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。

Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC 50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC 50 s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.

Solid

PLK1 0.87 nM (IC50) PLK2 5 nM (IC50

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.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

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

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Xie FF, et al. Volasertib suppresses tumor growth in cervical cancer. Am J Cancer Res. 2015 Nov 15;5(12):3548-59.
[2]. Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.Clin Cancer Res. 2009 May 1;15(9):3094-102. Epub

In Vitro: DMSO : 50 mg/mL (80.80 mM; Need ultrasonic)配制储备液