EPZ011969
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Grundinformationen
- CAS
1598383-40-4- Standard-SMILES
CCN(c1cc(C#CCN2CCOCC2)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)[C@H]1CC[C@H](N(C)CCOC)CC1- InChIKey
XQFINGFCBFHOPE-WXUXXXNLSA-N- Summenformel
- C35H51N5O4
- Durchschnittliche Molmasse
- 605,81 g/mol
Namen und Bezeichner
- Bevorzugter Name
- EPZ011969
- Englischer Name
- EPZ011969
- Summenformel
- C35H51N5O4
- Molmasse
- 605.81
Namen und Synonyme
EPZ011989CS-1609CS-2079EPZ011969EPZ011989EPZ-011989EPZ011989, 10 mM in DMSOEPZ011989,inhibit,Histone Methyltransferase,Inhibitor,EPZ 011989,EPZ-011989N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl((1r,4r)-4-((2-methoxyethyl)(methyl)amino)cyclohexyl)amino)-2-methyl-5-(3-morpholinoprop-1-ynyl)benzamideN-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-3-(ETHYL((TRANS)-4-((2-METHOXYETHYL)(METHYL)AMINO)CYCLOHEXYL)AMINO)-2-METHYL-5-(3-MORPHOLINOPROP-1-YN-1-YL)BENZAMIDEN-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]benzamide
Datenbank-Bezeichner
- CAS
1598383-40-4
Eigenschaften
Physikochemische Eigenschaften
- Siedepunkt
- 756.7 · 756.7±60.0 °C(Predicted)
- Dichte
- 1.17 · 1.17±0.1 g/cm3(Predicted)
- storage temp.
- -20 °C · Store at -20°C
- Löslichkeit
- 55 · DMSO:55.0(Max Conc. mg/mL);90.79(Max Conc. mM)DMF:10.0(Max Conc. mg/mL);16.51(Max Conc. mM)Ethanol:60.0(Max Conc. mg/mL);99.04(Max Conc. mM)Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.83(Max Conc. mM)
- Aggregatzustand
- A crystalline solid
- pka
- 11.88 · 11.88±0.10(Predicted)
- Farbe
- Light yellow to yellow
Chemie und Industrie
Anwendungen
BeschreibungThe lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells. EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2. It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
VerwendenN-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-benzamide is used in biological studies as inhibitors of EZH2 histone methyltransferase for the treatment of cancer.
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