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Nutlin-3

Cat. No. M2185
Nutlin-3 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 130 In stock
50mg USD 450 In stock
100mg USD 780 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Johann Wolfgang Goethe-Universität (2017). Figure 42. Nutlin (AbMole Bioscience; Houston, TX, USA)
Method Western Blot
Cell Lines UKF-NB-3 und UKF-NB-6 Zellen
Concentrations 1 μM
Incubation Time 24 h
Results Auch hier ist durch die kombinierte Behandlung mit 10 nM YM155 und 1 μM Nutlin-3 eine 15-fache Erhöhung des p21 Proteinlevels in UKF-NB-3 zu beobachten. Ebenfalls erfolgt ein Anstieg der γH2A.X Expression
Source Johann Wolfgang Goethe-Universität (2017). Figure 41. Nutlin (AbMole Bioscience; Houston, TX, USA)
Method Western Blot
Cell Lines UKF-NB-3 und UKF-NB-6 Zellen
Concentrations 1 μM
Incubation Time 24 h
Results Anhand der Quantifizierung ist in Abb. 41 A zu erkennen, dass die Nutlin-3 Behandlung (1 μM) einen signifikanten Anstieg von p53 in UKF-NB-3 bewirkt (3-fach).
Source Johann Wolfgang Goethe-Universität (2017). Figure 40. Nutlin (AbMole Bioscience; Houston, TX, USA)
Method Western Blot
Cell Lines UKF-NB-3 und UKF-NB-6 Zellen
Concentrations 1 μM
Incubation Time 24 h
Results Um diesen Effekt genauer zu untersuchen, wurde im Western-Blot geprüft, inwiefern die kombinierte YM155 und Nutlin-3 Behandlung einen Einfluss auf die Expression entsprechender Proteine in UKF-NB-3 und UKF-NB-6 Zellen ausübt
Source Johann Wolfgang Goethe-Universität (2017). Figure 39. Nutlin (AbMole Bioscience; Houston, TX, USA)
Method Western Blot
Cell Lines UKF-NB-3 und UKF-NB-6 Zellen
Concentrations 1 μM
Incubation Time 24 h
Results Eine kombinierte Behandlung der UKF-NB-3 und UKF-NB-6 Zellen mit 0,625 nM YM155 und 1 μM Nutlin-3 zeigt einen signifikant verstärkenden Effekt in beiden Zelllinien
Source Vitrual Biology (2015). Figure 3. Nutlin-3
Method Test for vitality with resazurin
Cell Lines NSCLC cells
Concentrations 30 μM
Incubation Time 24 h
Results On Figure 3 we selected several pathways that demonstrated an interesting dynamic in the change of significance (measured as -Log2(p-value)) of the moderately resistant cell lines in comparison with sensitive cell lines in different conditions with increased dosage of treatment by Nutlin-3.
Source Vitrual Biology (2015). Figure 1. Nutlin-3
Method Test of sensitivity of NSCLC cells to Nutlin-3
Cell Lines NSCLC cells
Concentrations 30 μM
Incubation Time 24 h
Results For further analysis we selected three cell lines: one, which was the most sensitive to Nutlin-3 – the H1944 cell line, and two, which were still reacting to Nutlin-3, but only under relatively high concentrations – H292 and A427
Protocol
Cell Experiment
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 581.49
Formula C30H30Cl2N4O4
CAS Number 548472-68-0
Purity 98.32%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.
Zhang Y, et al. Cancer Biol Ther. 2012 Aug;13(10):915-24. PMID: 22785205.

Recent advances in the therapeutic perspectives of Nutlin-3.
Secchiero P, et al. Curr Pharm Des. 2011;17(6):569-77. PMID: 21391907.

Nutlin3 blocks vascular endothelial growth factor induction by preventing the interaction between hypoxia inducible factor 1alpha and Hdm2.
LaRusch GA, et al. Cancer Res. 2007 Jan 15;67(2):450-4. PMID: 17234751.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Nutlin-3 supplier, Mdm2, inhibitors

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