货号	规格	价格	上海	北京	珠海	重庆	武汉
S88604-5mg促销	≥98%	￥229.00 ￥206.00 S88604-5mg ￥206.00 现货	3 3	-	-	-	-
S88604-10mg促销	≥98%	￥366.00 ￥330.00 S88604-10mg ￥330.00 现货	2 2	-	-	-	-
S88604-25mg促销	≥98%	￥662.00 ￥596.00 S88604-25mg ￥596.00 现货	3 3	-	-	-	-
S88604-50mg促销	≥98%	￥742.00 ￥666.00 S88604-50mg ￥666.00 现货	2 0 2	-	-	-	-
S88604-100mg促销	≥98%	￥1480.00 ￥1330.00 S88604-100mg ￥1330.00 现货	1 1	-	-	-	-

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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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