| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Imexon's mechanism of action involves the generation of reactive oxygen species (ROS) and the induction of apoptosis in cancer cells. It induces oxidative stress in the endoplasmic reticulum (ER), activating an ER stress response. This leads to the activation of caspases (caspase-3, caspase-9, and/or caspase-8) and the induction of apoptosis. Imexon is an apoptosis inducer agent.
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| ln Vitro |
The endoplasmic reticulum experiences oxidative stress due to Imexon (BM 06002), which also triggers the endoplasmic reticulum stress response. In MiaPaCa-2, Panc-1, and BxPC3 cells, imexon (BM 06002) enhances phosphorylation of eIF2α in a dose-dependent manner, but does not significantly change eIF2B5 levels [1]. In human A375 melanoma cells, imexon (BM 06002) caused single-strand breaks; however, this effect was only noticeable at the maximum dosage of each medication in comparison to the control. The cytotoxicity of Imexon plus DTIC is additive [2]. MiaPaCa-2, Panc-1, and BxPC3 are all inhibited by Imexon (BM 06002), with IC50 values of 275.5 ± 54.2, 147.4 ± 4.7, and 355.7 ± 114.7 μM, respectively [3].
In vitro, Imexon induces oxidative stress in the ER and activates an ER stress response. It induces apoptosis in cancer cells through the activation of caspases. The compound has shown antitumor activity in various cancer cell lines. Specific in vitro data, including IC50 values against different cell lines, are not extensively provided in the available literature. |
| ln Vivo |
In mice without tumors, Imexon (BM 06002) coupled with DTIC raises Imexon's peak plasma levels. When the two medications were taken together, Imec's plasma AUC rose by 22% (p=0.026). Imexon (BM 06002), administered intravenously at a dose of 100 mg/kg/day, decreased the body weight of SCID mice harboring human A375 melanoma tumors, but tumor development remained unaffected [2]. When coupled with GEM, Imexon (BM 06002) (100 mg/kg) significantly reduces the formation of Panc-1 tumors in SCID mice.
Imexon has been studied for its antitumor activity in vivo. It has shown activity in various types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. The compound was developed by AmpliMed Corp. in the United States and was investigated in clinical trials. Specific in vivo efficacy data, including dosing regimens and clinical trial results, are not extensively provided. |
| Enzyme Assay |
In vitro enzyme assays for Imexon are not standardly performed as the compound acts through the generation of ROS and induction of ER stress. Its effects can be assessed by measuring ROS levels using fluorescent probes. ER stress markers (e.g., BiP, CHOP, XBP1) can be measured by Western blot or qRT-PCR. Apoptosis can be assessed by measuring caspase activity or by Annexin V staining.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines are cultured and treated with Imexon at various concentrations. ROS levels are measured using fluorescent probes. ER stress markers are measured by Western blot or qRT-PCR. Apoptosis is measured by Annexin V/PI staining, caspase activity assays, or by assessing PARP cleavage. Cell viability and proliferation are assessed using MTT or similar assays.
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| Animal Protocol |
In vivo animal studies for Imexon would typically use tumor xenograft models in immunodeficient mice. Cancer cells are implanted subcutaneously, and tumors are allowed to establish. Imexon is administered intraperitoneally or intravenously at doses determined from pharmacokinetic studies. Tumor volume is measured twice weekly. Apoptosis and ER stress markers are assessed in tumor tissues by immunohistochemistry and Western blot.
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| ADME/Pharmacokinetics |
Imexon has a molecular formula of C4H5N3O and a molecular weight of 111.10. It is a 2-cyanoaziridine derivative. Detailed pharmacokinetic parameters (absorption, distribution, metabolism, excretion, half-life) are not extensively characterized in the available literature. The compound has been studied in clinical trials for cancer.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Imexon are not extensively provided in the available literature. As an inducer of oxidative stress and apoptosis, it would be expected to have a safety profile related to these mechanisms. The compound has been studied in clinical trials for cancer. Standard toxicology assessments would be required for therapeutic development.
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| References |
[1]. Sheveleva EV, et al. Imexon induces an oxidative endoplasmic reticulum stress response in pancreatic cancer cells. Mol Cancer Res. 2012 Mar;10(3):392-400.
[2]. Samulitis BK, et al. Interaction of dacarbazine and imexon, in vitro and in vivo, in human A375 melanoma cells. Anticancer Res. 2011 Sep;31(9):2781-5. [3]. Roman NO, et al. Imexon enhances gemcitabine cytotoxicity by inhibition of ribonucleotide reductase. Cancer Chemother Pharmacol. 2011 Jan;67(1):183-92 |
| Additional Infomation |
Imexon (BM 06002) is a synthetic small molecule that has been studied for its potential therapeutic applications in cancer. It is a 2-cyanoaziridine derivative with antitumor activity in various types of cancer. Imexon induces oxidative stress in the ER and activates an ER stress response, leading to apoptosis. The compound was developed by AmpliMed Corp. and investigated in clinical trials. No approved therapeutic status is reported.
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| Molecular Formula |
C4H5N3O
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| Molecular Weight |
111.1
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| Exact Mass |
111.043
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| CAS # |
59643-91-3
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| PubChem CID |
68791
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| Appearance |
White to off-white solid powder
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| Density |
2.26g/cm3
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| Boiling Point |
231.6ºC at 760 mmHg
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| Index of Refraction |
2.069
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| LogP |
-1.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
8
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| Complexity |
186
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N12C(C1)C(N)=NC2=O
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| InChi Key |
BIXBBIPTYBJTRY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H5N3O/c5-3-2-1-7(2)4(8)6-3/h2H,1H2,(H2,5,6,8)
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| Chemical Name |
4-amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one
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| Synonyms |
BM06002; BM-06002; BM 06002
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~62.5 mg/mL (~562.56 mM)
H2O : ~12.5 mg/mL (~112.51 mM) |
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| 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 | 9.0009 mL | 45.0045 mL | 90.0090 mL | |
| 5 mM | 1.8002 mL | 9.0009 mL | 18.0018 mL | |
| 10 mM | 0.9001 mL | 4.5005 mL | 9.0009 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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