Chemical Name: N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Restores mutant p53 activity. Binds p53 DNA binding domain (Kd = 1-2 μM) and restores wild-type function to many oncogenic mutants by acting as a chaperone. Inhibits ubiquitination of p53 by HDM2. Triggers apoptosis in tumor cell lines and reduces tumor growth in a xenograft model.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility
Soluble to 100 mM in ethanol and to 10 mM in DMSO with sonication
Preparing Stock Solutions
The following data is based on the product molecular weight 563.56. 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
1.77 mL
8.87 mL
17.74 mL
5 mM
0.35 mL
1.77 mL
3.55 mL
10 mM
0.18 mL
0.89 mL
1.77 mL
50 mM
0.04 mL
0.18 mL
0.35 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Demmaet al (2010) SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. J.Biol.Chem. 285 10198 PMID: 20124408
Essmann & Schulze-Osthoff
(2012) Translational approaches targeting the p53 pathway for anti-cancer therapy. Br.J.Pharmacol. 165 328 PMID: 21718309