Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂,IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍,具有潜在的放射增敏和化学增敏活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 583 | 现货 | ||
2 mg | ¥ 852 | 现货 | ||
5 mg | ¥ 1,280 | 现货 | ||
10 mg | ¥ 2,260 | 现货 | ||
25 mg | ¥ 3,890 | 现货 | ||
50 mg | ¥ 5,570 | 现货 | ||
100 mg | ¥ 7,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,060 | 现货 |
产品描述 | SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. |
靶点活性 | Chk1:3 nM, CDK2:0.16 μM |
体外活性 | 在吉西他滨后30分钟给药,4 mg/kg SCH 900776足以诱导γ-H2AX生物标志物,而8 mg/kg SCH 900776增强肿瘤药效动力学和退化响应.递增剂量16 mg/kg和32 mg/kg的SCH 900776诱导肿瘤响应持续改进.重要的是,在BALB/c小鼠体内,SCH 900776剂量与强的生物标志物活化相关,而提高的肿瘤响应与吉西他滨对血液学指标增强的毒性无关. |
体内活性 | 羟基脲暴露24小时后,SCH 900776诱导DNA复制能力的剂量依赖性丧失。SCH 900776增强γ-H2AX对羟基脲,5-氟尿嘧啶和阿糖孢苷的响应。SCH 900776与抗代谢物结合,在2小时内诱导γ-H2AX的累积,表明复制叉瓦解和并且双链DNA断裂。此外,SCH 900776以剂量依赖的方式抑制Chk1 pS296自磷酸化的积累。SCH 900776是Chk2和CDK2的低效抑制剂,IC50分别为1.5 μM和0.16 μM。SCH 900776对细胞色素P450人肝微粒体亚型1A2,2C9,2C19,2D6和3A4没有明显的抑制作用。 |
激酶实验 | The Millipore Kinase Profiler service is used to generate general selectivity data for SCH 900776 against a broad range of serine/threonine and tyrosine kinases. Assays are typically run at two concentrations of SCH 900776 (0.5 and 5 μM), at a fixed (10 μM) concentration of ATP. Data are provided as percent activity remaining, relative to uninhibited controls. |
细胞实验 | For cell growth assays, cells are seeded at low density (500-1000 cells) in 96-well plates and then incubated with drug for 24 h (8 wells per concentration). Following treatment, cells are washed and grown in fresh media for 5-7 days at 37°C. Prior to attaining confluence, cells are washed, lysed, and stained with Hoechst 33258. Fluorescence is read on a microplate spectrofluorometer. Results are expressed as mean and standard error for the concentration of drug that inhibited growth by 50%. |
别名 | MK 8776, MK-8776 |
分子量 | 376.25 |
分子式 | C15H18BrN7 |
CAS No. | 891494-63-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (265.78 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6578 mL | 13.289 mL | 26.5781 mL | 66.4452 mL |
5 mM | 0.5316 mL | 2.6578 mL | 5.3156 mL | 13.289 mL | |
10 mM | 0.2658 mL | 1.3289 mL | 2.6578 mL | 6.6445 mL | |
20 mM | 0.1329 mL | 0.6645 mL | 1.3289 mL | 3.3223 mL | |
50 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3289 mL | |
100 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6645 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。
SCH900776 891494-63-6 Cell Cycle/Checkpoint CDK Chk SCH-900776 Inhibitor MK 8776 SCH 900776 Checkpoint Kinase (Chk) inhibit MK-8776 MK8776 inhibitor