• 产品描述： Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

• 靶点： Cdk4/cyclin D1:2 nM (IC50);CDK6/cyclinD1:10 nM (IC50);CDK9/cyclinT1:57 nM (IC50);CDK5/p35:287 nM (IC50);Cdk5/p25:355 nM (IC50);CDK2/cyclinE:504 nM (IC50);CDK7/Mat1/cyclinH1:3910 nM (IC50);CDK1/cyclinB1:1627 nM (IC50);PIM1:50 nM (IC50);PIM2:3400 nM (IC50);HIPK2:31 nM (IC50);DYRK2:61 nM (IC50);CK2:117 nM (IC50);GSK3b:192 nM (IC50);JNK3:389 nM (IC50);FLT3 (D835Y):403 nM (IC50);FLT3:3960 nM (IC50);DRAK1:659 nM (IC50)

• 体外研究： Abemaciclib 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. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib 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. Abemaciclib 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 cell

• 体内研究： Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.974 ml	9.87 ml	19.74 ml
  5 mM	0.395 ml	1.974 ml	3.948 ml
  10 mM	0.197 ml	0.987 ml	1.974 ml
  50 mM	0.039 ml	0.197 ml	0.395 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *