Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SAR125844 是高度选择性可逆ATP 竞争性的MET 受体酪氨酸激酶抑制剂,其IC50值为4.2 nM。能抑制细胞中MET 的自磷酸化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,390 | 现货 | ||
50 mg | ¥ 3,870 | 现货 | ||
100 mg | ¥ 6,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 886 | 现货 |
产品描述 | SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol/L) |
靶点活性 | MET RTK:4.2 nM |
体外活性 | SAR125844 inhibits MET autophosphorylation in cell-based assays in the nanomolar range, and promotes low nanomolar proapoptotic and antiproliferative activities selectively in cell lines with MET gene amplification or pathway addiction. |
激酶实验 | SAR125844 was preincubated at room temperature with each enzyme for 30 minutes in a buffer containing 10 mmol/L MOPS-NaOH pH 7.0, 0.01% Tween 20, and 1 mmol/L dithiothreitol. The enzymatic reactions were initiated by the addition of a mix of 1 ng/μL of a biotinylated poly(glutamate-alanine-tyrosine) peptide ATP and MgCl2. After 5-minute incubation at room temperature, the reactions were stopped by the addition of anti-phosphotyrosine monoclonal antibody (mAb) PT-66 -Europium cryptate and streptavidin 61SAXLB. After two hours at room temperature, the emission signals at 620 and 665 nm were recorded with a GENios reader, with an excitation wavelength of 320 nm. The percentage of inhibition versus nontreated sample was estimated using the emission ratios at 665/620 nm. |
细胞实验 | 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 Biost@t-SPEED internal software and a 4-parameter logistic model |
动物实验 | Long duration of MET kinase inhibition up to 7 days was achieved with a nanosuspension formulation of SAR125844.?Daily or every-2-days intravenous treatment of SAR125844 promoted a dose-dependent tumor regression in MET-amplified human gastric cancer models at tolerated doses without treatment-related body weight loss. |
别名 | SAR125884 |
分子量 | 550.63 |
分子式 | C25H23FN8O2S2 |
CAS No. | 1116743-46-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (81.72 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8161 mL | 9.0805 mL | 18.161 mL | 45.4025 mL |
5 mM | 0.3632 mL | 1.8161 mL | 3.6322 mL | 9.0805 mL | |
10 mM | 0.1816 mL | 0.9081 mL | 1.8161 mL | 4.5403 mL | |
20 mM | 0.0908 mL | 0.454 mL | 0.9081 mL | 2.2701 mL | |
50 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9081 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。
SAR125844 1116743-46-4 Apoptosis Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor SAR-125844 SAR-125884 inhibit SAR125884 SAR 125884 SAR 125844 inhibitor