product name Deltarasin
Description: Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. The KRAS oncogene product is considered a major target in anticancer drug discovery. 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
References: Nature. 2013 May 30;497(7451):638-42.
603.75
Formula
C40H37N5O
CAS No.
1440898-61-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (165.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/L
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In liver cells, Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by Deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts. |
| Animal model | Mice bearing Panc-Tu-I xenografts |
| Formulation & Dosage | Dissolved in 10% PLR and 5% DMSO; 10 mg/kg; Administered through i.p. |
| References | Nature. 2013 May 30;497(7451):638-42. |
