中文名 | MKT 077 |
英文名 | MKT 077 |
别名 | 化合物MKT-077 1-乙基-2-((Z)-((Z)-3-乙基-5-(3-甲基苯并[D]噻唑-2(3H)-亚基)-4-氧代噻唑烷-2-亚基)甲基)吡啶-1-鎓氯化物 |
英文别名 | FJ 776 MKT077 FJ-776 MKT-077 MKT 077 1-Ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-pyridinium chloride 1-Ethyl-2-((Z)-((Z)-3-ethyl-5-(3-methylbenzo[d]thiazol-2(3H)-ylidene)-4-oxothiazolidin-2-ylidene)methyl)pyridin-1-ium chloride |
CAS | 147366-41-4 |
化学式 | C21H22ClN3OS2 |
分子量 | 432.00188 |
溶解度 | H2O: 可溶10mg/mL,澄清 |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | orange to red |
体外研究 | MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity. MKT-077 treatment (0.1 to 10 µM dose ranges) for 48 hours can effectively decrease TT cell viability. MKT-077 treatment results in accumulation of cells in the G0/G1 phase in a dose-dependent manner, and also increases 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, flow cytometry using different doses of MKT-077 reveales that TT cells can uptake and retain MKT-077 at significantly higher levels than MZ-CRC-1 cells. MKT-077 has EC 50 values of 1.4±0.2 and 2.2±0.2 μM against MDA-MB-231 and MCF7 breast cancer cells, respectivelyl. |
体内研究 | Systemic administration of MKT-077 significantly delays the growth of TT xenografts in mice throughout the treatment. At the end of MKT-077 treatment, it is found that tumor weights are about two-times less in MKT-077-treated group than in control group. MKT-077 treatment also results in weight loss and general toxicity in animals. Results show that 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. |
WGK Germany | 3 |
RTECS | UU4023332 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.315 ml | 11.574 ml | 23.148 ml |
5 mM | 0.463 ml | 2.315 ml | 4.63 ml |
10 mM | 0.231 ml | 1.157 ml | 2.315 ml |
5 mM | 0.046 ml | 0.231 ml | 0.463 ml |
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