LDN-211904
- Product Name
- LDN-211904
- CAS No.
- 1198408-39-7
- Chemical Name
- LDN-211904
- Synonyms
- CS-892;LDN-211904;N-(2-Chlorophenyl)-6-(4-piperidinyl)-imidazo[1,2-a]pyridine-3-carboxamide;N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide;Imidazo[1,2-a]pyridine-3-carboxamide, N-(2-chlorophenyl)-6-(4-piperidinyl)-
- CBNumber
- CB03033146
- Molecular Formula
- C19H19ClN4O
- Formula Weight
- 354.83
- MOL File
- 1198408-39-7.mol
LDN-211904 Chemical Properties,Usage,Production
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
LDN-211904 (0.1 mg/kg; i.p.; three times a week; for 21 days) inhibits and overcomes Cetuximab (HY-P9905) resistance in vivo[2].
| Animal Model: | Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells[2] |
| Dosage: | 0.1 mg/kg |
| Administration: | i.p.; three times a week; for 21 days |
| Result: | Inhibited tumor growth. |
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
LDN-211904 Preparation Products And Raw materials
Raw materials
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