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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About This Item
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 Code
10-13 - German Storage Class 10 to 13
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