IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-Nμ-(2-methylquinolin-4-yl)urea

Uses

PQ 401, a novel diarylurea compound, is an inhibitor of insulin-like growth factor 1 receptor (IGF-1R) autophosphorylation. Also used as a potential testing agent in the treatment of breast and other IGF-1-sensitive cancers.

Definition

ChEBI: 1-(5-chloro-2-methoxyphenyl)-3-(2-methyl-4-quinolinyl)urea is a member of quinolines.

Biological Activity

Insulin-like growth factor receptor (IGF1R) inhibitor. Suppresses IGF-stimulated IGF-IR autophosphorylation with an IC 50 value of 12 μ M. Inhibits growth of MCF-7 breast cancer cells in vitro and in vivo .

in vivo

a treatment with pq401 triple per week reduced the growth rate of mcneua cells implanted into mice [1].

storage

Store at +4°C

References

[1]. gable kl, maddux ba, penaranda c, zavodovskaya m, campbell mj, lobo m, robinson l, schow s, kerner ja, goldfine id, youngren jf. diarylureas are small-molecule inhibitors of insulin-like growth factor i receptor signaling and breast cancer cell growth. mol cancer ther. 2006 apr;5(4):1079-86.
[2]. wang h, qin j, gong s, feng b, zhang y, tao j. insulin-like growth factor-1 receptor-mediated inhibition of a-type k(+) current induces sensory neuronal hyperexcitability through the phosphatidylinositol 3-kinase and extracellular signal-regulated kinase 1/2 pathways, independently of akt. endocrinology. 2014 jan;155(1):168-79.