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147366-41-4

中文名稱 MKT 077
英文名稱 MKT 077
CAS 147366-41-4
分子式 C21H22ClN3OS2
分子量 432.002
MOL 文件 147366-41-4.mol
更新日期 2024/12/15 19:35:21
147366-41-4 結(jié)構(gòu)式 147366-41-4 結(jié)構(gòu)式

基本信息

中文別名
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)-亞基)-4-氧代噻唑烷-2-亞基)甲基)吡啶-1-鎓氯化物
英文別名
FJ 776
MKT 077
MKT077
MKT-077
FJ-776
MKT-077 >=98% (HPLC), powder
1-Ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-pyridinium chloride
Pyridinium, 1-ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-, chloride (1:1)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件2-8°C
溶解度在水中的溶解度為10mg/mL,澄清
形態(tài)粉末
顏色橙色至紅色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
WGK Germany3
RTECS號UU4023332
毒性LD50 intraperitoneal in mouse: 50mg/kg

常見問題列表

生物活性
MKT-077 (FJ-776)是一種新合成的、具有高水溶性的復(fù)合份菁染料(rhodacyanine dye),在多種模型中具有顯著的抗腫瘤活性。
靶點

HSP70

體外研究

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.

體內(nèi)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.

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