GSK3368715 dihydrochloride|1628925-77-8|(EPZ019997 dihydrochloride)-陌孚医药/Medlife

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GSK3368715 dihydrochloride (Synonyms: EPZ019997 dihydrochloride)

目录号: PL15069 纯度: ≥99%

CAS No. :1628925-77-8

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中文名称	GSK3368715 dihydrochloride
英文名称	GSK3368715 dihydrochloride
英文别名	GSK3368715 (dihydrochloride);EPZ019997;EPZ019997 dihydrochloride;GSK3368715 dihydrochloride;N-[3-(4,4-Bis-ethoxymethyl-cyclohexyl)-1H-pyrazol-4-ylmethyl]-N,N'-dimethyl-ethane-1,2-diamine dihydrochloride
Cas No.	1628925-77-8
分子式	C₂₀H₄₀Cl₂N₄O₂
分子量	439.46
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

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。

生物活性

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (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.

性状

Solid

IC50 & Target[1][2]

IC50: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)
Ki: 1.5 nM (PRMT1), 81 nM (PRMT3), 19 nM (PRMT4), 2.4 nM (PRMT6), 2 nM (PRMT8)

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.

溶解度数据	In Vitro: DMSO : 230 mg/mL (523.37 mM; Need ultrasonic)H₂O : 140 mg/mL (318.57 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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