产品描述	Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
靶点活性	CDK4:2 nM, CDK6:10 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.
别名	abemaciclib mesylate, LY2835219, LY2835219 mesylate, LY2835219 (methanesulfonate)

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

H2O: 45 mg/mL (74.7 mM)

DMSO: 6.03 mg/mL (10 mM), Sonication is recommended.

Ethanol: 23 mg/mL (38.2 mM)

溶液配制表

DMSO/Ethanol/H2O

Ethanol/H2O

	1mg	5mg	10mg	50mg
20 mM	0.0830 mL	0.4148 mL	0.8296 mL	4.1480 mL

H2O

	1mg	5mg	10mg	50mg
50 mM	0.0332 mL	0.1659 mL	0.3318 mL	1.6592 mL

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是 10 mg/kg ，每只动物体重 20 g ，给药体积 100 μL ， TargetMol | Animal experiments

一共给药动物 10 只 ，您使用的配方为 5% TargetMol | reagent

DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL 。

母液配置方法: 2 mg 药物溶于 50 μLDMSO TargetMol | reagent

（母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法: 取 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween 80, 混匀澄清，再加 600μLddH2O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多