| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
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| ln Vitro |
Compared to other demethylase subfamily members examined (IC50=127 μM for KDM3A, or higher for other demethylases), dacazine is >100-fold more selective for the KDM2/7 subfamily [1].
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| ln Vivo |
The model organism Drosophila melanogaster is teratogenic and genotoxic when exposed to doses of 200–20,000 ppm of dinonozide [2].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Daminozide has been studied in minipigs chosen because of the similar stomach conditions to the human. They were given oral doses of radio-labelled test material at 5 mg/kg bw. It was found to be rapidly excreted with approximately 60% excreted by 48 hours. The metabolite (UDMH) was found in urine at up to 2.8 ppm; lesser amounts were found in the feces. Radio-labelled 1,1-dimethylnitrosamine at levels of 0.69 ppm... were also found in the urine of the test animals. A second study was performed with a dermal application of radio-labelled daminozide covering dermal surfaces with concentrations of 0.5, 0.05, or 0.005 mg/cu cm for periods up to 24 hours. As much as 1.8% of the dose was absorbed and excreted by the test animals in 24 hours. Distribution and metabolic fate of (14)C daminozide in Silver maple and American sycamore seedlings were studied by auto radiography. Radioactivity was detected in all parts of plant. (14)C concentrated in meristematic regions of leaves. Analysis of extracts from red oak (Quercus rubra) administered (14)C-labeled maleic hydrazide or daminozide indicated that both growth inhibitors were distributed acropetally as well as basipetally over a 22 day period. When leaves of 3 yr old apple trees, CV Cox's orange pippin, were painted with (14)C-labeled daminozide, over half of radioactivity accumulated in fruits. Metabolism / Metabolites Metabolites /in plants/ include 1,1-dimethylhydrazine. |
| Toxicity/Toxicokinetics |
Toxicity Data
LC50 (rat) > 147,000 mg/m3/1h Non-Human Toxicity Values LD50 Rat oral 8,400 mg/kg LD50 Rabbit percutaneous > 5000 mg/kg LD50 Mouse oral 6300 mg/kg LD50 Mouse ip 1325 mg/kg LC50 Rat inhalation >20 mg/L/hr |
| References |
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| Additional Infomation |
Daminozide can cause cancer according to The Environmental Protection Agency (EPA).
Succinic acid 2,2-dimethylhydrazide appears as odorless white crystals or powder. (NTP, 1992) Daminozide is a straight-chain fatty acid. Daminozide — also known as Alar, Kylar, B-NINE, DMASA, SADH, or B 995 — is a plant growth regulator, a chemical sprayed on fruit to regulate their growth, make their harvest easier, and keep apples from falling off the trees before they are ripe. This makes sure they are red and firm for storage. Alar was first approved for use in the U.S. in 1963, it was primarily used on apples until 1989 when it was voluntarily withdrawn by the manufacturer after the U.S. Environmental Protection Agency proposed banning it based on unacceptably high cancer risks to consumers. |
| Molecular Formula |
C6H12N2O3
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|---|---|
| Molecular Weight |
160.173
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| Exact Mass |
160.084
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| CAS # |
1596-84-5
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| PubChem CID |
15331
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
329.5±44.0 °C at 760 mmHg
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| Melting Point |
162-164 °C(lit.)
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| Flash Point |
153.1±28.4 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.497
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
11
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| Complexity |
156
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NOQGZXFMHARMLW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H12N2O3/c1-8(2)7-5(9)3-4-6(10)11/h3-4H2,1-2H3,(H,7,9)(H,10,11)
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| Chemical Name |
4-(2,2-dimethylhydrazinyl)-4-oxobutanoic acid
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| Synonyms |
DIMG; B 995; Aminozide
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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 : ~106.67 mg/mL (~665.98 mM)
H2O : ~100 mg/mL (~624.34 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.61 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 25.0 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: ≥ 2.5 mg/mL (15.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (15.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (624.34 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2434 mL | 31.2168 mL | 62.4337 mL | |
| 5 mM | 1.2487 mL | 6.2434 mL | 12.4867 mL | |
| 10 mM | 0.6243 mL | 3.1217 mL | 6.2434 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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