GSK3368715 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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 dihydrochloride (EPZ019997 dihydrochloride) 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。

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.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types.

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.

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Others

Other Targets

Histone Methyltransferase

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1628925-77-8

439.46

C20H40Cl2N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 230 mg/mL (523.37 mM; 超声助溶 ) H2O 中的溶解度 : 140 mg/mL (318.57 mM; 超声助溶)

Cl.Cl.CCOCC1(COCC)CCC(CC1)c1n[nH]cc1CN(C)CCNC

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(-20℃)

With Ice Pack

≥ 2 years