品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S80203-5mg	99%	￥112.00元	9	-	-	-
源葉(MedMol)	S80203-10mg	99%	￥176.00元	10	-	-	-
源葉(MedMol)	S80203-25mg	99%	￥344.00元	8	-	-	-
源葉(MedMol)	S80203-50mg	99%	￥552.00元	5	-	-	-
源葉(MedMol)	S80203-100mg	99%	￥784.00元	4	-	-	-

產(chǎn)品介紹

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

產(chǎn)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

靶點： 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

體內(nèi)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.

參考文獻：
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)

保存條件： -20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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LY2835219 99%

2-Pyrimidinamine, N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimida