货号	规格	价格	上海	北京	珠海	重庆	武汉
S80938-2mg买3赠1	99.20%	￥216.00 S80938-2mg ￥216.00 现货（买3赠1）	4 4	-	-	-	-
S80938-5mg买3赠1	99.20%	￥260.00 S80938-5mg ￥260.00 现货（买3赠1）	3 3	-	-	-	-
S80938-10mg买3赠1	99.20%	￥290.00 S80938-10mg ￥290.00 现货（买3赠1）	4 4	-	-	-	-
S80938-25mg买3赠1	99.20%	￥550.00 S80938-25mg ￥550.00 现货（买3赠1）	4 4	-	-	-	-
S80938-50mg买3赠1	≥99%	￥980.00 S80938-50mg ￥980.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S80938-100mg	≥99%	￥1680.00 S80938-100mg ￥1680.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription

靶点：

PLK1:0.83 nM (IC50);Plk2/Snk:3.5 nM (IC50);Plk3/Fnk:9 nM (IC50);BRD4:25 nM (IC50);Apoptosis;EpigeneticReaderDomain;PLK

体内研究：

BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes

参考文献：

1. Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. 2. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9. 3. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. 4. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72.

溶解性：

DMSO : 65 mg/mL (124.60 mM; Need ultrasonic) 0.1 M HCL : 25 mg/mL (47.92 mM; ultrasonic and adjust pH to 4 with HCl)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.917 ml	9.585 ml	19.17 ml
5 mM	0.383 ml	1.917 ml	3.834 ml
10 mM	0.192 ml	0.958 ml	1.917 ml
50 mM	0.038 ml	0.192 ml	0.383 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。

参考文献

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