Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Triciribine (NSC-154020) 是一种 DNA 合成抑制剂,也抑制 Akt 和 HIV-1/2,IC50分别为 130 nM 和 0.02-0.46 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 439 | 现货 | ||
5 mg | ¥ 682 | 现货 | ||
10 mg | ¥ 945 | 现货 | ||
25 mg | ¥ 1,790 | 现货 | ||
50 mg | ¥ 3,160 | 现货 | ||
100 mg | ¥ 4,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 756 | 现货 |
产品描述 | Triciribine (NSC-154020) is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2. |
靶点活性 | HIV-1:20 nM, Akt:130 nM |
体外活性 | Triciribine 在1-10 μM 范围内展现出最大的生长抑制作用,且在100 μM 时能够将Akt及其下游的p70S6K的磷酸化水平抑制至基础水平(IC50 = 130 nM)。特别地,Triciribine 对于Nf1和Trp53突变的星形细胞瘤细胞的生长抑制表现出等级依赖性的承诺。WHO II K1861-10 线被部分抑制(最大抑制率为69%),Triciribine 的GI50值为1.7 μM,而更高级别的肿瘤线(KR158, KR130, 和 SF295)在更低的GI50值(0.4–1.1 mM)下被更大程度地抑制(>80%最大抑制率)。重要的是,Triciribine 对初级星形胶质细胞的抑制作用较弱(GI50 13.6 mM),这表明这种抑制剂可能对肿瘤细胞具有特异性。[1] Triciribine 对HIV-1的IC50为20 nM,在0.1 μM 时可实现超过90%的抑制,而在5 μM 时能完全抑制合胞体形成。Triciribine 在同一细胞系中的相关细胞毒性为46 μM,从而得到2250的选择性指数。Triciribine 显著地以剂量依赖性方式抑制HIV-1急性感染的CEM-SS、H9细胞和持续感染的H9III B和U1细胞中的p24核心抗原生产、逆转录酶和传染性病毒生产。[2] Triciribine 抑制人前列腺癌细胞系PC-3中的Akt在Thr308和Ser473的磷酸化和Akt活性,使PC-3细胞对TRAIL和抗CD95诱导的凋亡敏感,而对DNA损伤化疗药物则保持抵抗。[3] Triciribine 对Akt具有高度选择性,不抑制磷脂酰肌醇3激酶、磷脂酰肌醇依赖性激酶-1、蛋白激酶C、血清和糖皮质激素诱导激酶、蛋白激酶A、信号转导和转录激活因子3、外胞素信号调节激酶-1/2或c-Jun NH2-末端激酶的激活。[4] |
体内活性 | 1 mg/kg/day i.p. treated Triciribine inhibits OVCAR3, OVCAR8 and PANC1 tumor growth, which overexpressing Akt, by 90%, 88% and 80% in nude mice, respectively. However, Triciribine has little effect on the growth of OVCAR5 and COLO357 cells. [4] |
激酶实验 | Akt Phosphorylation Changes Assay: Cells are grown to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of epidermal growth factor or platelet derived growth factor (PDGF)–AA with or without 10–20 mM of U0126 or LY-294002. Protein lysates (5–20 μg) are separated by 12%–15% SDS PAGE and analyzed by Western blot for Akt, phosphorylated Akt (phospho-Ser 473), MAPK, and phosphorylated MAPK (p44/42 phospho-Thr202/Tyr204) antibodies (1:1000). |
细胞实验 | Triciribine is evaluated for cytotoxicity by seeding CEM-SS cells at a density of 1 × 104 cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of Triciribine are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [3H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis.(Only for Reference) |
别名 | VD-0002, Tricyclic nucleoside, NSC 154020, 曲西立滨, API-2, TCN |
分子量 | 320.3 |
分子式 | C13H16N6O4 |
CAS No. | 35943-35-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
1eq. HCl: 32 mg/mL (100 mM)
DMSO: 32 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
1eq. HCl / DMSO | 1 mM | 3.1221 mL | 15.6104 mL | 31.2207 mL | 78.0518 mL |
5 mM | 0.6244 mL | 3.1221 mL | 6.2441 mL | 15.6104 mL | |
10 mM | 0.3122 mL | 1.561 mL | 3.1221 mL | 7.8052 mL | |
20 mM | 0.1561 mL | 0.7805 mL | 1.561 mL | 3.9026 mL | |
50 mM | 0.0624 mL | 0.3122 mL | 0.6244 mL | 1.561 mL | |
100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7805 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。
Triciribine 35943-35-2 Cell Cycle/Checkpoint Cytoskeletal Signaling DNA Damage/DNA Repair Microbiology/Virology PI3K/Akt/mTOR signaling Proteases/Proteasome Akt HIV Protease DNA/RNA Synthesis Inhibitor HIV VD0002 inhibit VD-0002 PKB Protein kinase B Tricyclic nucleoside NSC 154020 曲西立滨 NSC-154020 API-2 NSC154020 Human immunodeficiency virus VD 0002 API2 API 2 TCN inhibitor