APR-246 (Eprenetapopt) is the first-in-class small molecule to restore wild-type p53 function in TP53 mutant cells.
APR-246 (Eprenetapopt), also known as PRIMA-1MET, is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. APR-246 (PRIMA-1MET) enhances apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. APR-246 treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that APR-246 can also act independently of the p53 status of the cell. APR-246 (Eprenetapopt) is the first small molecule to restore wild-type p53 function in TP53 mutant cells. APR-246 also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of REDOX balance in cells.
In animal studies, APR-246 (Eprenetapopt) is well tolerated, APR-246 single treatment inhibits tumor growth by 21% in mice bearing the aggressively growing A2780-CP20 tumor xenografts.
| Molecular Weight | 199.25 |
| Formula | C10H17NO3 |
| CAS Number | 5291-32-7 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL Water ≥ 40 mg/mL |
| 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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