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

Chemical Structure : Tulmimetostat

CAS No.: 2567686-02-4

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Tulmimetostat (CPI-0209, CPI 0209)

货号: PC-73451Not For Human Use, Lab Use Only.

Tulmimetostat (CPI-0209) is a potent, selective, orally available EZH2 inhibitor with Ki of 140 fM by kinetic analyses and Ki 180 fM by thermal shift assays.

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5 mg ￥2780 In stock
10 mg ￥4580 In stock
25 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tulmimetostat (CPI-0209) is a potent, selective, orally available EZH2 inhibitor with Ki of 140 fM by kinetic analyses and Ki 180 fM by thermal shift assays.
Tulmimetostat (CPI-0209) only inhibits EZH2 and the closely related EZH1 enzyme against a panel of over 30 protein and DNA methyltransferases at 10 uM.
Tulmimetostat (CPI-0209) potently inhibits global H3K27me3 levels in cell-based assays with IC50 of 0.38 nM, >50-fold more potent than Tazemetostat.
Tulmimetostat (CPI-0209) potently inhibits KARPAS-422 cell proliferation in a dose-dependent manner (IC50=6 nM), >50-fold more potent than Tazemetostat.
Tulmimetostat (CPI-0209) exhibits a profound reduction in global H3K27me3 levels in tumors and growth inhibitory effect in KARPAS-422 mouse xenograft model.

物理化学性质&存储条件

分子量 562.122
分子式 C28H36ClN3O5S
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

(2R)-7-cloro-2,4-dimetil-N-{[6-metil-4-(metilsulfanil)-2- oxo-1,2-dihidropiridin-3-il]metil}-2-[trans-4-(3- metoxiazetidin-1-il)ciclohexil]-2H-1,3-benzodioxol-5- carboxamida

参考文献

1. Patent WO2021016409 A1.
2. Keller PJ, et al. Cancer Res. 2024 Jun 4. doi: 10.1158/0008-5472.CAN-24-0398.

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