ZLD 1039 is a potent and selective EZH2 inhibitor (IC50 = 5.6 nM). Displays selectivity for EZH2 over a panel of HMTs (inhibition less than 30% at 16 μM). Blocks H3K27 methylation in breast cancer cell lines. Induces tumor regression and metastasis in breast cancer xenograft-bearing mice. Reactivates silenced tumor suppressors in vivo. Orally bioavailable.
- Nom chimique ou matériau
- 3-[Ethyl(tetrahydro-2H-pyran-4-yl)amino]-N-[(2,3,5,6,7,8-hexahydro-1-methyl-3-oxo-4-isoquinolinyl)methyl]-2-methyl-5-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]benzamide
- CAS
- 1826865-46-6
- Quantité
- 50 mg
- Formule moléculaire
- C36H48N6O3
- Pureté
- 98%
