2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. HSP Apoptosis
  4. Ganetespib

Ganetespib  (Synonyms: STA-9090)

Cat. No.: HY-15205 Purity: 99.94%
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Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 85 In-stock
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10 mg USD 110 In-stock
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Customer Review

Based on 42 publication(s) in Google Scholar

Ganetespib Related Antibodies

Top Publications Citing Use of Products

32 Publications Citing Use of MCE Ganetespib

IHC
WB

    Ganetespib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45.  [Abstract]

    Levels of HSP70, and phosphorylation and total protein of p38, ERK, JNK, JAK2, STAT3, IκB-α and p65 in total cell lysates are analysed using Western blotting with or without ganetespib (100 nM).

    Ganetespib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45.  [Abstract]

    Confocal immunofluorescence microscopy is performed on cultures that are immunoreacted with antibodies against HSP90β and phospho-Tyr705-STAT3 at 6-h recovery after heat shock with or without ganetespib (100 nM) and HSP90β esiRNA.

    Ganetespib purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2019 Apr;39(4):1767-1775.  [Abstract]

    Ganetespib suppresses epidermal growth factor receptor (EGFR) and its related downstream pathway molecules in non-small cell lung cancer cells with acquired resistance to EGFR-tyrosine kinase inhibitor. Cells are treated with the indicated concentration of ganetespib for 24 h, and lysates were analyzed by western blot. AKT: protein kinase B; EMT: epithelial-mesenchymal transition; MET: met proto-oncogene; amp: amplification; MAPK: mitogen-activated protein kinase.

    Ganetespib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Sep 10;34(3):411-426.e19.  [Abstract]

    Immunoblot of HSP70 expression in RD cells after treatment with Ganetespib (GSP) alone or CPT-11+NSC-67574.

    Ganetespib purchased from MedChemExpress. Usage Cited in: Cell Stress Chaperones. 2018 Sep;23(5):1137-1142.  [Abstract]

    Western blot analysis of human bladder cancer cell lysates (T24) treated with DMSO, the Hsp90 inhibitor STA9090, the Hsp70 inhibitors VER155008, and MAL3-101 or combinations of the various inhibitors. The blot is probed with a keratin 9 mouse monoclonal antibody

    Ganetespib purchased from MedChemExpress. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.

    Immunoblot of HEK293T-REx cells inducibly expressing dn-cHSF1 following pretreatment with vehicle or dox (18 h; 1 pg/mL) and then HSR activation by treatment with arsenite (6 h; 100 pM) or STA-9090 (6 h; 100 nM).

    Ganetespib purchased from MedChemExpress. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.

    Immunoblot of HEK293T-Rex cells upon treatment with increasing concentrations of the HSP90 inhibitor STA-9090.

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

    Protein level by immunoblotting for HSR target proteins.

    Ganetespib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2015 Aug 3;5:12728.  [Abstract]

    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 MedChemExpress. Usage Cited in: Oncotarget. 2015 Nov 24;6(37):39821-38.  [Abstract]

    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.

    View All HSP Isoform Specific Products:

    View All Isoforms
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3[1][2][3][4][5][6].

    IC50 & Target[1]

    HSP90

     

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    15 nM
    Compound: 6; STA9090
    Cytotoxicity against human A375 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Cytotoxicity against human A375 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 26844689]
    HCT-116 GI50
    0.15 μM
    Compound: 2; STA-9090
    Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
    		[PMID: 32683166]
    HeLa IC50
    11.65 nM
    Compound: 3
    Antiproliferative activity against human HeLa cells by MTT assay
    Antiproliferative activity against human HeLa cells by MTT assay
    		[PMID: 31839539]
    NCI-H2228 IC50
    13 nM
    Compound: 6; STA9090
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 26844689]
    NCI-H3122 IC50
    10 nM
    Compound: 6; STA9090
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 26844689]
    PC-3 IC50
    9.3 nM
    Compound: 3
    Antiproliferative activity against human PC3 cells by MTT assay
    Antiproliferative activity against human PC3 cells by MTT assay
    		[PMID: 31839539]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Ganetespib Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    364.40

    Formula

    C20H20N4O3
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (274.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (27.44 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    SDS (393 KB)

    COA (260 KB) LCMS (93 KB) Elemental Analysis Report (118 KB)

    Handling Instructions (2659 KB)
    References
    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]

    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7442 mL 13.7212 mL 27.4424 mL 68.6059 mL
    5 mM 0.5488 mL 2.7442 mL 5.4885 mL 13.7212 mL
    10 mM 0.2744 mL 1.3721 mL 2.7442 mL 6.8606 mL
    15 mM 0.1829 mL 0.9147 mL 1.8295 mL 4.5737 mL
    20 mM 0.1372 mL 0.6861 mL 1.3721 mL 3.4303 mL
    25 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
    30 mM 0.0915 mL 0.4574 mL 0.9147 mL 2.2869 mL
    40 mM 0.0686 mL 0.3430 mL 0.6861 mL 1.7151 mL
    50 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
    60 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1434 mL
    80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8576 mL
    100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
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    Ganetespib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ganetespib888216-25-9STA-9090STA9090STA 9090HSPApoptosisHeat shock proteinsInhibitorinhibitorinhibit

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