Abemaciclib methanesulfonate 是一种选择性的CDK4/6抑制剂,能够抑制 CDK4/CDK6 的活性,IC50分别为 2 nM 和 10 nM。
产品描述
LY2835219 is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
体外活性
MsOH处理皮下和颅内胶质瘤模型(U87 mg)中,LY2835219以剂量依赖的方式抑制肿瘤生长.
体内活性
在视网膜母细胞瘤中,LY2835219通过特异性抑制CDK4和6,使细胞周期停滞在G1期,抑制DNA合成,且抑制癌细胞生长。
激酶实验
Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.
细胞实验
LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of< 1 is synergistic and a CI of >1 is antagonistic.
Cas No.
1231930-82-7
分子式
C28H36F2N8O3S
分子量
602.71
别名
LY2835219 (methanesulfonate);LY2835219;LY2835219 mesylate;abemaciclib mesylate;Abemaciclib methanesulfonate
储存和溶解度
DMSO:77 mg/mL (127.8 mM)
Ethanol:23 mg/mL (38.2 mM)
H2O:45mg/mL (74.7mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years