GSK3368715 (EPZ019997) 是具有口服活性的，可逆的，SAM 非竞争性 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂 (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8))。GSK3368715 (EPZ019997) 导致精氨酸甲基化状态的转变，改变了外显子的使用，具有很强的抗癌活性。
| 生物活性 |
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. |
|---|---|
| 体外研究 |
GSK3368715 (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types. |
| 体内研究 |
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.
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| 分子式 |
C20H41Cl3N4O2
|
| 分子量 |
366.54
|
| CAS号 |
1629013-22-4
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 临床试验 |
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| 科研文献 |
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