NSC 66811

Names

[ Name ]:
NSC 66811

[Synonym ]:
(2-methyl-7-[phenyl(phenylamino)methyl]-8-quinolinol)
7-[Anilino(phenyl)methyl]-2-methyl-8-quinolinol
7-(anilino(phenyl)methyl)-2-methyl-8-quinolinol
2-methyl-7-[phenyl(phenylamino)methyl]quinolin-8-ol
7-[Anilino(phenyl)methyl]-2-methylquinolin-8-ol
8-Quinolinol, 2-methyl-7-[phenyl(phenylamino)methyl]-
7-(Anilino(phenyl)-methyl)-2-methyl-8-quinolinol

Biological Activity

[Description]:

NSC 66811 is a MDM2-p53 inhibitor, with a Ki of 120 nM for binding to MDM2[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> MDM-2/p53

[In Vitro]

NSC 66811 (0, 5, 10, 20 μM) dose-dependently induces the accumulation of p53, MDM2, and p21cip1/waf due to the functional activation of p53[1]. Western Blot Analysis[1] Cell Line: HCT-116 (p53+/+ and p53-/-) cells[1]. Concentration: 0, 5, 10, 20 μM. Incubation Time: 48 h. Result: Dose-dependently induced the accumulation of p53, MDM2, and p21cip1/waf proteins in the HCT-116 human colon cancer cell line with wild-type p53. Had no effect on the levels for p53, MDM2, and p21cip1/waf protein in the isogenic HCT-116 p53-/- cell line.

[References]

[1]. Yipin Lu, et al. Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. J Med Chem. 2006 Jun 29;49(13):3759-62.

[2]. Sanjeev Shangary, et al. Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction to Reactivate p53 Function: A Novel Approach for Cancer Therapy. Annu Rev Pharmacol Toxicol. 2009;49:223-41.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
529.5±45.0 °C at 760 mmHg

[ Melting Point ]:
145 °C

[ Molecular Formula ]:
C₂₃H₂₀N₂O

[ Molecular Weight ]:
340.418

[ Flash Point ]:
274.0±28.7 °C

[ Exact Mass ]:
340.157562

[ PSA ]:
45.15000

[ LogP ]:
4.73

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.708

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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