产品描述
Voruciclib hydrochloride is an orally active and selective inhibitor of CDK (Ki: 0.626 nM-9.1 nM).
体外活性
In both ABC and GCB subtypes, Voruciclib hydrochloride (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 . 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.
体内活性
Combination of Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) and Voruciclib hydrochloride (200 mpk; Oral gavage) 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.
Cas No.
1000023-05-1
分子式
C22H20Cl2F3NO5
分子量
506.3
别名
Voruciclib hydrochloride
储存和溶解度
DMSO:250 mg/mL (493.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years