Volasertib trihydrochloride 产品活性：Volasertib (BI 6727) trihydrochloride 是一种具有口服活性的、高效的、ATP 竞争性的 Polo 样激酶 1 (PLK1) 抑制剂，IC50 为 0.87 nM。Volasertib trihydrochloride 抑制 PLK2 和 PLK3，IC50 分别为 5 和 56 nM。Volasertib trihydrochloride 诱导有丝分裂停滞和细胞凋亡。Volasertib trihydrochloride 是一种二氢蝶呤酮衍生物，在多种癌症模型中显示出显着的抗肿瘤活性。 产品来源： https://www.medchemexpress.cn/volasertib-trihydrochloride.html 研究领域：Cell Cycle/DNA Damage | Apoptosis 作用靶点：Polo-like Kinase (PLK) | Apoptosis In Vitro: Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC50 values of 11 to 37 nmol/L in multiple cell lines. Volasertib trihydrochloride (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase. Volasertib trihydrochloride (100 nM; 24-72 hours) induces cell apoptosis at 48 hours. In Vivo: Volasertib trihydrochloride (BI 6727 trihydrochloride; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models. Volasertib trihydrochloride (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models . Volasertib trihydrochloride (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells. Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice. Volasertib has high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h). 相关产品：MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Y-27632 | LY294002 | Paclitaxel | Z-VAD-FMK | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Deferoxamine mesylate | Oxaliplatin | Trametinib | Sorafenib | Temozolomide | Gemcitabine | Decitabine | Mdivi-1 | Rotenone | Etoposide | Elesclomol | Ruxolitinib | Monomethyl auristatin E | DAPT 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。