NCT-505
目录号: PL02029 纯度: ≥98%
CAS No. :2231079-74-4
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中文名称
NCT-505
英文名称
NCT-505
英文别名
1-[6-Fluoro-3-(4-methylsulfonylpiperazine-1-carbonyl)quinolin-4-yl]-4-phenylpiperidine-4-carbonitril;NCT-505
Cas No.
2231079-74-4
分子式
C27H28FN5O3S
分子量
521.61
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
NCT-505 是一种有效的,选择性的乙醛脱氢酶 (aldehyde dehydrogenase (ALDH1A1)) 抑制剂,IC50 值为 7 nM,对 hALDH1A2,hALDH1A3,hALDH2,hALDH3A1 的抑制作用较弱,IC50 值分别为 >57,22.8,20.1,>57 μM。
生物活性
NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC 50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC 50 s, >57, 22.8, 20.1, >57 μM).
性状
Solid
IC50 & Target[1][2]
IC50: 7 nM (ALDH1A1), >57 μM (hALDH1A2), 22.8 μM (hALDH1A3), 20.1 μM (hALDH2), >57 μM (hALDH3A1)
体外研究(In Vitro)
NCT-505 (Compound 86) is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM). NCT-505 has no obvious inhibitory effec on 5-hydroxyprostaglandin dehydrogenase (HPGD) and type-4 hydroxysteroid dehydrogenase (HSD17β4) (IC50, >57 μM). Moreover, NCT-505 shows potent cellular activities, reducing the viability of OV-90 cells with an EC50 of 2.10-3.92 μM. NCT-505 is also cytotoxic to SKOV-3-TR cells, with IC50s of 1, 3, 10, 20, 30 μM, respectively, in the titration assay. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yang SM, et al. Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity. J Med Chem. 2018 Jun 14;61(11):4883-4903.
溶解度数据
In Vitro: DMSO : 100 mg/mL (191.71 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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