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Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Deltarasin selectively binds to the prenyl-binding pocket of PDEδ with nanomolar affinity (IC50 = 41 nM, binding to PDEδ in cell). Deltarasin was tested as an inhibitor in mice that had previously received injections of human tumor cells with KRAS mutations. Deltarasin was effective as an inhibitor in sharply reducing tumor growth in comparison to a placebo.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Mice bearing Panc-Tu-I xenografts |
| Formulation | Lipovenoes 10% PLR and 5% DMSO |
| Dosages | 10 mg/kg bid |
| Administration | i.p. |
| Molecular Weight | 603.75 |
| Formula | C40H37N5O |
| CAS Number | 1440898-61-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDE Products |
|---|
| MR-L2
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. |
| MMPX
MMPX is a potent PDE1 inhibitor. |
| T-0156
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. |
| TPN171
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH). |
| Mesopram
Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. |
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