STL127705
目录号: PL02561 纯度: ≥98%
STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白 Ku 70/80 heterodimer protein 抑制剂,IC50 为 3.5 μM。STL127705 通过抑制 DNA-PKCS 激酶的激活干扰 Ku70/80 与 DNA 的结合。STL127705 显示出抗增殖和抗肿瘤活性。 STL127705 诱导细胞凋亡 (apoptosis) 。
CAS No. :1326852-06-5
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中文名称
STL127705
英文名称
STL127705
英文别名
STL127705;Compound L;7-{[2-(3,4-dimethoxyphenyl)ethyl]amino}-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione;2-[2-(3,4-dimethoxyphenyl)ethylamino]-6-(3-fluorophenyl)-8H-pyrimido[4,5-d]pyrimidine-5,7-dione
Cas No.
1326852-06-5
分子式
C22H20FN5O4
分子量
437.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白 Ku 70/80 heterodimer protein 抑制剂,IC50 为 3.5 μM。STL127705 通过抑制 DNA-PKCS 激酶的激活干扰 Ku70/80 与 DNA 的结合。STL127705 显示出抗增殖和抗肿瘤活性。 STL127705 诱导细胞凋亡 (apoptosis) 。
生物活性
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC 50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis.
性状
Solid
IC50 & Target[1][2]
IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS)
体外研究(In Vitro)
STL127705 (Compound L) (0-100 μM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase.
antiproliferative activity (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells.
STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner.
TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine. 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]. Weterings E, et al. A novel small molecule inhibitor of the DNA repair protein Ku70/80. DNA Repair (Amst). 2016 Jul;43:98-106.
[2]. Guo N, et al. Inhibiting nonhomologous end-joining repair would promote the antitumor activity of gemcitabine in nonsmall cell lung cancer cell lines. Anticancer Drugs. 2022 Jun 1;33(5):502-508.
溶解度数据
In Vitro: DMSO : 2.4 mg/mL (5.49 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic) (insoluble) STL127705 is usually formulated as a suspension.
搜索质检报告(COA)

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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