPES, pH 7.4, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) and incubated with increasing concentrations of 17-AAG or ganetespib for 30 min at 4°C, and incubated with biotin-GM linked to Dynabeads MyOne Streptavidin T1 magnetic beads for 1 h at 4°C. Beads are washed three times in lysis buffer and heated for 5 min at 95°C in SDS-PAGE sample buffer. Samples are resolved on 4-12% Bis-Tris gradient gel and Western blots are performed using an anti-HSP90 antibody. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    Cells are grown in 96-well plates based on optimal growth rates determined empirically for each line. Twenty-four hours after plating, cells are treated with the indicated compounds or controls for 72 hours. AlamarBlue is added (10% v/v) to the cells, and the plates are incubated for 3 hours and, then, subjected to fluorescence detection. For the comparative viability/apoptosis assay, NCI-H1975 cells are treated with escalating concentrations of ganetespib for the indicated time periods and subjected to viability analysis via CellTiter Fluor and apoptosis via Caspase Glo 3/7. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Ganetespib is formulated in 10/18 DRD (10% DMSO, 18% Cremophor RH 40, 3.6% dextrose and 68.4% water).

    NCI-H1975 or HCC827 cells are cultured as above and 0.5-1×107 cells are mixed with 50% RPMI 1640/50% Matrigel and subcutaneously injected into the flanks of SCID mice. For efficacy studies, animals with 100-200 mm3 tumors are then randomized into treatments groups of eight. Tumor volumes (V) are calculated by the equation V=0.5236×L×W×T (Length, width, and thickness). Animals are treated by intravenous bolus tail vein injection at 10 mL/kg with ganetespib formulated in 10/18 DRD (10% DMSO, 18% Cremophor RH 40, 3.6% dextrose and 68.4% water). As a measurement of in vivo efficacy, the relative size of treated and control tumors [(%T/C) value] is determined from the change in average tumor volumes of each drug-treated group relative to the vehicle-treated group, or itself in the case of tumor regression. Body weights are monitored daily. For biomarker studies, mice bearing NCI-H1975 xenografts are treated with either a single dose of vehicle or ganetespib, or with 5 daily doses of vehicle or ganetespib, in groups of 3 or 8, and harvested at various time points. Tumors are excised and flash frozen in liquid nitrogen for preparation of protein lysates or fixed in 10% neutral buffered formalin for immunohistochemistry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    364.4

    Formula

    C₂₀H₂₀N₄O₃

    CAS No.

    888216-25-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 32 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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