PLK1-IN-6

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PLK1-IN-6

CAS No. :

MCE 国际站：PLK1-IN-6

产品活性：PLK1-IN-6 是一种有效和选择性的 PLK1 抑制剂，IC₅₀ 值为 0.45 nM。PLK1-IN-6 对癌细胞显示出显着的抗增殖活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：Polo-like Kinase (PLK)  |  Epigenetic Reader Domain

In Vitro: PLK1-IN-6 (compound 21 g) shows significant anti-proliferative activities against four tumor-derived cell lines (MCF-7 IC₅₀=8.64 nM, HCT-116 IC₅₀=26.0 nM, MDA-MB-231 IC₅₀=14.8 nM and MV4-11 IC₅₀=47.4 nM).
PLK1-IN-6 shows moderate metabolism and the half-life in human liver microsome is 25.7 min.

In Vivo: PLK1-IN-6 (compound 21 g) (1 mg/kg; i.v.) exhibits a good half-life (10.1 h) and area under plasma concentration curves in Sprague Dawley rats.
PLK1-IN-6 (10 mg/kg; i.g.) exhibits low clearance values and high plasma exposure (26800 ng•h/mL), with favorable bioavailability (11.4%) in Sprague Dawley rats.
PLK1-IN-6 (10 mg/kg; i.g.) exhibits long half-life (2.73 h), high plasma exposure (11227 ng•h/mL) and excellent bioavailability (77.4%) in Balb/c mice.
PLK1-IN-6 (20 mg/kg; i.g.) shows no apparent toxicity in mice.

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