ZLD1039| cas 1826865-46-6

Cas No.:	1826865-46-6
Chemical Name:	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
Synonyms:	ZLD1039;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;ZLD 1039;J3.544.027E;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
SMILES:	O1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N(C([H])([H])C([H])([H])[H])C1=C([H])C(C2=C([H])N=C(C([H])=C2[H])N2C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C2([H])[H])=C([H])C(C(N([H])C([H])([H])C2C(N([H])C(C([H])([H])[H])=C3C([H])([H])C([H])([H])C([H])([H])C([H])([H])C3=2)=O)=O)=C1C([H])([H])[H]
Formula:	C₃₆H₄₈N₆O₃
M.Wt:	612.8047
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

ZLD1039 is an inhibitor of enhancer of zeste homolog 2 (EZH2; IC50 = 5.6 nM).It is selective for EZH2 over EZH1 (IC50 = 81 nM) and is greater than 4,700-fold selective for EZH2 in a panel of 14 histone methyltransferases. ZLD1039 also inhibits mutant Y641F and A677G EZH2 (IC50s = 15 and 4 nM, respectively, in a cell-free enzyme assay). It inhibits methylation of histone 3 lysine 27 (H3K27) in MCF-7 breast cancer cells (IC50 = 0.29 µM) and decreases expression of cadherin-1 (CDH1), cyclin-dependent kinase inhibitor 1C (CDKN1C), CDKN2A, and runt-related transcription factor 3 (RUNX3) in MCF-7 cells when used at concentrations of 1 and 2 µM. It also suppresses migration of MCF-7 cells when used at a concentration of 2 µM. ZLD1039 (200 mg/kg) reduces tumor growth in MCF-7 and MDA-MB-231 mouse xenograft models and inhibits tumor metastasis and decreases tumor protein levels of matrix metalloproteinase-2 (MMP-2), MMP-9, and E-cadherin in a 4T1 mouse xenograft model when administered at a dose of 250 mg/kg.

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