| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
MDL-800 effectively activates SIRT6 at approximately 10 μM, but shows no activity against SIRT1, SIRT3, SIRT4, and HDAC1-11 at concentrations as high as 50 or 100 μM. Although MDL-800 exhibits weak activity against SIRT2, SIRT5, and SIRT7, its EC50 or IC50 values are greater than 100 μM, which is ten times lower than that against SIRT6 [1]. MDL-800 directly activates SIRT6 deacetylation by increasing the binding affinity of acetylated substrates and cofactors and improving the catalytic efficiency of SIRT6 [1]. MDL-800 (1-1000 μM; 48 h) reduced the proliferation of Bel7405, PLC/PRF/5 and Bel7402 cells, with IC50 values for cell growth of 23.3 μM, 18.6 μM and 24.0 μM, respectively, and EC50 values for cell death (EC50-death) of 90.4 μM, 87.0 μM and 106.5 μM, respectively [1]. MDL-800 (0-50 μM; 24 and 48 h) reduced H3K9ac and H3K56ac at a concentration of 10 μM and showed a dose-dependent effect on Bel7405, PLC/PRF/5 and Bel7402 cells at 24 and 48 h [1].
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| ln Vivo |
MDL800 showed potent antitumor efficacy in female BALB/c nude mice with xenografted Bel7405 tumor model. Compared with the use of the vector alone, MDL800 (50-150 mg/kg; intraperitoneal injection; over 2 weeks) inhibited the growth of Bel7405 xenografts in a dose-dependent manner [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Bel7405, PLC/PRF/5, and Bel7402 cells Tested Concentrations: 1, 10, 100 , 1000 μM Incubation Duration: 48 hours Experimental Results: Decreased the proliferation of Bel7405, PLC/PRF/5, and Bel7402 cells with IC50s of 23.3 μM, 18.6 μM, and 24.0 μM, respectively. Western Blot Analysis[1] Cell Types: Bel7405, PLC/PRF/5, and Bel7402 cells Tested Concentrations: 0, 5, 10, 25, and 50 μM Incubation Duration: 24 and 48 hours Experimental Results: Decreased both H3K9ac and H3K56ac at a concentration of 10 µM and showed a dose-dependent effect in all three cell lines at 24 h and 48 h. |
| Animal Protocol |
Animal/Disease Models: Six-week-old female BALB/c nude mice with Bel7405 xenograft tumor mode[1]
Doses: 50, 100, and 150 mg/kg Route of Administration: Intraperitoneal injection; over 2 weeks. Experimental Results: Suppressed the growth of Bel7405 xenografts in a dose-dependent manner. Decreased tumor weight and size. |
| References |
| Molecular Formula |
C21H16BRCL2FN2O6S2
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|---|---|
| Molecular Weight |
626.30
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| CAS # |
2275619-53-7
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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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) |
DMSO : ~125 mg/mL (~199.58 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.32 mM)(saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 clear DMSO stock solution (20.8 mg/mL) was added to 400 μL of PEG300 and mixed thoroughly. Then, 50 μL of Tween-80 was added to the above system and mixed thoroughly. Finally, 450 μL of physiological saline was added to bring the volume to 1 mL. Preparation of physiological saline: 0.9 g of sodium chloride was dissolved in ddH₂O and brought to a volume of 100 mL to obtain a clear and transparent physiological saline solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.32 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clarified DMSO stock solution to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5967 mL | 7.9834 mL | 15.9668 mL | |
| 5 mM | 0.3193 mL | 1.5967 mL | 3.1934 mL | |
| 10 mM | 0.1597 mL | 0.7983 mL | 1.5967 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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