| Description | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
| In vitro | 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. [1] |
| In vivo | Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumor cell xenografts [1]. The finding may inspire novel drug discovery efforts aimed at the development of drugs targeting oncogenic RAS. |
| Target activity | PDEδ:38 nM(Kd) |
| molecular weight | 603.75 |
| Molecular formula | C40H37N5O |
| CAS | 1440898-61-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 93 mg/mL (154 mM) DMSO: 93 mg/mL (154 mM) |
| References | 1. Zimmermann G, et al. Nature. 2013, 497(7451), 638-642. |