Nutlin-3 is a small molecule inhibitor of the MDM2/p53 interaction, which leads to the non-genotoxic p53 stabilization, activation of cell cycle arrest and apoptosis pathways. Nutlin-3 inhibits the MDM2-p53 interaction with IC50 of 0.09 μM and synergistically activates p53 to suppress tumor growth. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1. Nutlin-3 is currently in phase I clinical trial for the treatment of retinoblastoma.
Ecotoxicol Environ Saf. 2022 Jun 1;237:113564.
Environmental BPDE induced human trophoblast cell apoptosis by up-regulating lnc-HZ01/p53 positive feedback loop
Nutlin-3 purchased from AbMole
Cell Experiment | |
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Cell lines | wild-type p53 (HCT116, RKO, and SJSA-1) and mutant p53 (MDA-MB-435 and SW480) cell lines |
Preparation method | Effect of the enantiomers of Nutlin-3 on the growth and viability of cancer cells with wild-type p53 (HCT116, RKO, and SJSA-1) and mutant p53 (MDA-MB-435 and SW480). Cells were grown, treated, and analyzedAntiproliferative and cytotoxic activity of Nutlin-1. Exponentially growing cancer cells with wild-type p53 (HCT116, RKO, and SJSA-1) or mutant p53 (MDA-MB-435 and SW480) were incubated with a range of concentrations for 5 days and the cell mass and viability were measured by the MTT assay. |
Concentrations | 0~30µM |
Incubation time | 5 days |
Animal Experiment | |
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Animal models | Nude mice bearing subcutaneous human cancer xenografts |
Formulation | 2% Klucel, 0.5% Tween 80 |
Dosages | 200 mg/kg twice daily for 3 weeks |
Administration | oral gavage |
Molecular Weight | 581.49 |
Formula | C30H30Cl2N4O4 |
CAS Number | 548472-68-0 |
Solubility (25°C) | DMSO ≥ 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Secchiero P, et al. Curr Pharm Des. Recent advances in the therapeutic perspectives of Nutlin-3.
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