| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
HSP70
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| ln Vitro |
Preparation of MKT-077 solution 1.1 Preparation of stock solution Dissolve 1 milligram MKT-077 in 0.2315 mL DMSO to yield 10 mM MKT-077. Note: It is advised that the stock solution be stored at -20°C or -80°C away from light. Preparation of 1.2 MKT-077 functional solution. Use serum-free cell diluent or PBS to take 5-10 μM MKT-077 working solution. Note: Please adjust the concentration of MKT-077 working fluid according to the real conditions. Staining 2.1 Cell preparation. Suspension cells: Centrifuge at 1000 g for 3-5 minutes at 4°C and discard the supernatant. Wash twice with PBS, 5 minutes each time. Adherent cells: Discard the cell culture medium and add islet dissociated cells to produce a single cell suspension. Centrifuge at 1000g for 3-5 minutes at 4°C and discard the supernatant. Wash twice with PBS, 5 minutes each time. 2.2 Add 1 mL MKT-077 working solution and pre-working solution for 30 minutes. 2.3 Centrifuge at 400 g for 3-4 minutes at 4°C and discard the supernatant. 2.4 Wash twice with PBS, 5 minutes each time. 2.5 Resuspend cells in serum-free cell culture media or PBS and detect with fluorescence microscopy or flow cytometer.
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| ln Vivo |
Systemic dormancy of MKT-077 greatly inhibited the growth of mouse TT xenografts throughout therapy. At the completion of MKT-077 treatment, the tumor weight in the MKT-077-treated group was determined to be nearly two times lower than that of the head. MKT-077 administration also leads in weight loss and overall toxicity in rats [1]. The results demonstrated that succinate-induced, ADP-stimulated respiratory rhythms in mitochondria separated from transplants given with a daily bolus injection of 15 mg MKT-077 at 1 kg body weight for 5 days were considerably lower than those in untreated cells [3 ].
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| References |
[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 |
| Molecular Formula |
C21H22CLN3OS2
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|---|---|
| Molecular Weight |
431.99
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| Exact Mass |
431.09
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| Elemental Analysis |
C, 58.39; H, 5.13; Cl, 8.21; N, 9.73; O, 3.70; S, 14.84
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| CAS # |
147366-41-4
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| Related CAS # |
147366-41-4
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| Appearance |
Solid powder
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| SMILES |
CCN1/C(=C/C2=CC=CC=[N+]2CC)/S/C(=C/3\N(C4=CC=CC=C4S3)C)/C1=O.[Cl-]
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| InChi Key |
VSKYOTRJSLYFHX-UXJRWBAGSA-M
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| InChi Code |
InChI=1S/C21H22N3OS2.ClH/c1-4-23-13-9-8-10-15(23)14-18-24(5-2)20(25)19(27-18)21-22(3)16-11-6-7-12-17(16)26-21;/h6-14H,4-5H2,1-3H3;1H/q+1;/p-1/b21-19+;
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| Chemical Name |
(2Z,5E)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride
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| Synonyms |
MKT-077; MKT077; FJ 776; FJ776; FJ-776; MKT 077;
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Water : 86 mg/mL
DMSO : 13~56.7 mg/mL (30.1~131.2 mM) Ethanol : 10 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.25 mg/mL (9.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 42.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 4.25 mg/mL (9.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 42.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3149 mL | 11.5743 mL | 23.1487 mL | |
| 5 mM | 0.4630 mL | 2.3149 mL | 4.6297 mL | |
| 10 mM | 0.2315 mL | 1.1574 mL | 2.3149 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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