Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UM-164 (DAS-DFGO-II) 是一种高效的c-Src 抑制剂,Kd 为 2.7 nM。它还抑制p38α和p38β活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
2 mg | ¥ 392 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,130 | 现货 | ||
100 mg | ¥ 4,480 | 现货 |
产品描述 | UM-164 (DAS-DFGO-II), a highly potent c-Src inhibitor with a dissociation constant (Kd) of 2.7 nM, also effectively inhibits p38α and p38β. |
靶点活性 | c-Src:2.7 nM |
体外活性 | UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 Kd=2.7 nM, Dasatinib Kd=0.7 nM) in biochemical assays. To confirm that UM-164 is capable of inhibiting the activation of c-Src in vitro, the effect of UM-164 is examined on the c-Src autophosphorylation in two TNBC cell lines (MDA-MB 231 and SUM 149). Inhibition of c-Src autophosphorylation is detected in a concentration- and a time-dependent manner. At 120 minutes, complete abrogation of c-Src autophosphorylation is observed at 50 nM, demonstrating that UM-164 is a potent c-Src inhibitor in vitro. Flow cytometry experiments demonstrate that UM-164 treatment of MDA-MB 231 and SUM 149 increased the proportion of G0-G1 cells by 25% and 28%, respectively, and concurrently decreased the fraction of S cells by 16% and 19%, respectively[1]. |
体内活性 | A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 and SUM 149 cell lines. After the tumors become palpable, the mice are randomized into control and treatment groups. Mice are injected intraperitoneally with either drug (10 and 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164, there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg and 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 and P<0.004, respectively)[1]. |
细胞实验 | MDA-MB 231 and SUM 149 cells are plated in triplicate on 60 mm dishes at a density of 1×106 cells/flask. After 24 h, a final concentration of 1 μM UM-164 is added to the cells and incubated for 24 h. Growth medium is then removed and cells are washed with PBS. The remaining cells are trypsinized, harvested, and placed together with growth medium and PBS. Cells are pelleted and re-suspended in 3 mL of 75% ethanol, followed by overnight storage at - 20°C. After incubation, cells are centrifuged at 1,500 rpm for 5 min and the cell pellets are re-suspended in 0.05 mg/mL propidium iodide (10 μg/mL) containing 300 μg/mL RNase. Cell clumps are filtered. Cell DNA content is measured on flow cytometer and cell cycle distribution is calculated from 10,000 cells using FACS analysis[1] . |
动物实验 | Mice[1] |
别名 | UM164, DAS-DFGO-II |
分子量 | 640.68 |
分子式 | C30H31F3N8O3S |
CAS No. | 903564-48-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 156.1 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5608 mL | 7.8042 mL | 15.6084 mL | 39.021 mL |
5 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL | 7.8042 mL | |
10 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9021 mL | |
20 mM | 0.078 mL | 0.3902 mL | 0.7804 mL | 1.9511 mL | |
50 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL | |
100 mM | 0.0156 mL | 0.078 mL | 0.1561 mL | 0.3902 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。
UM-164 903564-48-7 Angiogenesis Autophagy MAPK Tyrosine Kinase/Adaptors p38 MAPK Src UM164 DAS-DFGO-II inhibit UM 164 Inhibitor inhibitor