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    Ganetespib (STA-9090)
    Ganetespib (STA-9090)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0875
    CAS #: 888216-25-9Purity ≥98%

    Description: Ganetespib (formerly STA-9090; STA 9090; STA9090), the active metabolite of STA-1474 (a prodrug of ganetespib), is a potent and triazolone-based small-molecule HSP90 (heat shock protein 90) inhibitor with potential anticancer activity. It inhibits HSP90 with an IC50 of 4 nM in OSA 8 cells, and induces apoptosis of OSA cells while normal osteoblasts are not affected. Ganetespib is being investigated for the treatment of various cancers such as  Small Cell Lung Cancer, breast cancer, Acute Myeloid Leukaemia, and Myelodysplastic Syndrome.

    References: Int J Cancer. 2009 Dec 15;125(12):2792-801; Curr Opin Investig Drugs. 2010 Dec;11(12):1466-76.

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    Molecular Weight (MW)364.4
    CAS No.888216-25-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 40 mg/mL (109.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
    SynonymsSTA-9090; Ganetespib; STA 9090; STA9090 

    Chemical Name: 5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-4-(1-methyl-1H-indol-5-yl)-2,4-dihydro-3H- 1,2,4-triazol-3-one


    InChi Code: InChI=1S/C20H20N4O3/c1-11(2)14-9-15(18(26)10-17(14)25)19-21-22-20(27)24(19)13-4-5-16-12(8-13)6-7-23(16)3/h4-11,25-26H,1-3H3,(H,22,27)

    SMILES Code: O=C1NN=C(C2=CC(C(C)C)=C(O)C=C2O)N1C3=CC4=C(N(C)C=C4)C=C3

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    In Vitro

    In vitro activity: 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. Ganetespib inhibits MG63 cell lines with IC50 of 43 NM. 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. 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. 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. 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. 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.

    Kinase Assay: 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.

    Cell Assay: 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.

    In VivoAdministration 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. 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.
    Animal modelFemale severe combined immune-deficient (SCID) mice
    Formulation & DosageDissolved in  DMSO and diluted 1:10 with 20% Cremophor RH 40; 25 mg/kg; Tail vein injection
    ReferencesInt J Cancer. 2009 Dec 15;125(12):2792-801; Curr Opin Investig Drugs. 2010 Dec;11(12):1466-76.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Ganetespib (STA-9090)

    Comparison of once-weekly and five times per week dosing of ganetespib.  2012 Sep 15;18(18):4973-85.

    Ganetespib (STA-9090)

    Ganetespib induces tumor regression in a mouse lung carcinoma model driven by ERRB2YVMA.   2012 Sep 15;18(18):4973-85.

    Ganetespib (STA-9090)

    Ganetespib accumulates in tumor relative to normal tissues and displays greater in vivo efficacy than 17-AAG.  2012 Sep 15;18(18):4973-85.  

    Ganetespib (STA-9090)

    Ganetespib (STA-9090)

    Ganetespib (STA-9090)


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