[CAS NO. 548472-68-0] Nutlin-3

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PRODUCTS SPECIFICATIONS [548472-68-0]

Catalog

HY-50696

Brand

MCE

CAS

548472-68-0

DESCRIPTION [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

For research use only. We do not sell to patients.

13 Publications Citing Use of MCE

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

In Vitro:

Ethanol : 100 mg/mL ( 171.97 mM ; Need ultrasonic)

DMSO : ≥ 50 mg/mL ( 85.99 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% EtOH >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% EtOH >> 90% corn oil

Solubility: 5 mg/mL (8.60 mM); Clear solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

2-Piperazinone, 4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-, rel-

Piperazinone, 4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-, rel-

rel-4-[[(4R,5S)-4,5-Bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone

cis-4-[[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-yl]carbonyl]piperazin-2-one

Nutlin 3

N 6287