Voruciclib  98%

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沸点:587.6±50.0 °C(Predicted)
密度:1.493±0.06 g/cm3(Predicted)
包装规格:1mg 5mg 10mg 25mg in glass bottle
产品简介:一种具有口服活性和选择性 CDK 抑制剂,Ki 为 0.626 nM-9.1 nM。Voruciclib 可以有效阻断MCL-1的转录调节子CDK9。Voruciclib 抑制多种弥漫性大B细胞淋巴瘤 (DLBCL)模型中MCL-1的表达。
溶解性:可溶性二甲基亚砜
储备液保存:-80°C, 2 years -20°C, 1 year
靶点:CDK9/cyc T2:0.626nM (Ki) CDK9/CycT1:1.68nM (Ki) CDK6/cycD1:2.92nM (Ki) CDK4/Cyc D1:3.96nM (Ki) CDK1/cycB:5.4nM (Ki) CDK1/cyc A:9.1nM (Ki)
体外研究:Voruciclib (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes. Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively.
体内研究:Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL.
保存条件:-20°C 密封干燥
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。