MKT 077|147366-41-4|(FJ-776)-陌孚医药/Medlife

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MKT 077 (Synonyms: FJ-776)

目录号: PC15739 纯度: ≥98%

CAS No. :147366-41-4

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中文名称	MKT 077
英文名称	MKT 077
英文别名	Pyridinium,1-ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-,chloride (1:1);3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one,chloride;MKT 077;1-ethyl-2-{(Z)-[(5E)-3-ethyl-5-(3-methyl-1,3-benzothiazol-2(3H)-ylidene)-4-oxo-1,3-thiazolidin-2-ylidene]methyl}pyridinium chloride;FJ-776(formerly);MKT-077;SDZ-MKT-077;1-Ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-pyridinium chloride;FJ-776;FJ 776;1,3-thiazolidin-4-one chloride;D70021;(2Z,5E)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-;yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-
Cas No.	147366-41-4
分子式	C₂₁H₂₂ClN₃Os₂
分子量	432.00
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.

性状

Solid

IC50 & Target[1][2]

HSP70

体外研究(In Vitro)

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 EC₅₀ values of 1.4±0.2 and 2.2±0.2 μM against MDA-MB-231 and MCF7 breast cancer cells, respectivelyl.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Starenki D, et al. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival 体外研究 and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. [Information]

[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). [Information]

[3]. 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. [Information]

溶解度数据

体外研究:

DMSO : 56.67 mg/mL (131.18 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3148 mL	11.5741 mL	23.1481 mL
5 mM	0.4630 mL	2.3148 mL	4.6296 mL
10 mM	0.2315 mL	1.1574 mL	2.3148 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 4.25 mg/mL (9.84 mM); Clear solution

此方案可获得 ≥ 4.25 mg/mL (9.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 4.25 mg/mL (9.84 mM); Suspended solution; Need ultrasonic

此方案可获得 4.25 mg/mL (9.84 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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