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| | LDN-211904 Basic information |
| Product Name: | LDN-211904 | | Synonyms: | LDN-211904;N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide;N-(2-Chlorophenyl)-6-(4-piperidinyl)-imidazo[1,2-a]pyridine-3-carboxamide;CS-892;Imidazo[1,2-a]pyridine-3-carboxamide, N-(2-chlorophenyl)-6-(4-piperidinyl)- | | CAS: | 1198408-39-7 | | MF: | C19H19ClN4O | | MW: | 354.83 | | EINECS: | | | Product Categories: | | | Mol File: | 1198408-39-7.mol |  |
| | LDN-211904 Chemical Properties |
| | LDN-211904 Usage And Synthesis |
| 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 |
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