| In Vitro | Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM, only in cells with wild-type p53 such as HCT116, RKO and SJSA-1, but not in the mutant p53 cell lines SW480 and MDA-MB-435. |
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| In Vivo | Oral administration of Nutlin-3 at 200 mg/kg twice daily for 3 weeks significantly inhibits the tumor growth of SJAS-1 xenografts by 90%, comparable with the effect of doxorubicin treatment with 81% inhibition of tumor growth. |
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| Animal model | Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells |
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| Formulation & Dosage | Formulated in 2% Klucel, 0.5% Tween 80; 100 mg/kg; Oral BID |
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| References | [1] Vassilev LT, et al. Science, 2004, 303(5659), 844-848. |
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