506166
p53 Modulator, CP-31398 - CAS 259199-65-0 - Calbiochem
Synonym(s):
Nʹ-(2-(2-(4-Methoxyphenyl)ethenyl)-4-quinazolinyl)-N,N-dimethyl-1,3-propanediamine, 2HCl, p53 Activator V
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assay
≥90% (HPLC)
form
solid
color
yellow
solubility
DMSO: 50 mg/mL
General description
A cell-permeable styrylquinazoline compound that protects wild-type p53 against heat-induced denaturation and locks newly synthesized mutant p53 in an active conformation as determined by mAb PAb1620 reactivity and DNA binding in both intact cells and in cell-free assays. Shown to induce p21WAF1 and Bax expressions and apoptosis (2.5 to 10 μg/ml) in mutant p53-carrying, but not p53-null, cells. Reported to suppress the growths of human cancer cells, A375-S2 and DLD-1, in mice (100 mg/kg/day; i.p.) and Azoxymethane-induced colorectal cancer in F344 rats (supplemented at 100 to 400 ppm in animal feed) in vivo. Unlike PRIMA-1, CP-31398 directly targets the DBD (DNA binding domain) of p53. Also known to induce p53-independent cytotoxicity in cultures at concentrations above 15 μg/ml.
Preparation Note
Solution unstable. Prepare solution just prior to use.
Storage Class
10-13 - German Storage Class 10 to 13
Regulatory Information
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Thomas M Rippin et al.
Oncogene, 21(14), 2119-2129 (2002-04-12)
The Pfizer compound CP-31398 has been reported to stabilize the core domain of the tumour suppressor p53 in vitro and be an effective anti-cancer drug by virtue of rescuing destabilized mutants of p53. We did not detect any interaction between
B A Foster et al.
Science (New York, N.Y.), 286(5449), 2507-2510 (2000-01-05)
Compounds that stabilize the DNA binding domain of p53 in the active conformation were identified. These small synthetic molecules not only promoted the stability of wild-type p53 but also allowed mutant p53 to maintain an active conformation. A prototype compound
Wenge Wang et al.
Molecular and cellular biology, 23(6), 2171-2181 (2003-03-04)
CP-31398, a styrylquinazoline, emerged from a high throughput screen for therapeutic agents that restore a wild-type-associated epitope (monoclonal antibody 1620) on the DNA-binding domain of the p53 protein. We found that CP-31398 can not only restore p53 function in mutant