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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 | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
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| GSK256066
GSK256066 is a selective phosphodiesterase 4 (PDE4)inhibitor with an IC50 of 3.2 pM. *The compound is unstable in solutions, freshly prepared is recommended |
| BAY-60-7550
BAY-60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). |
| Roflumilast
Roflumilast (APTA-2217; BYK 20869; B9302-107) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4). |
| Piclamilast
Piclamilast (RP 73401) is a potent and selective inhibitor of phosphodiesterase (PDE) 4. |
| Apremilast
Apremilast is a novel, orally available small molecule inhibitor of PDE4 with IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM. |
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