Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SF2523 是一种选择性PI3K 抑制剂,抑制DNA-PK、PI3Kα、PI3Kγ、BRD4 和 mTOR,IC50分别为 9 nM、34 nM、158 nM、241 nM 和 280 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 311 | 现货 | ||
5 mg | ¥ 743 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,270 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
500 mg | ¥ 12,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 821 | 现货 |
产品描述 | SF2523 is a highly selective and potent inhibitor. |
靶点活性 | mTOR:280 nM, PI3Kγ:158 nM, BRD4:241 nM, PI3Kα:34 nM, DNA-PK:9 nM |
体外活性 | SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target. SF2523 treatment inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs[1]. |
体内活性 | SF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, because there is no notable change in body weight. Tumors from SF2523-treated mice have significantly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors[1]. |
分子量 | 371.41 |
分子式 | C19H17NO5S |
CAS No. | 1174428-47-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (26.92 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6924 mL | 13.4622 mL | 26.9244 mL | 67.3111 mL |
5 mM | 0.5385 mL | 2.6924 mL | 5.3849 mL | 13.4622 mL | |
10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7311 mL | |
20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3656 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SF2523 1174428-47-7 Chromatin/Epigenetic DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK Epigenetic Reader Domain PI3K mTOR SF 2523 SF-2523 Inhibitor Phosphoinositide 3-kinase DNA-dependent protein kinase inhibit inhibitor