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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 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 1440898-61-2.mol |  |
| | 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. |
| | Deltarasin Preparation Products And Raw materials |
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