Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CH5138303 是一种可口服的 Hsp90 抑制剂,Kd 为 0.48 nM。
产品描述 | CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. |
靶点活性 | HSP90 α:0.48 nM(Kd) |
体外活性 | CH5138303 shows high affinity to Hsp90αand potent cell growth inhibitory activity against an HCT116 colorectal cancer cell line and an NCI-N87 gastric cancer cell line with IC50 of 98 nM and 66 nM, respectively. [1] Besides, CH5138303 also demonstrates liver microsomal stability. [1] |
体内活性 | CH5138303 (50 mg/kg p.o.) displays high oral bioavailability in mice and produces potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.[1] |
激酶实验 | Surface plasmon resonance direct binding assay for Hsp90α: Measurements are performed on a Biacore2000 at a flow rate of 30 μL/min, 25 °C in 50 mM Tris-based saline, pH 7.6, 0.005% Tween20 and 1% DMSO. Biotinylated N-terminal Hsp90α (9–236) is coupled on a streptavidin-coated surface of a sensorchip to a density of ca. 2000 RU. |
细胞实验 | HCT116 cell line and NCI-N87 cell line are cultured according to the supplier's instructions. Cells suspended in a medium are added to solutions containing various concentrations of the test substance, and the cells are cultured at 37 °C in 5% CO2. Four days later, Cell Counting Kit-8 solution is added and absorbance at 450 nm is measured with Microplate-Reader iMark. Antiproliferative activity is calculated by the formula (1?T/C) × 100 (%), where T represents the absorbance of drug-treated cells and C that of untreated control cells at 450 nm. The 50% inhibition concentration (IC50) values are calculated using Microsoft Excel 2007.(Only for Reference) |
分子量 | 415.9 |
分子式 | C19H18ClN5O2S |
CAS No. | 959763-06-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 77 mg/mL (185.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4044 mL | 12.0221 mL | 24.0442 mL | 60.1106 mL |
5 mM | 0.4809 mL | 2.4044 mL | 4.8088 mL | 12.0221 mL | |
10 mM | 0.2404 mL | 1.2022 mL | 2.4044 mL | 6.0111 mL | |
20 mM | 0.1202 mL | 0.6011 mL | 1.2022 mL | 3.0055 mL | |
50 mM | 0.0481 mL | 0.2404 mL | 0.4809 mL | 1.2022 mL | |
100 mM | 0.024 mL | 0.1202 mL | 0.2404 mL | 0.6011 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。
CH5138303 959763-06-5 Cytoskeletal Signaling Metabolism HSP gastric cancer inhibit CH-5138303 Inhibitor antitumor agent Hsp90 inhibitor orally active Heat shock proteins NCI-N87 CH 5138303 HCT116 inhibitor