| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
|
||
| Other Sizes |
| Targets |
Not applicable. DNA (alkylating agent; no specific receptor).
|
|---|---|
| ln Vitro |
In vitro, N,N'-Dimethylhydrazine is a DNA alkylating agent. It is not used to measure a specific biological activity as a drug; rather, it is a mutagen and carcinogen. After metabolic activation in vivo (primarily in the liver), it generates reactive metabolites (methylating species) that alkylate DNA, particularly at the O6-position of guanine and N7-position of guanine, leading to G:C to A:T transition mutations. In colon epithelial cells, this initiates tumorigenesis through mutations in key genes such as APC, beta-catenin, K-ras, and p53. In vitro studies using isolated DNA or cultured cells (e.g., colon epithelial cells) show DNA adduct formation and increased mutation frequency.
|
| ln Vivo |
N,N'-Dimethylhydrazine (DMH) (20 mg/kg; sc; once a week, 24 wk) induces colon cancer in ICR mice[1]. N,N'-Dimethylhydrazine (20 mg/kg; sc; 20 wk) induces colon cancer tumors in rats intraperitoneally, an effect that is effectively inhibited by Lactobacillus acidophilus. Mice fed a beef diet that mimics a "Western" diet have a higher incidence of colon cancer than grain-fed mice (83% vs. 31%, respectively)[2].
In vivo, N,N'-Dimethylhydrazine is used to induce colon tumors in rodents. Administered subcutaneously (s.c.) or intraperitoneally (i.p.) to mice or rats, it causes DNA alkylation specifically in the colon epithelium, leading to adenoma and adenocarcinoma formation. The tumor incidence is dose- and time-dependent. It is NOT a therapeutic drug; rather, it is a disease-inducing agent used to create animal models of colorectal cancer (CRC) for chemoprevention studies and to study the molecular mechanisms of colon carcinogenesis. It produces a spectrum of tumors that resemble human sporadic colorectal cancer. |
| Enzyme Assay |
As a DNA alkylating agent, there is no specific enzyme/receptor binding protocol. The mechanism of action involves metabolic activation by cytochrome P450 enzymes (primarily CYP2E1) in the liver to form the reactive methylating species methylazoxymethanol (MAM). This can be studied in vitro using liver microsomes (S9 fraction) incubated with N,N'-Dimethylhydrazine, followed by DNA incubation to detect O6-methylguanine adducts by LC-MS/MS or by 32P-postlabeling. The mutagenic potential can be assessed in the Ames test (Salmonella typhimurium TA100) with metabolic activation (S9).
|
| Cell Assay |
In vitro, N,N'-Dimethylhydrazine is used to study its genotoxic and cytotoxic effects on colon epithelial cell lines (e.g., NCM460, Caco-2). Typically, cells are treated with N,N'-Dimethylhydrazine (1-100 ug/mL) in culture medium for 1-4 hours (exposure times may vary), then washed and allowed to recover for 24-72 hours. DNA damage is measured by Comet assay (single-cell gel electrophoresis), gamma-H2AX foci staining, or micronucleus formation. Cytotoxicity is assessed by MTT or LDH release assays. Cell proliferation and apoptosis are measured by flow cytometry.
|
| Animal Protocol |
Animal/Disease Models: ICR mouse[1]
Doses: 20 mg/kg Route of Administration: sc; once weekly for 24 weeks; sacrificed mouse after between 23 and 33 weeks. Experimental Results: Induced colon cancer in ICR mice. Animal/Disease Models: Male inbred F344 rats[1] Doses: 20 mg, 4 mg/mL dissolved in normal saline containing 1.5% EDTA (pH 6.4 and filter sterilized) Route of Administration: sc; weekly for 20 or 35 weeks Experimental Results: Produced a higher incidence of adenocarci?nomas in the small and large intestines of animals that were consuming the meat diet. The standard animal model for N,N'-Dimethylhydrazine-induced colon cancer is well-established. For mice (e.g., ICR or BALB/c), N,N'-Dimethylhydrazine dihydrochloride is dissolved in saline (pH adjusted to 6.5-7.0 with NaOH) and administered at a dose of 20 mg/kg body weight by subcutaneous injection once weekly for 20-24 weeks. For rats (e.g., Sprague-Dawley or Fischer 344), the dose is typically 20-40 mg/kg once weekly for 10-20 weeks. Animals are maintained on standard chow and monitored weekly. After the induction period (4-6 months), animals are euthanized, colons are removed, opened longitudinally, and tumors are counted and measured. Histopathological analysis confirms adenoma and adenocarcinoma. A 24-week study in ICR mice at 20 mg/kg (s.c., weekly) induces colon tumors. |
| ADME/Pharmacokinetics |
Not applicable. N,N'-Dimethylhydrazine dihydrochloride is a carcinogen, not a therapeutic drug, so no PK parameters relevant to human therapy exist. However, its absorption, distribution, metabolism, and excretion have been studied in rats. After subcutaneous or intraperitoneal administration, it is rapidly absorbed and metabolized in the liver by CYP2E1 to methylazoxymethanol (MAM), which is further metabolized to a reactive methylating species. The half-life in plasma is short. It is primarily excreted in urine as metabolites. Chemically, the compound is water-soluble (e.g., >100 mg/mL). Storage: -20degC, dry, dark, under inert atmosphere.
