LDN-214117

LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [1][2].

Product Specifications

CAS Number

[1627503-67-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LDN-214117.html

Purity

99.54

Solubility

DMSO : 20 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(C(C1=CC(OC)=C(OC)C(OC)=C1)=C2)=NC=C2C3=CC=C(N4CCNCC4)C=C3

Molecular Formula

C25H29N3O3

Molecular Weight

419.52

Precautions

H302, H315, H319, H335

References & Citations

[1]Agustin H Mohedas, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57 (19) :7900-15. |[2]Jelena Mihajlović, et al. Inhibition of bone morphogenetic protein signaling reduces viability, growth and migratory potential of non-small cell lung carcinoma cells. J Cancer Res Clin Oncol. 2019 Nov;145 (11) :2675-2687.|[3]Diana Carvalho, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019 May 9;2:156.