LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. There are currently no effective therapies for fibrodysplasia ossificans progressiva (FOP), a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 shows a high degree of selectivity for ALK2 and low cytotoxicity that could provide a template for preclinical development.
MedKoo Cat#: 406619
Name: LDN-214117
CAS#: 1627503-67-6
Chemical Formula: C25H29N3O3
Exact Mass: 419.2209
Molecular Weight: 419.53
Elemental Analysis: C, 71.57; H, 6.97; N, 10.02; O, 11.44
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMF | 30.0 | 71.51 | ||
| DMF:PBS (pH 7.2) (1:1) | 0.5 | 1.19 | ||
| DMSO | 42.7 | 101.70 | ||
| Ethanol | 54.0 | 128.72 |
The following data is based on the product molecular weight 419.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
