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DMU-212

Cat No.:V52171 Purity: ≥98%
DMU-212 is a methylated analogue of resveratrol with anti-mitotic, antiproliferation, antioxidant and pro-apoptotic activities.
DMU-212
DMU-212 Chemical Structure CAS No.: 134029-62-2
Product category: Apoptosis
This product is for research use only, not for human use. We do not sell to patients.
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5mg
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50mg
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Product Description
DMU-212 is a methylated analogue of resveratrol with anti-mitotic, antiproliferation, antioxidant and pro-apoptotic activities. DMU-212 causes mitotic arrest by inducing apoptosis and activating ERK1/2 proteins. DMU-212 is orally bioactive.
DMU-212 is a methylated derivative of resveratrol with anti-mitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It is an orally active compound that induces apoptosis and activates ERK1/2 protein to block mitosis. DMU-212 has anti-angiogenic and anti-tumor properties. The compound has the molecular formula C18H20O4 and a molecular weight of 300.34.
Biological Activity I Assay Protocols (From Reference)
Targets
DMU-212 targets ERK (extracellular signal-regulated kinase) signaling pathways. The compound is a methylated derivative of resveratrol, a natural polyphenol with known anticancer and antioxidant activities. DMU-212 induces apoptosis and activates ERK1/2 protein to block mitosis. The compound has anti-mitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities.
ln Vitro
DMU-212 (0.3125-40 μM) prevents human melanoma cells A375, MeWo, Bro, and M5 from growing [1]. In A375 cells, DMU-212 (30–50 μM; 24 hours) causes apoptosis, ERK activation, and the overexpression of cell cycle inhibitors [1].
In vitro studies demonstrate that DMU-212 has anti-mitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. The compound induces apoptosis and activates ERK1/2 protein to block mitosis. DMU-212 has anti-angiogenic and anti-tumor properties. The compound is a derivative of resveratrol with enhanced activity. No detailed IC50 or EC50 values have been published in the available literature.
ln Vivo
In human ovarian cancer xenograft models, DMU-212 (50 mg/kg; ig; three times weekly; for 14 days) inhibits the growth of tumors [2].
In vivo, DMU-212 is orally active and has anti-tumor properties. The compound has shown anti-angiogenic activity in preclinical models. Its ability to induce apoptosis and activate ERK1/2 suggests that it could have potential for in vivo applications in cancer therapy. Further studies would be needed to evaluate its efficacy in animal models of cancer.
Enzyme Assay
The ERK activating activity of DMU-212 can be assessed using in vitro kinase assays or cell-based assays. In a typical assay, cells are treated with varying concentrations of DMU-212, and ERK1/2 phosphorylation is assessed by Western blotting using phospho-specific antibodies. Apoptosis is assessed by annexin V/propidium iodide staining or caspase activation assays. Cell proliferation is measured using MTT or CellTiter-Glo assays.
Cell Assay
Cell Proliferation Assay[1]
Cell Types: A375 cells, MeWo cells, M5 cells, Bro cells
Tested Concentrations: 0.3125 μM, 0,625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Duration: 96 hrs (hours)
Experimental Results: Inhibited the cellular proliferation of human melanoma cells at submicromolar or micromolar concentrations (IC50=0.5 μM for A375 and Bro and IC50= 1.25 μM for MeWo and M5 cells).

Cell Cycle Analysis[1]
Cell Types: A375 cells
Tested Concentrations: 20 μM, 30 μM, 50 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Caused a marked increase in the levels of p21, p53 and cyclin B1 proteins with a concomitant decrease in the levels of cyclin A2.

Western Blot Analysis[1]
Cell Types: A375 cells
Tested Concentrations: 20 μM, 30 μM, 50 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Significant upregulated Bax, caspase 3 and caspase 9 protein levels, while diminished the levels of the anti-apoptotic protein Bcl-2.

Apoptosis Analysis[1]
Cell Types: A375 cells
Tested Concentrations: 10 μM, 20 μM
Incubation Duration: 24 hrs (hours), 36 hrs (hours)
Experimental Results: Induced apoptosi
The cellular activity of DMU-212 is assessed using cancer cell lines. Cells are treated with varying concentrations of DMU-212. ERK1/2 activation is assessed by Western blotting using phospho-specific antibodies. Apoptosis is assessed by annexin V/propidium iodide staining or caspase activation assays. Cell proliferation is measured using MTT or CellTiter-Glo assays. Anti-angiogenic activity is assessed using endothelial cell tube formation assays.
Animal Protocol
Animal/Disease Models: 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenografts[2]
Doses: 50 mg/kg
Route of Administration: po (oral gavage), three times a week, for 14 days
Experimental Results: Lowered tumor burden.
DMU-212 has been evaluated in preclinical animal models of cancer. In these studies, the compound is administered orally. Tumor growth, angiogenesis, and apoptosis are assessed. The compound has shown anti-angiogenic and anti-tumor properties. Its oral activity makes it suitable for oral administration in animal models.
ADME/Pharmacokinetics
DMU-212 is orally active, indicating favorable oral bioavailability. The compound has a molecular weight of 300.34 and a molecular formula of C18H20O4. It has a purity of ≥98%. The compound is soluble in DMSO. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including plasma protein binding, clearance, and half-life.
Toxicity/Toxicokinetics
No detailed toxicity data has been published for DMU-212. As a derivative of resveratrol, it may have a favorable safety profile. Resveratrol and its derivatives are generally well-tolerated and have antioxidant properties that may be beneficial. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
References

[1]. Activation of ERK1/2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4.

[2]. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.

Additional Infomation
DMU-212 (CAS# 134029-62-2) is a methylated derivative of resveratrol with anti-mitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It is orally active and induces apoptosis and activates ERK1/2 to block mitosis. DMU-212 has anti-angiogenic and anti-tumor properties. The molecular formula is C18H20O4 and molecular weight is 300.34. The compound is a research tool for studying resveratrol derivatives and cancer therapy.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H20O4
Molecular Weight
300.35
Exact Mass
300.136
CAS #
134029-62-2
PubChem CID
5388065
Appearance
White to off-white solid powder
Density
1.1±0.1 g/cm3
Boiling Point
444.0±40.0 °C at 760 mmHg
Flash Point
144.1±34.2 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.588
LogP
4.37
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
6
Heavy Atom Count
22
Complexity
322
Defined Atom Stereocenter Count
0
SMILES
COC1=CC=C(C=C1)/C=C/C2=CC(=C(C(=C2)OC)OC)OC
InChi Key
GGFQQRXTLIJXNY-AATRIKPKSA-N
InChi Code
InChI=1S/C18H20O4/c1-19-15-9-7-13(8-10-15)5-6-14-11-16(20-2)18(22-4)17(12-14)21-3/h5-12H,1-4H3/b6-5+
Chemical Name
1,2,3-trimethoxy-5-[(E)-2-(4-methoxyphenyl)ethenyl]benzene
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : 20 mg/mL (66.59 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2 mg/mL (6.66 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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3294 mL 16.6472 mL 33.2945 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 mL
10 mM 0.3329 mL 1.6647 mL 3.3294 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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