Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SAR125884 hydrochlorid (1116743-46-4(free base)) 是一种有效的选择性 MET 激酶抑制剂,具有良好的临床前毒性特征 (IC50=4.2 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 516 | 现货 | ||
5 mg | ¥ 898 | 现货 | ||
10 mg | ¥ 1,480 | 现货 | ||
25 mg | ¥ 3,190 | 现货 | ||
50 mg | ¥ 4,670 | 现货 | ||
100 mg | ¥ 6,670 | 现货 | ||
200 mg | ¥ 8,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,470 | 现货 |
产品描述 | SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM). |
靶点活性 | MET RTK:4.2 nM |
体外活性 | MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium. Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated. IC50 values were calculated using the software and a 4-parameter logistic model[1]. |
体内活性 | SAR125844 inhibited autophosphorylation of AXL and cell proliferation of TPM–NTRK1-overexpressing KM12 cell line with IC50 values of 110 and 1,400 nmol/L, respectively, indicating a 30- and 500-fold selectivity index for AXL and NTRK1 in cell-based assays. The selectivity profile of SAR125844 was further confirmed in cell lines with a single-digit nanomolar antiproliferative activity in MET-addicted cell lines and a complete lack of impact in cells not addicted to the MET pathway. This is in contrast to ARQ197 that has equal antiproliferative activity on MET-addicted and MET-independent tumor cell lines[1]. |
动物实验 | The antitumor activity of SAR125844 was investigated after administration of SAR125844 solution daily in SNU-5 bearing mice at 10, 20, and 45 mg/kg and every 2 days in Hs 746T tumor–bearing mice (at 5, 10, 20, and 45 mg/kg for SAR125844 solution and at 5, 11, 21, 53, 106, and 213 mg/kg for SAR125844 nanosuspension). Tumor volumes (in mm^3, based on the following formula, volume = length (mm) × width2 (mm2)/2), were measured twice weekly and body weight recorded every day. Endpoints collected were complete regressions (CR, regression below the palpable limit), partial regressions (PR, regression of 50% of the initial tumor volume), and the percentage of tumor regression (% of volume decrease posttreatment compared with pretreatment). Statistical significance was determined by a Dunnett test versus vehicle after a two-way ANOVA with repeated measures performed separately on ranks of changes from baseline with P < 0.05 considered significant[1]. |
分子量 | 587 |
分子式 | C25H23FN8O2S2.HCl |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (93.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7036 mL | 8.5179 mL | 17.0358 mL | 42.5894 mL |
5 mM | 0.3407 mL | 1.7036 mL | 3.4072 mL | 8.5179 mL | |
10 mM | 0.1704 mL | 0.8518 mL | 1.7036 mL | 4.2589 mL | |
20 mM | 0.0852 mL | 0.4259 mL | 0.8518 mL | 2.1295 mL | |
50 mM | 0.0341 mL | 0.1704 mL | 0.3407 mL | 0.8518 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。
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