LDN-211904 (oxalate)

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

Product Specifications

CAS Number

[1198408-78-4]

UNSPSC

12352005

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-oxalate.html

Concentration

10mM

Purity

99.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H21ClN4O5

Molecular Weight

444.87

References & Citations

[1]Qiao L, et al. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Nov 1;19 (21) :6122-6.|[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.