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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 |
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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. |
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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) |
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保存条件：
-20℃ |
配置溶液浓度参考：
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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 |
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| 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。 |
上海工商
北京