Nutlin 3a

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Cat.No. 6075 - Nutlin 3a | C30H30Cl2N4O4 | CAS No. 675576-98-4
Description: MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
Chemical Name: 4-[[(4S,5R)-4,5-Bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

MDM2 antagonist (IC50 = 90 nM); inhibits the MDM2-p53 interaction. Active enantiomer of Nutlin-3 (Cat. No. 3984). Induces expression for P53 regulated genes. Suppresses tumor growth in vivo >98% in prostate cancer and osteosarcoma cancer models. Antiproliferative.

Technical Data

M. Wt 581.49
Formula C30H30Cl2N4O4
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 675576-98-4
PubChem ID 11433190
InChI Key BDUHCSBCVGXTJM-WUFINQPMSA-N
Smiles ClC1=CC=C([C@H]2[C@H](N(C(N3CC(NCC3)=O)=O)C(C4=CC=C(OC)C=C4OC(C)C)=N2)C5=CC=C(Cl)C=C5)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 58.15 100
ethanol 58.15 100

Preparing Stock Solutions

The following data is based on the product molecular weight 581.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.72 mL 8.6 mL 17.2 mL
5 mM 0.34 mL 1.72 mL 3.44 mL
10 mM 0.17 mL 0.86 mL 1.72 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References

References are publications that support the biological activity of the product.

Tovar et al (2006) Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc.Natl.Acad.Sci.USA. 103 1888 PMID: 16443686

Vassilev et al (2004) In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303 844 PMID: 14704432


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