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  3. MKT-077

MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity. 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.

For research use only. We do not sell to patients.

MKT-077 Chemical Structure

MKT-077 Chemical Structure

CAS No. : 147366-41-4

Size Price Stock Quantity
1 mg USD 52 In-stock
5 mg USD 110 In-stock
10 mg USD 198 In-stock
50 mg USD 550 In-stock
100 mg USD 715 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

HSP70

 

Cellular Effect
Cell Line Type Value Description References
L6 IC50
114.8 μM
Compound: 1, MKT-077
Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
[PMID: 19894726]
MCF7 EC50
2.2 μM
Compound: MKT-077
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24312699]
MDA-MB-231 EC50
1.4 μM
Compound: MKT-077
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24312699]
MEF EC50
> 50 μM
Compound: MKT-077
Cytotoxicity against C57BL/6 mouse MEF assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against C57BL/6 mouse MEF assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24312699]
In Vitro

Preparation of MKT-077 solution
1.1 Preparation of the stock solution
Dissolve 1 mg MKT-077 in 0.2315 mL DMSO to obtain 10 mM of MKT-077 .
Note: It is recommended to store the stock solution at -20 °C -80 °C away from light and avoid repetitive freeze-thaw cycles.
1.2 Preparation of MKT-077 working solution
Dilute the stock solution in serum-free cell culture medium or PBS to obtain 5-10 μM of MKT-077 working solution.
Note: Please adjust the concentration of MKT-077 working solution according to the actual situation.

Cell staining
2.1 Cell preparation.
For suspension cells: Centrifuge at 1000 g at 4°C for 3-5 minutes and then discard the supernatant. Wash twice with PBS, 5 minutes each time.
For adherent cells: Discard the cell culture medium, and add trypsin to dissociate cells to make a single-cell suspension. Centrifuge at 1000 g at 4°C for 3-5 minutes and then discard the supernatant. Wash twice with PBS, 5 minutes each time.
2.2 Add 1 mL of MKT-077 working solution, and then incubate at room temperature for 30 minutes.
2.3 Centrifuge at 400 g at 4°C for 3-4 minutes and then discard the supernatant.
2.4 Wash twice with PBS, 5 minutes each time.
2.5 Resuspend cells with serum-free cell culture medium or PBS, and then detect by fluorescence microscope or flow cytometer.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

432.00

Formula

C21H22ClN3OS2

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

CN(C1=CC=CC=C1S/2)C2=C3C(N(CC)/C(S\3)=C/C4=[N+](CC)C=CC=C4)=O.[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 56.67 mg/mL (131.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.25 mg/mL (9.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 4.25 mg/mL (9.84 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.05%

References
Cell Assay
[1]

Cells are incubated with 1 µM MKT-077 and 100 nM Mitotracker Green FM in culture medium for 30 minutes at 37°C in the dark, washed with PBS, switched into phenol-red free medium before visualizing fluorescence under a microscope. Pictures are acquired and processed with software. For flow cytometric measurement, MKT-077-treated cells are resuspended in 0.1% bovine serum albumin/PBS and analyzed by flow cytometry. Data from 20,000 cells are analyzed using FCS Express software[1].

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

Animal Administration
[1]

The 1×107 TT cells in 200 µL Hank's balanced salt solution are inoculated subcutaneously into the rear flanks of 6-week-old female athymic nude (nu/nu) mice. Once palpable, tumors are measured using calipers at intervals indicated in the text. When tumor volume reaches 100 mm3, mice are sorted into groups of 8 to achieve equal distribution of tumor size in all treatment groups. Group 1 receives only the vehicle (1:9 mixture of DMSO/saline) and group 2 receives MKT-077 (10 mg/kg body weight/dose). A 200 µL of ether solution is administered by intraperitoneal injection every 2 days (total 10 doses). At the end of the experiments, animals are euthanized by CO2 asphyxiation[1].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3148 mL 11.5741 mL 23.1481 mL 57.8704 mL
5 mM 0.4630 mL 2.3148 mL 4.6296 mL 11.5741 mL
10 mM 0.2315 mL 1.1574 mL 2.3148 mL 5.7870 mL
15 mM 0.1543 mL 0.7716 mL 1.5432 mL 3.8580 mL
20 mM 0.1157 mL 0.5787 mL 1.1574 mL 2.8935 mL
25 mM 0.0926 mL 0.4630 mL 0.9259 mL 2.3148 mL
30 mM 0.0772 mL 0.3858 mL 0.7716 mL 1.9290 mL
40 mM 0.0579 mL 0.2894 mL 0.5787 mL 1.4468 mL
50 mM 0.0463 mL 0.2315 mL 0.4630 mL 1.1574 mL
60 mM 0.0386 mL 0.1929 mL 0.3858 mL 0.9645 mL
80 mM 0.0289 mL 0.1447 mL 0.2894 mL 0.7234 mL
100 mM 0.0231 mL 0.1157 mL 0.2315 mL 0.5787 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MKT-077
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HY-15096
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