LDN-211904

LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC[1][2].

Product Specifications

CAS Number

[1198408-39-7]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Ephrin Receptor

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ldn-211904.html

Smiles

O=C(C1=CN=C2C=CC(C3CCNCC3)=CN21)NC4=C(Cl)C=CC=C4

Molecular Formula

C19H19ClN4O

Molecular Weight

354.83

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501

References & Citations

[1]Qiao L, et al. Structure–activity relationship study of EphB3 receptor tyrosine kinase inhibitors[J]. Bioorganic & medicinal chemistry letters, 2009, 19 (21) : 6122-6126.|[2]Park SH, et al. Sonic hedgehog pathway activation is associated with cetuximab resistance and EPHB3 receptor induction in colorectal cancer. Theranostics. 2019 Apr 12;9 (8) :2235-2251.