IMS2186

Names

[ Name ]:
IMS2186

[Synonym ]:
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

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Others

Signaling Pathways >> Others >> Others

[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]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₆O₄

[ Molecular Weight ]:
296.31700

[ Exact Mass ]:
296.10500

[ PSA ]:
55.76000

[ LogP ]:
3.36790

MSDS

Click to get detail MSDS

Safety Information

[ 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