| Bioactivity | 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]. | |||||||||
| Invitro | 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: | |||||||||
| 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: | |||||||||
| Name | IMS2186 | |||||||||
| CAS | 1031206-36-6 | |||||||||
| Formula | C18H16O4 | |||||||||
| Molar Mass | 296.32 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Falkenstein IA, et al. Toxicity and intraocular properties of a novel long-acting anti-proliferative and anti-angiogenic compound IMS2186. Curr Eye Res. 2008 Jul;33(7):599-609. |