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.

MKT-077(0.1-10 μM)处理48小时后能有效降低TT细胞的活力。MKT-077使细胞在G0/G1期的积累以剂量依赖的方式增加，并且也以剂量依赖的方式增加TT细胞培养中的sub-G0/G1期细胞群体。此外，MKT-077还下调TT和MZ-CRC-1细胞中的增殖标志物Ki67和S期转录因子E2F-1的细胞水平。而且，与MZ-CRC-1细胞相比，TT细胞能够摄取并保留更高水平的MKT-077 [1]。MKT-077对MCF7和MDA-MB-231乳腺癌细胞的EC50值分别为1.4±0.2和2.2±0.2 μM [2]。

系统性给药MKT-077显著延缓了小鼠TT异种移植瘤的生长。在化合物治疗结束时，我们发现MKT-077治疗组的瘤重量约为对照组的两倍。这些数据与我们在体外环境中观察到的MKT-077的生长抑制效果一致[1]。来自接受了连续5天每天一次15 mg/kg体重MKT-077的静脉注射的大鼠肝脏中分离出的线粒体，在琥珀酸诱导、ADP刺激的呼吸率显著低于未处理对照组[3]。

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].

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].