名称 | Roniciclib |
描述 | Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol/L. |
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 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 249 mg/mL (578.47 mM)
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关键字 | CDK | Cyclin dependent kinase | BAY1000394 | BAY-1000394 | inhibit | Inhibitor | Roniciclib |
相关产品 | Ribociclib | Ro-3306 | GSK 3 Inhibitor IX | Rafoxanide | Palbociclib monohydrochloride | CASIN | Palbociclib | GW 441756 | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |