INH154,1587705-63-2

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INH154

CAS No. : 1587705-63-2

MCE 国际站：INH154

产品活性：INH154 是 Nek2 和 Hec1 结合的高效抑制剂 (INH)，其在 Hela 和 MB468 细胞中的 IC₅₀ 值分别为 200 nM 和 120 nM。

研究领域：Others

作用靶点：Others

In Vitro: INH154 is highly potent in treating breast tumors with co-elevated expression of Hec1 and Nek2. INH154 is the most potent inhibitor of tumor cell growth. The IC₅₀ values of INH154 in HeLa and MDA-MB-468 cancer cells are 0.20 and 0.12 μM, respectively. INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells.

In Vivo: Tumor growth rates in mice treated with INH154 are evidently slower than those in control animals in a dose-dependent manner. In agreement with the tumor-growth data, the tumor proliferation index, determined by measuring BrdU staining, is clearly reduced in residual tumors treated with INH154 in comparison with vehicle alone. The expression levels of Nek2 and Hec1 S165 phosphorylation are also substantially reduced in INH154-treated tumors than in vehicle-treated tumors. On the other hand, mice body weights are measured during the 6.5 weeks treatment period and show little difference among treated and control groups. In addition, the toxicity of INHs by treating normal BALB/c ByJNarl mice with high dosage of INH154 (20 mg/kg) shows no significant difference of body weights, blood chemistry, and complete blood count (CBC) analysis among these groups of animals.

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