化合物Roniciclib T16784

Product Introduction
Bioactivity


英文名: Roniciclib

描述: Roniciclib (BAY 1000394) 是一种有效的泛 CDK 抑制剂和新型口服细胞毒剂，对 CDK1、CDK2、CDK3、CDK4、CDK7 和 CDK9 的 IC50值为 5-25 nM。

体外活性: Roniciclib inhibits the kinase activity of the cell-cycle CDKs CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclinD (IC50: 7, 9, and 11 nM, respectively). Roniciclibeffectively inhibits the proliferation of various human and murine tumor cell lines with a very balanced profile (mean IC50 on human tumor cells: 16 nM). The transcriptional CDKs CDK9/cyclin T1 and CDK7/cyclin H/MAT1 are inhibited in a similar range (5 and 25 nM) [1][2].

体内活性: Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh-1kg-1, respectively). Roniciclib strongly inhibits the growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm2 before the start of treatment. Roniciclib (1.5 and 1 mg/kg) treatment slow tumor growth to T/C values of 0.15 and 0.62, respectively. The addition of Roniciclib to cisplatin causes a strong tumor growth inhibition with T/C values of 0.01 (1.0 mg/kg Roniciclib) and -0.02 (1.5 mg/kg Roniciclib) [1][2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 249 mg/mL (578.47 mM)


关键字: CDK | Cyclin dependent kinase | BAY1000394 | BAY-1000394 | inhibit | Inhibitor | Roniciclib

相关产品: BRD6989 | CDK8-IN-13 | CDK7-IN-22 | CDK2-IN-20 | Aloisine B | CAN508 | CDKI-73 | AT7519 | MSC2530818 | AZ1495

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