GSK-3685032
目录号: PL03868 纯度: ≥99%
CAS No. :2170137-61-6
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中文名称
GSK-3685032
英文名称
GSK-3685032
英文别名
α-[[6-(4-Amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]benzeneacetamide;GSK3685032;GSK3685032 HCl;GTPL11750;BDBM491199;NSC837081;US10975056, Example 143;GSK-3685032
Cas No.
2170137-61-6
分子式
C22H24N6Os
分子量
420.53
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK-3685032 是一种非时间依赖、非共价、可逆的 DNMT1 选择性抑制剂,IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
生物活性
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
性状
Solid
IC50 & Target[1][2]
DNMT1
体外研究(In Vitro)
GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM.
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course.
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription.
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression.
GSK3685032 induces DNA hypomethylation and gene activation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models.

Summary of mouse pharmacokinetic parameters for GSK-3685032
Dose,Route C max
(ng/mL) AUC
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.
溶解度数据
In Vitro: DMSO : 25 mg/mL (59.45 mM; Need ultrasonic)配制储备液
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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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