PK11000 is a sulfhydryl active anticancer compound that stabilizes wild-type and mutated p53 through selective alkylation of two surface cysteines without interfering with their DNA binding. In addition, PK11007 is independent of p53 and disrupts reactive oxygen species (ROS) detoxification in many mutated P53 cancer cells. PK11007 has shown anticancer activity in many cancer cell lines while pushing low cytotoxicity into normal cells.
| Molecular Weight | 236.63 |
| Formula | C6H5ClN2O4S |
| CAS Number | 38275-34-2 |
| Form | Solid |
| Solubility (25°C) | Water: 10 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.
[3] Michael J Duffy, et al. Mutant p53 as a target for cancer treatment
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