Name: Ganetespib (STA-9090)
Price: 252.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Ganetespib (also known as STA-9090), 5-[2,4-dihydroxy-5-(1 methylethyl)phenyl]-2,4 dihydro-4-(1-methyl-1H indol-5 yl)-3H-1,2,4 triazole-3-one, is a potent small-molecule inhibitor of heat shock protein 90 (Hsp90), which binds to the ATP pocket in the N-terminus of Hsp90 resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile. Results of previous studies indicate that ganetespib exhibits antitumor activity against a broad range of human cancers, including lung cancer, prostate cancer, colon cancer, breast cancer, melanoma and leukemia.
- Properties
  - Alternative Name
    
    STA9090, STA 9090; (5Z)-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-(1-methylindol-5-yl)-1,2,4-triazolidin-3-one
    
    CAS Number
    
    888216-25-9
    
    Molecular Formula
    
    C20H20N4O3
    
    Molecular Weight
    
    364.4
    
    Appearance
    
    A solid
    
    Purity
    
    99.85%
    
    Solubility
    
    insoluble in H2O; ≥18.22 mg/mL in DMSO; ≥6.4 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Shuai Zhao, Lanlan Zhou, et al. "Anti-cancer efficacy including Rb-deficient tumors and VHL-independent HIF1α proteasomal destabilization by dual targeting of CDK1 or CDK4/6 and HSP90." Sci Rep. 2021 Oct 22;11(1):20871. PMID:34686682
    2. Diwei Zheng, Weihai Liu, et al. "AHA1 upregulates IDH1 and metabolic activity to promote growth and metastasis and predicts prognosis in osteosarcoma." Signal Transduct Target Ther. 2021 Jan 20;6(1):25. PMID:33468990
    3. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
    4. Karney-Grobe S, Russo A, et al. "HSP90 is a chaperone for DLK and is required for axon injury signaling." Proc Natl Acad Sci U S A. 2018 Oct 16;115(42):E9899-E9908. PMID:30275300
    5. Khurana N, Kim H, et al. "Multimodal actions of the phytochemical sulforaphane suppress both AR and AR-V7 in 22Rv1 cells: Advocating a potent pharmaceutical combination against castration-resistant prostate cancer." Oncol Rep. 2017 Aug 30. PMID:28901514
    6. Li QQ, Hao JJ, et al. "Proteomic analysis of proteome and histone post-translational modifications in heat shock protein 90 inhibition-mediated bladder cancer therapeutics." Sci Rep. 2017 Mar 15;7(1):201. PMID:28298630

Ganetespib (STA-9090)

Ganetespib (STA-9090)

Background

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