MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Volasertib trihydrochloride

CAS No. : 946161-17-7

MCE 站：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。

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 (V_ss=7.6 L/kg, t_1/2=46 h) ａnd rats (V_ss=22 L/kg, t_1/2=54 h).

相关产品：MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  Sorafenib  |  Staurosporine  |  5-Fluorouracil  |  Bortezomib  |  Trametinib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  MK-2206 dihydrochloride  |  Temozolomide  |  Verteporfin  |  Actinomycin D  |  Decitabine  |  Etoposide  |  BAY 11-7082  |  Pexidartinib  |  Mitomycin C  |  CCCP  |  DAPT  |  Ruxolitinib

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。