Volasertib伏拉塞替,755038-65-4

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Volasertib

CAS No. : 755038-65-4

MCE 国际站：Volasertib

产品活性：Volasertib (BI 6727) 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 抑制 PLK2 和 PLK3，IC₅₀ 分别为 5 和 56 nM。Volasertib 诱导有丝分裂停滞和细胞凋亡。Volasertib 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 (BI 6727; 0.01-10000 nM; 72 hours) has EC₅₀ values of 11 to 37 nmol/L in multiple cell lines.
?Volasertib (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.
?Volasertib (100 nM; 24-72 hours) induces cell apoptosis at 48 hours.

In Vivo: Volasertib (BI 6727; 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 (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 (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).

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