| 名称 | BAY-1816032 |
| 描述 | BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM. |
| 体外活性 | METHODS: BAY-1816032 (0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM, 48 hours) treated ATC cells (TPC-1, 8505C), and CCK-8 assay was used to study cell viability.
RESULTS BAY-1816032 treatment resulted in a decrease in ATC cell viability, with IC50 values of 4.230 μM in TPC-1 cells and 6.216 μM in 8505C cells. [2]
METHODS: Colony formation assay, cell cycle, invasion, migration and wound healing assay were performed after ATC cells were treated with BAY-1816032 (0, 2.5, 5 μM).
RESULTS BAY-1816032 can significantly reduce colony formation ability; BAY-1816032 can cause cell cycle arrest similar to siRNA; BAY-1816032 treatment can significantly hinder the invasion and migration of ATC cells in a dose-dependent manner. [2] |
| 体内活性 | METHODS: BAY-1816032 (100 mg/kg, oral, 24 days) was used to treat 8505C xenograft model mice to evaluate the anti-ATC activity and safety of BAY-1816032 in mice.
RESULTS There was no significant difference in the body weight of each group of mice; the tumor weight of mice treated with BAY-1816032 was significantly reduced. [2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 0.1 mg/mL (insoluble)
DMSO : 15 mg/mL (28.06 mM), Sonication and heating are recommended.
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| 关键字 | inhibit | Inhibitor | BAY 1816032 | BAY1816032 | BAY-1816032 |
| 相关库 | 经典已知活性库 | 激酶抑制剂库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 |
United States
