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MS4078

    
≥98%

MS4078

源叶(MedMol)
S88604 一键复制产品信息
2229036-62-6
C45H52ClN9O8S
914.47
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S88604-5mg促销
≥98%

¥229.00 ¥206.00

3 - - - -
S88604-10mg促销
≥98%

¥366.00 ¥330.00

2 - - - -
S88604-25mg促销
≥98%

¥662.00 ¥596.00

3 - - - -
S88604-50mg促销
≥98%

¥742.00 ¥666.00

2 - - - -
S88604-100mg促销
≥98%

¥1480.00 ¥1330.00

1 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK
靶点: ALK;Cereblon;ALK; LigandforE3Ligase
体外研究: MS4078 effectively inhibits cancer cell proliferation. MS4078 (10-3, 10-2.5, 10-2, 10-1.5, 10-1, 10-0.5, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 33±1  nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4078(10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM; 3 days) MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 11±2 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of 59 ± 16 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels. Cell Viability Assay Cell Line: SU-DHL-1 and NCI-H2228 cells Concentration: 10-3, 10-2.5, 10-2,10-1.5, 10-1, 10-0.5, and 1 μM for SU-DHL-1  cells; 10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM for NCI-H2228 cells Incubation Time: 3 days Result: Inhibited proliferation of SU-DHL-1 cells (IC50=33 ± 1 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells. Western Blot Analysis Cell Line: SU-DHL-1 and NCI-H2228 cells Concentration: 1, 3, 10, 30, and 1
参考文献: 1. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.
溶解性: Soluble  in  DMSO
保存条件: -20°C
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.094 ml 5.468 ml 10.935 ml
5 mM 0.219 ml 1.094 ml 2.187 ml
10 mM 0.109 ml 0.547 ml 1.094 ml
50 mM 0.022 ml 0.109 ml 0.219 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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