|
| Toxicity/Toxicokinetics |
N,N'-Dimethylhydrazine dihydrochloride is a potent carcinogen. It is classified as a Group 2A carcinogen (probably carcinogenic to humans) by IARC. In animals, chronic administration causes colon tumors with high incidence. Acute toxicity: LD50 in mice is approximately 100-200 mg/kg (oral/ip). Symptoms of acute poisoning include severe gastrointestinal distress, liver and kidney damage, and central nervous system depression. The compound is a reducing agent and can be explosive in some conditions. It is corrosive to skin and eyes. It is highly toxic by inhalation, ingestion, and skin absorption. It is strictly for research use in animals only; it has no human therapeutic applications. Extreme caution is required; handle in a chemical fume hood with full PPE.
|
| References |
|
| Additional Infomation |
Prismatic crystals (soluble in water) or white crystalline powder. Has a distinct amine-like fishy or ammonia-like odor. (NTP, 1992)
1,2-Dimethylhydrazine dihydrochloride is the hydrochloride formed by the reaction of 1,2-dimethylhydrazine with 2 molar equivalents of hydrogen chloride. It contains 1,2-dimethylhydrazine(2+) ions. 1,2-Dimethylhydrazine dihydrochloride is the chloride of an experimental compound used to induce tumors in animal carcinogenic models. In mice and rats, 1,2-dimethylhydrazine may induce carcinogenesis through cell cycle dysregulation. This substance primarily induces gastrointestinal and vascular tumors. Due to its industrial and agricultural applications, trace amounts of 1,2-dimethylhydrazine may be present in the environment. (NCI04) See also: N,N'-Dimethylhydrazine dichloride (note moved to). This compound is NOT a drug. It is a research chemical used exclusively in laboratory settings to induce colon tumors in rodents for the study of colorectal cancer biology and for testing chemopreventive agents. It is NOT approved for human use and has no therapeutic indications. It is strictly for research use by trained professionals in animal facilities. The compound is a classic colon-specific carcinogen and has been used for decades in carcinogenesis research. It is also known as 1,2-Dimethylhydrazine (SDMH) dihydrochloride. |
| Molecular Formula |
C2H10CL2N2
|
|---|---|
| Molecular Weight |
133.02
|
| Exact Mass |
132.022
|
| CAS # |
306-37-6
|
| PubChem CID |
9380
|
| Appearance |
Solid powder ; White to off-white
|
| Density |
0.759 g/cm3
|
| Boiling Point |
81.5ºC at 760 mmHg
|
| Melting Point |
333 to 336 °F (decomposes) (NTP, 1992)
|
| LogP |
1.726
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
6
|
| Complexity |
6
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CNNC.Cl.Cl
|
| InChi Key |
WLDRFJDGKMTPPV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C2H8N2.2ClH/c1-3-4-2;;/h3-4H,1-2H3;2*1H
|
| Chemical Name |
1,2-dimethylhydrazine;dihydrochloride
|
| Synonyms |
1,2-Dimethylhydrazine dihydrochloride
|
| 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 Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~175 mg/mL (~1315.59 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.5177 mL | 37.5883 mL | 75.1767 mL | |
| 5 mM | 1.5035 mL | 7.5177 mL | 15.0353 mL | |
| 10 mM | 0.7518 mL | 3.7588 mL | 7.5177 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
