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Abemaciclib methanesulfonate

Abemaciclib methanesulfonate (LY2835219) 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。

CAS号

1231930-82-7

分子式

C27H32F2N8·CH4O3S

主要靶点

CDK

仅限科研使用

Cat No : CM03384

Print datasheet

Synonyms

LY2835219|abemaciclib mesylate|LY2835219 mesylate|LY2835219 (methanesulfonate)

验证数据展示

  • CAS No.: 1231930-82-7

    Abemaciclib methanesulfonate
    CAS#: 1231930-82-7

产品信息

LY2835219 is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

CAS号 1231930-82-7
分子式 C27H32F2N8·CH4O3S
主要靶点 CDK
主要通路 细胞周期
分子量 602.7
纯度 98.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LY2835219|abemaciclib mesylate|LY2835219 mesylate|LY2835219 (methanesulfonate)

靶点活性

CDK4:2 nM|CDK6:10 nM

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。

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.

溶解度

Ethanol:23 mg/mL (38.2 mM),DMSO:77 mg/mL (127.8 mM),H2O:45mg/mL (74.7mM)

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.

参考文献

1.Sanchez-Martinez et al. Mol Cancer Ther, 2011,10(11 Suppl), Abstract nr B234.
2.Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

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