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    GDC-0152
    GDC-0152

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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 #: V0052
    CAS #: 873652-48-3 (free base);Purity ≥98%

    Description: GDC-0152 (RG-7419) is a novel and potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM in cell-free assays, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. It is under Phase 1 trial. GDC-0152 binds to the BIR domain of ML-IAP and the BIR3 domains of XIAP, cIAP1 and cIAP2 with values of inhibition constant Ki of 14 nM, 28 nM, 17 nM and 43 nM respectively. GDC-0152 potentially inhibits tumor growth of breast cancer by promoting cIAP1 degradation and inducing caspase-3/7 activation which result in the decreasing of cell viability of breast cancer cells with normal epithelial cells unaffected. 

    References: J Med Chem. 2012 May 10;55(9):4101-13.

    Related CAS: 873581-21-6 (HCl)

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    Molecular Weight (MW)498.64
    FormulaC25H34N6O3S
    CAS No.873652-48-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 99 mg/mL (198.5 mM)
    Water: 3 mg/mL (6.0 mM)
    Ethanol: 99 mg/mL (198.5 mM)
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 5mg/mL
    Synonym/Chemical NameGDC0152; GDC0152; GDC 0152; RG 7419; RG-7419; RG7419.; (2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide


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    In VitroGDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac.
    In VivoGDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma−protein binding of GDC-0152 is moderate and comparable among mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) over the range of concentrations investigated (0.1−100 μM); higher plasma−protein binding is observed in rabbits (95−96%).
    Animal modelHuman-tumor xenograft mouse models of MDA-MB-231 breast cancer
    Formulation & Dosagephosphate-buffered saline; 10, 50, 100 mg/kg; Oral
    References[1] Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.


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

    GDC-0152

     

    GDC-0152

     

    GDC-0152

    Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.


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