| Identification | Back Directory | [Name]
1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl- | [CAS]
1629013-22-4 | [Synonyms]
EPZ019997
GSK3368715
GSK3368715,GSK-3368715
N-[3-(4,4-Bis-ethoxymethyl-cyclohexyl)-1H-pyrazol-4-ylmethyl]-N,N'-dimethyl-ethane-1,2-diamine
N'-[[5-[4,4-Bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N,N'-dimethylethane-1,2-diamine
1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl- | [Molecular Formula]
C20H38N4O2 | [MDL Number]
MFCD32174310 | [MOL File]
1629013-22-4.mol | [Molecular Weight]
366.54 |
| Chemical Properties | Back Directory | [Boiling point ]
482.7±35.0 °C(Predicted) | [density ]
1.018±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
15.29±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1]. | [in vivo]
GSK3368715 (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively[1]. | [IC 50]
PRMT1; PRMT4; PRMT3; PRMT6; PRMT8 | [References]
[1] Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25. DOI:10.1016/j.ccell.2019.05.014 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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