MS8815 | EZH2 PROTAC | Probechem Biochemicals

Chemical Structure : MS8815

CAS No.: 2855085-25-3

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MS8815 (MS 8815)

货号: 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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2 mg	￥2580	In stock
5 mg	￥3980	In stock
10 mg	￥5880	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	1154.526
分子式	C65H87N9O8S
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	(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

参考文献

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

MS8815 (MS 8815)

生物&药学活性

物理化学性质&存储条件

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MS8815 (MS 8815)

生物&药学活性

物理化学性质&存储条件

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