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MS8815

Chemical Structure : MS8815

CAS No.: 2855085-25-3

MS8815 (MS 8815)

Catalog No.: PC-49077Not For Human Use, Lab Use Only.

MS8815 is a potent, selective EZH2 PROTAC degrader with IC50 of 8.6 nM against EZH2, induces robust EZH2 degradation in a concentration-, time-, and proteasome-dependent manner in TNBC cells.

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

Biological Activity

MS8815 is a potent, selective EZH2 PROTAC degrader with IC50 of 8.6 nM against EZH2, induces robust EZH2 degradation in a concentration-, time-, and proteasome-dependent manner in TNBC cells.
MS8815 effectively suppressed the cell growth in multiple TNBC cell lines (BT549 cell, GI50=2.0 uM) and primary patient TNBC cells (Patient 515a cells, GI50=1.4 uM).
MS8815 displays superior growth inhibition and EZH2 degradation to MS177 in BT549 cells.
The EZH2 degradation induced by MS8815 is rescued by the NEDD8 activating E1 enzyme (NAE) inhibitor MLN4924.

Physicochemical Properties

M.Wt 1154.526
Formula C65H87N9O8S
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

(2S,4R)-1-((S)-2-(9-(4-((3'-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-5'-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-methyl-[1,1'-biphenyl]-4-yl)methyl)piperazin-1-yl)-9-oxononanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

References

1. Brandon Dale, et al. ACS Pharmacol. Transl. Sci. 2022, 5, 7, 491-507.

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