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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.
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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 |
[5] Agustin H Mohedas, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor
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| F-1
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
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