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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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