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STL127705
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STL127705图片
CAS NO:1326852-06-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
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产品介绍
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 potentKu 70/80 heterodimer proteininhibitor with anIC50of 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 inducesapoptosis[1][2].

IC50& Target

IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS)[1]

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[1].
antiproliferative activity (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells[1].
STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner[1].
TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine[2].

Cell Viability Assay[1]

Cell Line:SF-767, PrEC cells
Concentration:0-40 μM
Incubation Time:6 h
Result:Showed cytotoxicity in a dose dependent manner.

Western Blot Analysis[1]

Cell Line:SF-767 cells
Concentration:0-100 μM
Incubation Time:pre-treated for 2 h and then co-incubation 4 h
Result:Decreased the DNA-PKCS autophosphorylation but total DNA-PKCS was not suppressed by STL127705.

Apoptosis Analysis[1]

Cell Line:H1299 cells
Concentration:1 μM
Incubation Time:48 h
Result:Induced apoptosis with apoptosis rate significantly increased to 76% when treated with STL127705 in combination with gemcitabine.
分子量

437.42

性状

Solid

Formula

C22H20FN5O4

CAS 号

1326852-06-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
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.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2861 mL11.4307 mL22.8613 mL
5 mM0.4572 mL2.2861 mL4.5723 mL
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。