| 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 |
|---|---|
| Molecular Weight | 296.31700 |
| Exact Mass | 296.10500 |
| PSA | 55.76000 |
| LogP | 3.36790 |
| Symbol |
GHS09 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H400 |
| Precautionary Statements | P273 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| RIDADR | UN 3077 9 / PGIII |