DCZ19931 是一种有效的多靶向激酶抑制剂。DCZ19931 对眼部新生血管有抗血管生成作用。DCZ19931 还抑制 ERK1/2-MAPK 和 p38-MAPK 信号。
| 生物活性 | DCZ19931 is a potent multi-targeting kinase inhibitor. DCZ19931 has anti-angiogenic effects on ocular neovascularization. DCZ19931 also inhibits ERK1/2-MAPK and p38-MAPK signaling[1]. |
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体外研究
(In Vitro) | DCZ19931 (1 nM-10 μM; 24 h) 对人脐静脉内皮细胞 (HUVECs) 无明显的细胞毒性[1]。
DCZ19931 (500 nM; 24 h) 抑制 (10 ng/mL; 12 h) VEGFs 诱导的内皮细胞增殖、迁移和成管能力[1]。
DCZ19931 (500 nM; 24 h) 通过下调 ICAM-1，表达抑制血管通透性[1]。
DCZ19931 (500 nM; 24 h) 降低 HUVECs 中 p-ERK1/2、p-p38 和 p-JNK 的表达水平[1]。
DCZ19931 在小鼠脉络膜发芽试验中也显示出抗血管生成作用[1]。
Western Blot Analysis[1] | Cell Line: | Human umbilical vein endothelial cells (HUVECs) | | Concentration: | 500 nM; with or without 50 ng/mL VEGF for 30 min | | Incubation Time: | 24 hours | | Result: | Decreased expression of phosphorylated ERK and phosphorylated p38. |
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体内研究
(In Vivo) | DCZ19931 (1 μL, 1 μg/μL; 静脉注射; 单剂量) 抑制小鼠氧诱导视网膜病变 (OIR) 模型眼新生血管生成[1].
DCZ19931 (2 μL, 1 μg/μL; 静脉注射; 7 d) 无组织毒性，并抑制激光诱导脉络膜新生血管 (CNV) 模型小鼠的眼部新生血管生成[1]。
| Animal Model: | Laser-induced choroidal neovascularization (CNV) model in mice[1] | | Dosage: | 2 μL, 1 μg/μL | | Administration: | Intravitreal injection; single dose, monitored for 7 d following laser photocoagulation | | Result: | Did not cause marked histopathological changes in retinal structures.
Decreased the areas of CNV lesions, showed anti-angiogenic effect in vivo. |
| Animal Model: | Oxygen-induced retinopathy (OIR) model in mice[1] | | Dosage: | 1 μL, 1 μg/μL | | Administration: | Intravitreal injection; single dose | | Result: | Further showed anti-angiogenic effect in vivo, inhibited ocular neovascularization. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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