| Identification | Back Directory | [Name]
Deltarasin | [CAS]
1440898-61-2 | [Synonyms]
Deltarasin
deltarasine
Deltarasin-HCl
Deltarasin USP/EP/BP
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)- | [Molecular Formula]
C40H37N5O | [MDL Number]
MFCD26793865 | [MOL File]
1440898-61-2.mol | [Molecular Weight]
603.755 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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. |
|
|