keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MKT-077 (FJ-776) 是一种阳离子红花青染料,通过抑制 Hsp70 分子伴侣家族成员的能力,显示出对癌细胞系的抗增殖活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,520 | 现货 | ||
50 mg | ¥ 3,760 | 现货 | ||
100 mg | ¥ 5,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | MKT-077 (FJ-776) is a cationic rhodacyanine dye that demonstrates antiproliferative activity against cancer cell lines (EC50s: 1.4-2.2 μM in vitro) through its ability to inhibit members of the Hsp70 family of molecular chaperones. |
体外活性 | MKT-077 treatment (0.1-10 μM) for 48 hours can effectively decrease TT cell viability. MKT-077 treatment results in the accumulation of cells in the G0/G1 phase in a dose-dependent manner, and also increases the sub-G0/G1 phase population in TT cell culture in a dose-dependent manner. MKT-077 also downregulates cellular levels of the proliferation marker, Ki67, and the S-phase transcription factor, E2F-1, in TT and MZ-CRC-1 cells. Moreover, TT cells can uptake and retain MKT-077 at significantly higher levels than MZ-CRC-1 cells [1]. MKT-077 has EC50 values of 1.4±0.2 and 2.2±0.2 μM against MCF7 and MDA-MB-231 breast cancer cells, respectively [2]. |
体内活性 | Systemic administration of MKT-077 significantly delayed the growth of TT xenografts in mice throughout the treatment. At the end of the drug treatment, we found that tumor weights were about two-timed less in MKT-077-treated group than in the control group. These data are consistent with the growth inhibitory effects of MKT-077 observed in the in vitro setting above [1]. The succinate-induced, ADP-stimulated respiratory rate in mitochondria isolated from the liver of rats treated with a bolus i.v. injection of 15 mg MKT-077 1kg body weight each day for 5 days is significantly lower than that of untreated controls [3]. |
细胞实验 | MTT assay was performed as previously described. Briefly, cells were seeded in 24 well plates and allowed to attach for 48 hours. After drug treatment, cells were incubated with 400 μL of MTT (0.5 mg/mL) in complete medium for 2 hours at 37℃, switched into 200 μL DMSO, and shaken for 5 minutes at room temperature before measuring absorbance at 540 nm [1]. |
动物实验 | The 1×10^7 TT cells in 200 μL Hank's balanced salt solution were inoculated subcutaneously into the rear flanks of 6-week-old female athymic nude (nu/nu) mice. Once palpable, tumors were measured using Vernier calipers at intervals indicated in the text. Tumor volumes (TVs) were calculated using the formula: TV=L×W^2×0.5 (L, length; W, width). When TV reached 100 mm^3, mice were sorted into groups of 8 to achieve equal distribution of tumor size in all treatment groups. Group 1 received only the vehicle (1:9 mixture of DMSO/saline) and group 2 received MKT-077 (10 mg/kg body weight/dose). A 200 μL of ether solution was administered by intraperitoneal injection every 2 days (total 10 doses). At the end of the experiments, animals were euthanized by CO2 asphyxiation [1]. |
别名 | MKT 077, FJ-776, MKT077 |
分子量 | 432 |
分子式 | C21H22ClN3OS2 |
CAS No. | 147366-41-4 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 20 mg/mL
DMSO: 55 mg/mL (127.31 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3148 mL | 11.5741 mL | 23.1481 mL | 57.8704 mL |
5 mM | 0.463 mL | 2.3148 mL | 4.6296 mL | 11.5741 mL | |
10 mM | 0.2315 mL | 1.1574 mL | 2.3148 mL | 5.787 mL | |
20 mM | 0.1157 mL | 0.5787 mL | 1.1574 mL | 2.8935 mL | |
50 mM | 0.0463 mL | 0.2315 mL | 0.463 mL | 1.1574 mL | |
100 mM | 0.0231 mL | 0.1157 mL | 0.2315 mL | 0.5787 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。
MKT-077 147366-41-4 Cytoskeletal Signaling Metabolism HSP FJ 776 MKT 077 Heat shock proteins Inhibitor FJ776 inhibit FJ-776 MKT077 inhibitor