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LDN-211904

Names

[ CAS No. ]:
1198408-78-4

[ Name ]:
LDN-211904

[Synonym ]:
LDN211904
N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate

Biological Activity

[Description]:

LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Ephrin Receptor

[Target]

IC50: 0.079 µM (EphB3)[1]


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H21ClN4O5

[ Molecular Weight ]:
444.86800

[ Exact Mass ]:
444.12000

[ PSA ]:
133.03000

[ LogP ]:
3.26440

Related Compounds