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[CAS NO. 548472-68-0] Nutlin-3
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-50696 |
| Brand: | MCE |
| CAS: | 548472-68-0 |
Overview
| MDL | MFCD07784509 |
|---|---|
| Molecular Weight | 581.49 |
| Molecular Formula | C30H30Cl2N4O4 |
| SMILES | O=C1NCCN(C(N2[C@@H](C3=CC=C(Cl)C=C3)[C@@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1 |
13 Publications Citing Use of MCE
- [1]Cancer Res. 2019 Feb 1;79(3):534-545.
- [2]Cancer Lett. 2022 Feb 9;532:215588.
- [3]Cell Death Dis. 2020 Nov 12;11(11):976.
- [4]Mater Sci Eng C Mater Biol Appl. 2020 Mar;108:110403.
- [5]EBioMedicine. 2019 Oct;48:248-263.
- [6]Acta Pharmacol Sin. 2022 Aug 22.
- [7]Front Mol Biosci. 2021 Aug 19;8:697457.
- [8]Sci Rep. 2019 Nov 19;9(1):17050.
- [9]Int J Oncol. 2022 Mar;60(3):32.
- [10]Int J Mol Med. 2021 May 7.
- [11]Int J Mol Med. 2019 Apr;43(4):1758-1768.
- [12]Research Square Print. 2022 Aug.
- [13]Oncotarget. 2016 Mar 22;7(12):14458-75.
Summary
Nutlin-3 is a commercial available p53-MDM2 inhibitor, with K i of 90 nM.
IC50 & Target
Ki: 90 nM (p53-MDM2) [1]
In Vitro
Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis [2] . Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21 WAF levels and is toxic to WTp53-22RV1 cells (IC 50 , 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC 50 , >10 μM). Nutlin-3 induces p53 and p21 WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G 1 -phase fraction and decreasea S-phase fraction of all three cell lines [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model [2] . Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 100 mg/mL ( 171.97 mM ; Need ultrasonic)
DMSO : ≥ 50 mg/mL ( 85.99 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7197 mL | 8.5986 mL | 17.1972 mL |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7197 mL |
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1.
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2.
Add each solvent one by one: 10% EtOH >> 90% corn oil
Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic
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3.
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4.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic
-
5.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution
References
- [1] Yu Z, et al. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int J Mol Sci. 2014 Sep 5;15(9):15741-53.
- [2] Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.Cancer Biol Ther. Cancer Biol Ther. 2012 Aug;13(10):915-24.
- [3] Supiot S, et al. Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. Mol Cancer Ther. 2008 Apr;7(4):993-9.
Synonyms
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