Name | (3E)-3-(3-Hydroxy-4-methoxybenzylidene)-6-methyl-2,3-dihydro-4H-c hromen-4-one |
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Synonyms |
Azetidine,3-[1-(3,5-difluorophenyl)-2,2-dimethylpropylidene]
3-[1-(3-hydroxy-4-methoxyphenyl)meth-(E)-ylidene]-6-methylchroman-4-one 3-[1-(3-difluoromethoxy-benzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine-5-yl]-azetidine-1-carboxylic acid tert-butyl ester |
Description | IMS2186 is an antichoroidal neovascularization (CNV) reagent. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells[1]. |
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Related Catalog | |
In Vitro | IMS2186 (0.3-10 μM; 22 h) 抑制剂人成纤维细胞、人癌症细胞增殖,IC50 分别为 1.0-3.0 μM,0.3-3.0 μM[1]。 IMS2186 (0-10 μM; 22 h) 在 10 ng/mL VEGF 刺激下,抑制内皮管形成,IC50 为 0.1-0.3 μM[1]。 IMS2186 (0.1-10 μM; 24 h) 抑制巨噬细胞中促炎细胞因子 PGE2/TNF-a 的产生,IC50 为 0.3-1 μM[1]。 IMS2186 (0.1-10 μM; 1.5 h) 还抑制巨噬细胞迁移,IC50 为 1 μM[1]。 Cell Cycle Analysis[1] Cell Line: Cancer H460 cells Concentration: 3 μM, 10 μM Incubation Time: Result: Showed anti-proliferative activity mediated by arresting cell cycle at G2/M. |
In Vivo | IMS2186 (2.5 mg in 0.5 mL; 玻璃体注射; 单次剂量) 施用于兔子眼睛后,未出现眼毒性[1]。 IMS2186 (100 μg/眼,即 50 μg/μL 溶液用量 2.0 μL; 单次剂量) 对激光诱导脉络膜新生血管 (CNV) 的大鼠模型表现出抗增殖效力[1]。 Animal Model: Rat model of laser induced CNV[1] Dosage: 100 μg/eye, 2.0 μL of the solution of 50 μg/μL Administration: Intravitreal injection; single dose Result: Resulted 30% reduction of lesion area compared to PBS in the lesion area measurement. |
References |
Molecular Formula | C18H16O4 |
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Molecular Weight | 296.31700 |
Exact Mass | 296.10500 |
PSA | 55.76000 |
LogP | 3.36790 |