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首页-抗体药物偶连体和PROTACs-PROTAC-MS115
MS115

Chemical Structure : MS115

CAS No.:

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MS115

货号: PC-24376Not For Human Use, Lab Use Only.

MS115 is a potent, selective best-in-class PRMT5 PROTAC degrader, induces rapid and robust degradation of PRMT5 (DC50=17.4 nM) and its binding partner MEP50 (DC50=11.3 nM, MDAMB468 cells), in a time-, concentration-, VHL- and UPS-dependent manner.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MS115 is a potent, selective best-in-class PRMT5 PROTAC degrader, induces rapid and robust degradation of PRMT5 (DC50=17.4 nM) and its binding partner MEP50 (DC50=11.3 nM, MDAMB468 cells), in a time-, concentration-, VHL- and UPS-dependent manner.
MS115 achieves greater than 85% degradation of both PRMT5 and MEP50.
MS115 is significantly more potent in degrading the PRMT5/MEP50 complex than the cereblon-recruiting YZ-836P and MS4322.
MS115 is a highly selective PRMT5/MEP50 complex degrader.
MS115 effectively inhibits the proliferation and clonogenicity of breast cancer cells, potently degrades PRMT5 and MEP50, reduces downstream sDMA, and inhibits proliferation of PC-3 prostate cancer cells.

物理化学性质&存储条件

分子量 1258.52
分子式 C63H88FN11O13S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((S)-3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-((S)-1-((2S,4R)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidin-2-yl)-3-(4-(4-methylthiazol-5-yl)phenyl)-1,5-dioxo-9,12,15,18,21-pentaoxa-2,6-diazatetracosan-24-oyl)piperidin-4-yl)amino)pyrimidine-4-carboxamide

参考文献

1. Zhong Y, et al. J Med Chem. 2025 Apr 15. doi: 10.1021/acs.jmedchem.5c00198.

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