LDN-211904

Uses

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].

in vivo

References

[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. DOI:10.1016/j.bmcl.2009.09.010
[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. DOI:10.7150/thno.30678