| Identification | Back Directory | [Name]
GSK3368715 dihydrochloride | [CAS]
1628925-77-8 | [Synonyms]
EPZ019997 dihydrochloride
GSK3368715 dihydrochloride
N-[3-(4,4-Bis-ethoxymethyl-cyclohexyl)-1H-pyrazol-4-ylmethyl]-N,N'-dimethyl-ethane-1,2-diamine dihydrochloride | [Molecular Formula]
C20H39ClN4O2 | [MDL Number]
MFCD32197254 | [MOL File]
1628925-77-8.mol | [Molecular Weight]
403.01 |
| Hazard Information | Back Directory | [Description]
GSK3368715 dihydrochloride is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor. | [Uses]
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1]. | [in vivo]
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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]. | [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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