R1530 is a multi-kinase inhibitor with activity against several kinases associated with tumor growth and angiogenesis, including VEGFR, FGFR, PDGFR, Chk2 and Cdk2. In tumor cells, R1530 inhibits tubulin polyerization and mitotic checkpoint function, resulting in polyploidy. The compound R1530 inhibits tumor growth and angiogenesis in animal models.
| Molecular Weight | 356.78 |
| Formula | C18H14ClFN4O |
| CAS Number | 882531-87-5 |
| Solubility (25°C) | DMSO ≥ 30 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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