Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Abemaciclib 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 an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM). |
靶点活性 | CDK4:2 nM, CDK6:10 nM |
体外活性 | LY2835219 reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; LY2835219 inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3]. |
体内活性 | LY2835219 (45 mg/kg, p.o.) in combination with everolimus causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. LY2835219 (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2]. |
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 | LY2835219, CDK4/6 dual inhibitor |
化合物与蛋白结合的复合物 |
Crystal structure of the human HIPK3 kinase domain bound to abemaciclib |
分子量 | 506.59 |
分子式 | C27H32F2N8 |
CAS No. | 1231929-97-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 10mg/mL(19.74mM)
Ethanol: 5.06mg/mL (10mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
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,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
bottom
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Abemaciclib 1231929-97-7 Cell Cycle/Checkpoint CDK inhibit LY-2835219 LY 2835219 LY2835219 Inhibitor CDK4/6 dual inhibitor Cyclin dependent kinase inhibitor