Deltarasin Chemical Properties

Boiling point:

824.3±75.0 °C(Predicted)

Density 

1.23±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

solid

pka

10.35±0.10(Predicted)

color 

White

CAS DataBase Reference

1440898-61-2

Deltarasin Usage And Synthesis

Uses

Deltarasin is an inhibitior of KRAS-PDEδ which has been shown to impair oncogenic signalling.

Biological Activity

the kras oncogene product is considered a major target in anticancer drug discovery. interfering with binding of mammalian pdeδ to kras by means of small molecules provides a novel opportunity to suppress oncogenic ras signalling by altering its localization to endomembranes. deltarasin is an inhibitor of the kras-pdeδ interaction to impair oncogenic kras signalling.

in vitro

within a minute, 5 mm of deltarasin completely inhibited pdeδ-kras interaction and released the insolubilized mcitrine-rheb/kras6q to the endomembrane system. this showed that deltarasin interfered with the binding of kras to pdeδ in cells and thereby inhibited its solubilization [1].

in vivo

a clear dose-dependent reduction in panc-tu-i tumour growth rate could be observed in deltarasin treated mice with respect to the vehicle-injected controls, where the growth of tumours in mice that were treated with 10mg kg/1 bid deltarasin was almost completely blocked [1].

References

[1] zimmermann g, papke b, ismail s, vartak n, chandra a, hoffmann m, hahn sa, triola g, wittinghofer a, bastiaens pi, waldmann h. small molecule inhibition of the kras-pdeδ interaction impairs oncogenic kras signalling. nature. 2013;497(7451):638-42.

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