444143

MDM2 Antagonist, Nutlin-3, Racemic

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(s): MDM2 Antagonist, Nutlin-3, Racemic, MDM2 Inhibitor IV
• Empirical Formula (Hill Notation): C₃₀H₃₀Cl₂N₄O₄
• CAS Number: 548472-68-0
• Molecular Weight: 581.49
• MDL number: MFCD07784509
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (TLC and HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• solubility: DMSO: 25 mg/mL; ethanol: 25 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• 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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable