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Abemaciclib

Abemaciclib

产品编号 T2381   CAS 1231929-97-7
别名: LY2835219, CDK4/6 dual inhibitor

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。

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Abemaciclib, CAS 1231929-97-7
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其他形式的 Abemaciclib:
产品目录号及名称: Abemaciclib (T2381)
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选择批次  
纯度: 99.87%
纯度: 99.46%
纯度: 99.43%
纯度: 99.39%
纯度: 99.39%
纯度: 99.39%
纯度: 99.39%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

T2381_2

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 10mg/mL(19.74mM)

Ethanol: 5.06mg/mL (10mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Ku B M , Yi S Y , Koh J , et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma[J]. Oncotarget, 2016, 7(12):14803-14813. 2. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. 3. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Oct;32(5):825-37.

文献引用

1. Ni J, Kabraji S, Xie S, et al. p16INK4A-deficiency predicts response to combined HER2 and CDK4/6 inhibition in HER2+ breast cancer brain metastases. Nature Communications. 2022, 13(1): 1-8. 2. Liu X, Hu Q, Wang W, et al. A protein-fragment complementation assay reveals that celastrol and gambogic acid suppress ERα mutants in breast cancer. Biochemical Pharmacology. 2021, 188: 114583. 3. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642. 4. Quan C, Wu Z, Xiong J, et al.Upregulated PARP1 confers breast cancer resistance to CDK4/6 inhibitors via YB-1 phosphorylation.Experimental Hematology & Oncology.2023, 12(1): 1-21.
SB1317 BS-181 Ganoderic acid DM CDK8-IN-4 Kobophenol A (R)-CR8 trihydrochloride PROTAC CDK9 Degrader-1 CDK4/6-IN-3

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 NO PAINS 化合物库 已知活性化合物库 抗衰老化合物库 抗乳腺癌化合物库 含氟化合物库 上市药物库 血液病分子库 细胞周期化合物库 激酶抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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,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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

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技术支持

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。

Keywords

Abemaciclib 1231929-97-7 Cell Cycle/Checkpoint CDK inhibit LY-2835219 LY 2835219 LY2835219 Inhibitor CDK4/6 dual inhibitor Cyclin dependent kinase inhibitor

 

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