Fluzoparib (SHR3162) is an effective oral active PARP1 inhibitor (IC50=1.46±0.72 nM) with superior antitumor activity. Fluzoparib selectively inhibited the proliferation of homologous recombination repair (HR) deficient cells and sensitized HR deficient cells to cytotoxic drugs. Fluzoparib has good pharmacokinetic properties in vivo and can be used in cancer research.
Molecular Weight | 472.40 |
Formula | C22H16F4N6O2 |
CAS Number | 1358715-18-0 |
Solubility (25°C) | DMSO 35 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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