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444143 Sigma-Aldrich

MDM2 Antagonist, Nutlin-3, Racemic - CAS 548472-68-0 - Calbiochem

The MDM2 Antagonist, Nutlin-3, Racemic, also referenced under CAS 548472-68-0, controls the biological activity of MDM2. This small molecule/inhibitor is primarily used for Cancer applications.

Synonym: MDM2 Antagonist, Nutlin-3, Racemic - CAS 548472-68-0 - Calbiochem, MDM2 Inhibitor IV

  • CAS Number 548472-68-0

  • Empirical Formula (Hill Notation) C30H30Cl2N4O4

  • Molecular Weight 581.49

  •  MDL number MFCD07784509

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Properties

Quality Level   100
assay   ≥98% (TLC and HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
solubility   DMSO: 25 mg/mL
  ethanol: 25 mg/mL
shipped in   wet ice
InChI   1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)
InChI key   BDUHCSBCVGXTJM-UHFFFAOYSA-N

Description

General description

A cell-permeable cis-imidazoline compound that acts as a potent and selective MDM2 antagonist (IC50 = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) and displays antitumor properties. Activates p53 pathway by binding MDM2 in the p53-binding pocket and inhibits MDM2-p53 interaction. Shown to suppress tumor growth by induction of apoptosis in several cancer cells with wild-type p53 and in xenografted tumor mice. A 10 mM (1 mg/172 µl) solution of MDM2 Antagonist, Nutlin-3, Racemic (Cat. No. 444151) in DMSO is also available.

A cell-permeable, potent, and selective MDM2 antagonist (IC50 = 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b) that displays antitumor properties. Activates the p53 pathway by binding MDM2 in the p53-binding pocket and inhibiting the MDM2-p53 interaction. Shown to induce apoptosis in several cancer cell lines with wild-type p53 and in xenografted tumor mice.

Packaging

1 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MDM2

Product does not compete with ATP.

Reversible: no

Target IC50: 90 nM for Nutlin-3a and 13.6 µM for Nutlin-3b

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot, purge with inert gas, and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.
Vassilev, L.T., et al. 2004. Science303, 844.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
Protocols & Articles
Peer-Reviewed Papers
15

References

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