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GSK3368715 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.
GSK3368715 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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 19,400 | 10-14周 | |
50 mg | ¥ 25,800 | 10-14周 | |
100 mg | ¥ 33,500 | 10-14周 |
产品描述 | GSK3368715 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. |
靶点活性 | PRMT8:1.7 nM , PRMT6:5.7 nM , PRMT1:3.1 nM , PRMT4:1148 nM , PRMT3:48 nM |
体外活性 | GSK3368715 ?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 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. |
别名 | EPZ019997 |
分子量 | 366.54 |
分子式 | C20H38N4O2 |
CAS No. | 1629013-22-4 |
密度 | 1.018 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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