产品描述
GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
体外活性
GSK3368715 dihydrochloride ?shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.
体内活性
GSK3368715 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.
Cas No.
1628925-77-8
分子式
C20H40Cl2N4O2
分子量
439.46
别名
EPZ019997 dihydrochloride
储存和溶解度
DMSO:250 mg/mL (568.88 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years