CP-31398 dihydrochloride is a novel p53-stabilizing agent, stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53. CP-31398 (36.75 μM, 16 h) induces p21 in p53-mutant cells. CP-31398 (15 μg/mL, 20 hours) could induce apoptosis and cell cycle arrest in SW480 cells.
In vivo, CP-31398 (100 mg/kg, orally) exhibits significant anti-tumor activity in mice models.
| Molecular Weight | 435.39 |
| Formula | C22H28Cl2N4O |
| CAS Number | 1217195-61-3 |
| Solubility (25°C) | Water ≥ 90 mg/mL DMSO 5 mg/mL (ultrasonic and warming) |
| Storage | 4°C, protect from light, dry, sealed |
| 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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