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Merck
CN

SML3539

MS177

≥98% (HPLC)

Synonym(s):

N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-(2-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4- yl)amino)ethoxy)propanamido)ethyl)piperazin-1-yl)pyridin-3-yl)-1-isopropyl-1H- indazole-4-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C48H55N11O8
CAS Number:
2225938-86-1
Molecular Weight:
914.02
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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SMILES string

O=C(NCC1=C(C=C(NC1=O)C)C)C2=CC(C3=CC=C(N=C3)N4CCN(CC4)CCNC(CCOCCNC5=CC=CC(C(N6C(C(N7)=O)CCC7=O)=O)=C5C6=O)=O)=CC8=C2C=NN8C(C)C

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Cell penetrant and potent PROTAC degrader of EZH2 that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes
MS177 is a cell penetrant and potent PROTAC degrader of EZH2 (enhancer of zeste homologue 2) that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 is fast-acting suppressor of cancer growth. MS177 comprises pomalidomide conjugated to a potent EZH2 inhibitor C24 via a short polyethylene glycol linker. It is much more effective and potent in suppressing cancer growth than catalytic inhibitors of EZH2.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000220804
0000220805
0000211506
0000220804
0000220805

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EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis
Nature Cell Biology, 24, 384-399 (2022)

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