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• 产品描述： Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively

• 靶点： Cdk4/cyclin D1：2 nM (IC50)；CDK6/cyclinD1：10 nM (IC50)；CDK2/cyclinE：504 nM (IC50)；CDK9/cyclinT1：57 nM (IC50)；CDK1/cyclinB1：1627 nM (IC50)；CDK7/Mat1/cyclinH1：3910 nM (IC50)；Cdk5/p25：355 nM (IC50)；CDK5/p35：287 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);CDK

• 体内研究：
  Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (LY2835219) (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. 4. Wu T, et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.

• 溶解性： H2O  :  125  mg/mL  (207.40  mM;  Need  ultrasonic)    DMSO  :  10  mg/mL  (16.59  mM;  ultrasonic  and  warming  and  heat  to  80°C)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.659 ml	8.296 ml	16.592 ml
  5 mM	0.332 ml	1.659 ml	3.318 ml
  10 mM	0.166 ml	0.83 ml	1.659 ml
  50 mM	0.033 ml	0.166 ml	0.332 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 分子摩尔量 (g/mol)

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