Bioactivity | MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity[1]. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm[2]. Storage: protect from light. |
Invitro | MKT-077 工作液的配制1.1 制备储存液用 DMSO 配制 10 mM 的 MKT-077。如用0.2315 mL DMSO 溶解 1 mg MKT-077。注:MKT-077 储存液建议分装后于 -20 ℃ 或 -80 ℃ 避光保存。1.2 工作液的配制用预热好的无血清细胞培养基或 PBS 稀释储存液,配制成 5-10 μM 的 MKT-077 工作液。注:请根据实际情况调整 MKT-077 工作液浓度,且现用现配。细胞染色2.1 准备工作悬浮细胞:离心收集细胞,加入 PBS 洗涤两次,每次 5 分钟。贴壁细胞:弃去培养基,加入胰蛋白酶消化细胞。离心弃去上清后,加入 PBS 洗涤两次,每次 5 分钟。2.2 加入 1 mL MKT-077 工作液,室温孵育 15 分钟。2.3 400 g,4℃ 离心 3-4 分钟,弃去上清。2.4 加入 PBS 洗涤细胞两次,每次 5 分钟。2.5 用 1 mL 无血清培养基或 PBS 重悬细胞后,在荧光显微镜或流式细胞仪下检测。 |
In Vivo | 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[1]. 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[3]. |
Name | MKT-077 |
CAS | 147366-41-4 |
Formula | C21H22ClN3OS2 |
Molar Mass | 432.00 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Starenki D, et al. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. [2]. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11).. [3]. Starenki D, et al. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. [4]. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11). [5]. Weisberg EL, et al. In vivo administration of MKT-077 causes partial yet reversible impairment of mitochondrial function. Cancer Res. 1996 Feb 1;56(3):551-5. |