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MS4078

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Chemical Structure| 2229036-62-6 同义名 : -
CAS号 : 2229036-62-6
货号 : A360284
分子式 : C45H52ClN9O8S
纯度 : 99%+
分子量 : 914.468
MDL号 : MFCD31812728
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(54.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MS4078 is a PROTAC targeting on ALK with DC50 value of 11nM, consist of ALK inhibitor ceritinib as a warhead linked to CRBN ligand Pomalidomide. Treatment with MS4078 led a degradation of both ALK fusion protein, including NPM-ALK of SU-DHL-1 cells and EML4-ALK of NCI-H2228 cells, as well as downregulation of ALK auto phosphorylation and down-steam STAT3 phosphorylation, in both cell lines in a dose-dependent manner at concentration ranging in 3-100nM for 16h and in a time-dependent manner at concentration of 30nM for SU-DHL-1 cells or 60nM for NCI-H2228 cells within 24h. MS4078 exhibited potent antiproliferation against SU-DHL-1 cells with IC50 value of 33nM post 3 days. MS4078 is available in mice through intraperitoneal administration with highest plasma concentration 3,000nM achieved at 2 h at dose of 50mg/kg. MS4748 and MS4740 work as the negative controls for MS4078[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.09mL

0.22mL

0.11mL

5.47mL

1.09mL

0.55mL

10.94mL

2.19mL

1.09mL
参考文献

[1]Zhang C, Han XR, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.