Name: SAR245409 (XL765)
Price: 306.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SAR245409 (XL765) is a selective dual inhibitor of PI3K and mTOR (IC50= 9 nM for PI3Kγ).
    PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.
    In PA cell lines, combination of XL765 and TMZ blocked the cell growth and led to apoptosis [1]. In a variety of tumor cell lines that mutated on PI3K signaling, XL765 inhibited PIP3 formation in the membrane and AKT/p70S6K/S6 phosphorylation [2].
    In GH3 xenograft tumor mouse models, combination use of XL765 and TMZ inhibited tumor growth, reduced serum GH and prolactin levels with no increased systemic side effects [1]. In severe combined immunodeficient mice, XL765 abolished MPNST local and metastatic growth. [3]. In multiple human xenograft models in nude mice, repeat dose administration showed significant tumor growth inhibition that related to antiproliferative and antiangiogenic response etc. [2]
    
    1. Dai C, Zhang B, Liu X et al. Inhibition of PI3K/AKT/mTOR pathway enhances temozolomide-induced cytotoxicity in pituitary adenoma cell lines in vitro and xenografted pituitary adenoma in female nude mice. Endocrinology. 2013 Mar;154(3):1247-59.
    2. Yu P, Laird AD, Du X et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol Cancer Ther. 2014 May;13(5):1078-91.
    3. Ghadimi MP, Lopez G, Torres KE et al. Targeting the PI3K/mTOR axis, alone and in combination with autophagy blockade, for the treatment of malignant peripheral nerve sheath tumors. Mol Cancer Ther. 2012 Aug;11(8):1758-69.
- Properties
  - Alternative Name
    
    N-[4-[[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-3-methoxy-4-methylbenzamide
    
    CAS Number
    
    1349796-36-6
    
    Molecular Formula
    
    C31H29N5O6S
    
    Molecular Weight
    
    599.66
    
    Appearance
    
    A solid
    
    Purity
    
    97.25%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥15 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

SAR245409 (XL765)

SAR245409 (XL765)

Background

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