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Deltarasin

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Deltarasin Basic information

Product Name:
Deltarasin
Synonyms:
  • Deltarasin
  • Deltarasin-HCl
  • 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole
  • 1H-Benzimidazole,2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-
  • deltarasine
  • Deltarasin USP/EP/BP
  • (S)-1-benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole
  • Deltarasin,Phosphodiesterase (PDE),inhibit,Inhibitor,Ras
CAS:
1440898-61-2
MF:
C40H37N5O
MW:
603.75
Product Categories:
  • Inhibitors
  • API
Mol File:
1440898-61-2.mol
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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
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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.

DeltarasinSupplier

Shanghai Boyle Chemical Co., Ltd.
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