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MS1943

Chemical Structure : MS1943

CAS No.: 2225938-17-8

MS1943 (MS-1943)

Catalog No.: PC-38300Not For Human Use, Lab Use Only.

MS1943 (MS-1943) is a first-in-class, orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells, inhibits EZH2 methyltransferase activity with IC50 of 120 nM.

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Biological Activity

MS1943 (MS-1943) is a first-in-class, orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells, inhibits EZH2 methyltransferase activity with IC50 of 120 nM.
MS1943 is highly selective for EZH2 over a wide range of methyltransferases including EZH1, as well as 45 kinases.
MS1943 inhibited TNBC cells that express EZH2 (HCC1187, HCC70, BT549 and HCC1954, GI50s=1.1-4.9 uM), but not EZH2 inhibitors (GSK126, CPI-1205, EPZ6438 and C24).
MS1943 reduces EZH2 levels in cancer cells, suppresses tumor growth in vivo.

Physicochemical Properties

M.Wt 718.95
Formula C42H54N8O3
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

100 mM in DMSO

Chemical Name/SMILES

6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide

References

1. Anqi Ma, et al. Nat Chem Biol. 2020 Feb;16(2):214-222.

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