GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor ( IC 50 =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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8), Ki app : 1.5 nM (PRMT1), 81 nM (PRMT3), 19 nM (PRMT4), 2.4 nM (PRMT6), 2 nM (PRMT8)
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GSK3368715 dihydrochloride
Dangerous GoodsCAS number：1628925-77-8 molecular formula：C20H38N4O2·2[HCl]
overview
compound introduction
Specs
| Chinese alias | GSK3368715 二盐酸盐 | ||
| English alias | - | ||
| CAS number | 1628925-77-8 | molecular formula | C20H38N4O2·2[HCl] |
| molecular weight | 439.46 g/mol | Exact mass | ≥99% |
| PSA | 62.400 Ų | logp | - |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。
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