LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
 |
Source | Oncotarget (2017). Figure 2. LDN-212854 |
| Method | i.p. | |
| Cell Lines | C57BL/6J mice | |
| Concentrations | 6 mg/kg | |
| Incubation Time | - | |
| Results | "CNV size in eyes from metformin treated group was significantly smaller than the PBS treated controls and vascular density in the CNV lesion was also less (p<0.05). In another set of experiment, animals were treated by intraperitoneal injection of PBS or LDN-212854 (6 mg/kg, twice daily), an ALK1/2 specific inhibitor. LDN-212854 also significantly inhibited laser-induced CNV and vascular density" |
| Molecular Weight | 406.48 |
| Formula | C25H22N6 |
| CAS Number | 1432597-26-6 |
| 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.
[5] Agustin H Mohedas, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor
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