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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-HH2853
HH2853

Chemical Structure : HH2853

CAS No.: 2202678-05-3

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HH2853 (HH-2853, (S)-HH2853)

货号: PC-24527Not For Human Use, Lab Use Only.

HH2853 is a novel potent dual EZH1/2 inhibitor that effectively inhibit the catalytic activity of wild-type EZH2 and mutated forms (A677G, Y641F, Y641N, and Y641C) with IC50 of 3.75, 2.21, 2.65, and 2.62 nM respectively, synchronously suppresses EZH1 activity with IC50 of 9.26 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HH2853 is a novel potent dual EZH1/2 inhibitor that effectively inhibit the catalytic activity of wild-type EZH2 and mutated forms (A677G, Y641F, Y641N, and Y641C) with IC50 of 3.75, 2.21, 2.65, and 2.62 nM respectively, synchronously suppresses EZH1 activity with IC50 of 9.26 nM.
HH2853 increases H3K27 acetylation in insensitive DLBCL cells.
HH2853 has the same or a slightly stronger inhibitory effect on cancer cells proliferation than EPZ-6438 against a panel of 24 cell lines expressing EZH2 mutations or wild type.
HH2853 exhibits superior anti-tumor efficacy in several tumor xenograft models compared with FDA-approved EZH2 selective inhibitor EPZ-6438 at a comparable dose level.
HH2853 also shows weak anti-tumor activity against EZH2 wild type (EZH2-WT) DLBCL cells in vitro and in vivo.

物理化学性质&存储条件

分子量 611.67
分子式 C31H36F3N7O3
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

(S)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-methyl-1-(6-methylpyridazin-3-yl)-5-(1-(4-(2,2,2-trifluoroethyl)piperazin-1-yl)ethyl)indolizine-7-carboxamide

参考文献

1. Yu L, et al. Acta Pharmacol Sin. 2023 Oct;44(10):2113-2124.

2. Chen XX, et al. Abstract 5436: HH2853 is a selective small molecular dual inhibitor of EZH1/2 with potent anti-tumor activities. Cancer Res. 2022;82:5436.

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