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

Ganetespib (Synonyms: STA-9090)

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

Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with antitumor activity.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 120 In-stock
50 mg USD 288 In-stock
100 mg USD 528 In-stock
200 mg USD 888 In-stock
500 mg USD 1440 In-stock
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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.

    Ganetespib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.

    Western blot analysis of MCF-7 cells treated with Tan IIA at the specified concentrations for the expression of cytosolic PKC isoforms. The compound Go 6983 (GO, 20 μM) is included as a positive control.

    Ganetespib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.

    Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24 h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10 μM) is included as a positive control

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with antitumor activity.

    IC50 & Target[1]

    HSP90

     

    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
    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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).

    Mice: 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

    SMILES

    CN1C2=CC=C(N3C(NN=C3C4=CC(C(C)C)=C(O)C=C4O)=O)C=C2C=C1

    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.

    Purity: 99.56%

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    Product Name:
    Ganetespib
    Cat. No.:
    HY-15205
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