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Abemaciclib

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Chemical Structure| 1231929-97-7 同义名 : -
CAS号 : 1231929-97-7
货号 : A106236
分子式 : C27H32F2N8
纯度 : 99%
分子量 : 506.593
MDL号 : MFCD22665744
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(3.95 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CDK4

    CDK4, IC50:2 nM

  • CDK6

    CDK6, IC50:10 nM
描述 Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, which also inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. Abemaciclib exhibits effectiveness against A375R1-4, M14R, and SH4R cells with EC50 values from 0.3 to 0.6 μM, and similarly inhibits the proliferation of both parental A375 and resistant variants A375RV1 and A375RV2 with IC50 values of 395, 260, and 463 nM, respectively[2]. Abemaciclib specifically targets CDK4 and CDK6 with low nanomolar potency, leading to G1 arrest and proliferation inhibition in Rb-proficient cells by preventing Rb phosphorylation[3].
作用机制 LY2835219 is a competitive ATP CDK4/6 inhibitor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL
参考文献

[1]Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13.

[2]Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 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 NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.