UC2288 is a novel p21 attenuator with cellular permeability and oral activity (relatively selective activity for P21), based on the structural synthesis of sorafenib. UC2288 down-regulated the expression of P21 mRNA and reduced the level of P21 protein independently of p53, and had little effect on the stability of P21 protein. UC2288 did not inhibit VEGFR2 and Raf kinases, even at 10 μM.
| Molecular Weight | 481.82 |
| Formula | C20H18ClF6N3O2 |
| CAS Number | 1394011-91-6 |
| Solubility (25°C) | DMSO 48 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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