WF-536 是一种 Rho 相关卷曲螺旋蛋白激酶(ROCK)抑制剂，具有口服活性。WF-536 具有肿瘤抗转移活性。WF-536 可用于癌症研究。
| 生物活性 | WF-536 is an orally active inhibitor ofRho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research ofcancer[1]. |
体外研究
(In Vitro) | WF-536（1、3、10、30、100 μM）抑制 LLC 细胞的侵袭和迁移以及内皮细胞在 Matrigel 上的侵袭、迁移和毛细管样管的形成，在这两种细胞类型下均无细胞毒性或抗增殖作用[1]。
Cell Migration Assay[1] | Cell Line: | LLC cells, Human umbilical vein endothelial cells | | Concentration: | 1, 3, 10, 30 μM | | Incubation Time: | 6 h (tumor cells), 4 h (endothelial cells) | | Result: | Significantly inhibited LLC-cell migration, with inhibitory rates of 23% and 44% at 10 and 30 μM, respectively. |
Cell Invasion Assay[1] | Cell Line: | LLC cells, Human umbilical vein endothelial cells | | Concentration: | 1, 3, 10, 30 μM | | Incubation Time: | 18 h | | Result: | Showed significant and concentration-dependent inhibition of LLC-cell invasion. |
Cell Proliferation Assay[1] | Cell Line: | LLC cells, Human umbilical vein endothelial cells | | Concentration: | 1, 30, 100 μM | | Incubation Time: | 24, 48, 72, and 96 h | | Result: | Showed no significant effect at 1-30 μM on the proliferation up to 96 h incubation, although the proliferation was decreased at 100 μM over 48 h. |
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体内研究
(In Vivo) | WF-536（口服；0.3-3 mg/kg/天；持续 28 天）抑制小鼠 Lewis 肺癌 (LLC) 转移和 LLC 诱导的血管生成[1]。
| Animal Model: | C57BL/6 mice (male, 6-week old)[1] | | Dosage: | 0.3, 1, 3 mg/kg | | Administration: | Oral; daily; for 28 days | | Result: | Significantly reduced the number of pulmonary metastatic colonies of LLC in a dose-dependent manner (0.3- 3 mg/kg). |
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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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