Tulmimetostat (CPI-0209) | EZH2 inhibitor

Chemical Structure : Tulmimetostat

CAS No.: 2567686-02-4

Tulmimetostat (CPI-0209, CPI 0209)

Catalog No.: 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.

Packing	Price	Stock
5 mg	$278	In stock
10 mg	$458	In stock
25 mg	$758	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	562.122
Formula	C28H36ClN3O5S
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	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

References

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

Tulmimetostat (CPI-0209, CPI 0209)

Biological Activity

Physicochemical Properties

References

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