ReACp53 is a cell-penetrating peptide inhibitor of p53 aggregation, inhibits p53 amyloid formation, rescues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC). ReACp53 penetrates into HGSOC primary cancer cells and converts mutant p53 from a punctate state into soluble WT-like p53. ReACp53 also induces cancer cell death, cell cycle arrest and results in p53 degradation.
Administration of ReACp53 results in a significant increase in p21 and MDM2 transcription in OVCAR3 but not MCF7 xenografts. A significantly increased population is also found in G0/G1 phase, supporting proliferative arrest upon ReACp53 administration in vivo.
| Molecular Weight | 2617.13 |
| Formula | C108H206N52O24 |
| Solubility (25°C) | DMSO 90 mg/mL Water 25 mg/mL |
| Storage | -20°C, 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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