Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0575 (ARRY-575) 是一种高选择性,有口服活性的小分子Chk1抑制剂,IC50值为1.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 645 | 现货 | ||
5 mg | ¥ 1,570 | 现货 | ||
10 mg | ¥ 2,490 | 现货 | ||
25 mg | ¥ 4,190 | 现货 | ||
50 mg | ¥ 5,880 | 现货 | ||
100 mg | ¥ 8,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM). |
靶点活性 | Chk1:1.2 nM |
体外活性 | GDC-0575 is significantly more potent in promoting DNA damage, replication stress and cell death than V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines[1] |
体内活性 | CHK1 inhibitor (CHK1i) GDC-0575 enhances AraC-mediated killing of AML cells both in vitro and in vivo, thus abrogating any potential chemoresistance mechanisms involving DNA repair. Importantly, this combination of drugs does not affect normal long-term hematopoietic stem/progenitors[2]. |
动物实验 | For in vivo experiments, aliquots of GDC-0575 (10 mg/mL) were stored at ?20℃and diluted in 100 mM sodium citrate buffer immediately prior to each experiment. GDC-0575 was used at 1.8 mg/ml for female mice (~25 g) and 2.6 mg/ml for male mice (~35 g) via oral gavage (final concentration 7.5 mg/kg). For in vitro experiments, aliquots of GDC-0575 (100 μM) were stored at ?20 ℃ and used at a final concentration of 100 nM. AraC (Cytosine β-D-arabinofuranoside C1768, Sigma) was used at 10 mg/kg (commonly used in clinical practice) for in vivo and at 100 nM and 500 nM for in vitro experiments. For in vivo experiments, toxicity of GDC-0575 was assessed in non-engrafted NSG mice using a range of concentrations of GDC-0575 in combination with AraC. 7.5 mg/kg GDC-0575 was the highest concentration to have no significant or lasting adverse effects in mice. Similarly, for in vitro experiments, 100 nM GDC-0575 in combination with 500 nM AraC was the highest concentration non-cytotoxic to MS5 stoma cell. ATR inhibitor was used at a final concentration of 0.5 μM[2]. |
别名 | ARRY-575, RG7741 |
分子量 | 378.27 |
分子式 | C16H20BrN5O |
CAS No. | 1196541-47-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (132.18 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6436 mL | 13.2181 mL | 26.4361 mL | 66.0904 mL |
5 mM | 0.5287 mL | 2.6436 mL | 5.2872 mL | 13.2181 mL | |
10 mM | 0.2644 mL | 1.3218 mL | 2.6436 mL | 6.609 mL | |
20 mM | 0.1322 mL | 0.6609 mL | 1.3218 mL | 3.3045 mL | |
50 mM | 0.0529 mL | 0.2644 mL | 0.5287 mL | 1.3218 mL | |
100 mM | 0.0264 mL | 0.1322 mL | 0.2644 mL | 0.6609 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。
GDC-0575 1196541-47-5 Cell Cycle/Checkpoint Chk RG 7741 RG-7741 GDC0575 ARRY-575 ARRY575 inhibit Inhibitor Checkpoint Kinase (Chk) ARRY 575 RG7741 GDC 0575 inhibitor