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MS4322

Chemical Structure : MS4322

CAS No.: 2375432-47-4

MS4322 (MS-4322)

Catalog No.: PC-72471Not For Human Use, Lab Use Only.

MS4322 (MS-4322) is a potent, highly selective PRMT5 degrader (PROTAC) by linking the PRMT5 inhibitor EPZ015666 to a von Hippel-Lindau (VHL) E3 ligase ligand, with PRMT5 protein DC50 of 1.1 uM in MCF-7 cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MS4322 (MS-4322) is a potent, highly selective PRMT5 degrader (PROTAC) by linking the PRMT5 inhibitor EPZ015666 to a von Hippel-Lindau (VHL) E3 ligase ligand, with PRMT5 protein DC50 of 1.1 uM in MCF-7 cells.
MS4322 effectively reduced PRMT5 protein levels in multiple cell lines, reduced the PRMT5 protein level in MCF7 cells in a concentration-, time-, VHL- and proteasome-dependent manner.
MS4322 inhibited cell growth at least as effectively as EPZ015666 in multiple cancer cell lines and exhibited good plasma exposure in a mouse pharmacokinetic (PK) study.

Physicochemical Properties

M.Wt 1101.32
Formula C55H76N10O12S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-((S)-19-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidine-1-carbonyl)-20,20-dimethyl-17-oxo-3,6,9,12,15-pentaoxa-18-azahenicosanoyl)azetidin-3-yl)amino)pyrimidine-4-carboxamide

References

1. Yudao Shen, et al. J Med Chem. 2020 Sep 10;63(17):9977-9989.

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