In vitro: The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.
In vivo: The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.
Cell Experiment | |
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Cell lines | Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells |
Preparation method | Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay. |
Concentrations | |
Incubation time | 96 h |
Animal Experiment | |
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Animal models | Female Balb/c mice |
Formulation | |
Dosages | 12.5, 25, 50 mg/kg |
Administration | 12.5, 25, 50 mg/kg |
Molecular Weight | 571.55 |
Formula | C31H24F3N5O3 |
CAS Number | 1532533-67-7 |
Solubility (25°C) | 50 mg/mL in 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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