| In Vitro | Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) |
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| In Vivo | Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors |
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| Animal model | Nude mice bearing subcutaneous human cancer xenografts |
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| Formulation & Dosage | 1% Klucel, 0.1% Tween 80; 100, 200 mg/kg; p.o.; b.i.d |
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| References | [1] Tovar C, et al. Proc Natl Acad Sci U S A, 2006, 103(6), 1888-1893. |
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