| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S88414-5mg买3赠1 |
≥98% | ￥540.00 |
货期：2-3天 | - | - | - | - |
|
S88414-10mg买3赠1 |
99.80% | ￥960.00 |
4 | - | - | - | - |
|
S88414-25mg买3赠1 |
99.80% | ￥1920.00 |
5 | - | - | - | - |
|
S88414-100mg买3赠1 |
≥98% | ￥3360.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | MKT-077 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 | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | HSP | ||||||||||||||||||||
| 体外研究： | 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. 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 | ||||||||||||||||||||
| 体内研究： | 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. 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 | ||||||||||||||||||||
| 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 | ||||||||||||||||||||
| 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 | ||||||||||||||||||||
| 参考文献： | 1. 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. 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. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | 2-8℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
