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Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.

For research use only. We do not sell to patients.

Imexon Chemical Structure

Imexon Chemical Structure

CAS No. : 59643-91-3

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Based on 1 publication(s) in Google Scholar

Imexon Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Imexon

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.

In Vitro

Imexon (BM 06002) induces oxidative stress in the ER, activates an ER stress response. Imexon (BM 06002) does not significantly alter the levels of eIF2B5, however there is a dose-dependent increase in the phosphorylation of eIF2alpha, as well as an increase in the levels of GTP exchange protein eIF2B2 in MiaPaCa-2, Panc-1, and BxPC3 cells[1]. Imexon (BM 06002) induces single-stranded breaks in the human A375 melanoma cells but only significantly at the highest concentrations for each agent compared to controls. Imexon plus DTIC cytotoxicity is additive[2]. Imexon (BM 06002) show inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, with IC50s of 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Imexon Related Antibodies
In Vivo

Imexon (BM 06002) in combination with DTIC results in an increase in the peak plasma imexon level in non-tumor-bearing mice. The combination of both drugs increases plasma imexon AUC by 22% (p=0.026). Imexon (BM 06002) (100 mg/kg/day, i.v.) treatment decreases the body weight of SCID mice bearing human A375 melanoma tumors, but there is no significant difference in tumor growth[2]. Imexon (BM 06002) (100 mg/kg) in combination with GEM shows synergistic inhibition of Panc-1 tumor growth in SCID mice.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

111.10

Formula

C4H5N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N2CC2C(N)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (562.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 12.5 mg/mL (112.51 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.79%

COA (252 KB) HNMR (227 KB) RP-HPLC (89 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Cell survival for the siRNA screening experiments are calculated by the conversion of resazurin to resorufin by metabolically active cells resulting in a fluorescent product. Confirmatory growth inhibition assays with eIF2b silencing are done using the methyl-thiazolyl-diphenyl-tetrazolium bromide (MTT) assay. Cell growth inhibition data are expressed as percent survival, compared to untreated cells. The IC50 is defined as the drug concentration required to produce 50% growth inhibition.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

The effect of the combination on tumor growth in vivo is evaluated in 25-30 g male SCID mice (n=8/group). Mice receive 5×106 A375 cells subcutaneously and are pair matched on day 30, when the average tumor burden is approximately 100 mm3. Treatment begins the following day, as follows: (i) saline vehicle control; (ii) 80 mg/kg/day DTIC; (iii) 100 mg/kg/day imexon; (iv) a combination of both drugs at the same doses. Drugs are administered (i.p.) for nine consecutive days and imexon is administered 15 min before DTIC when combined. Measurement of tumor burden and body weights are made every 3-4 days. Tumor burden (mm3) is calculated as (length × width2)/2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 9.0009 mL 45.0045 mL 90.0090 mL 225.0225 mL
5 mM 1.8002 mL 9.0009 mL 18.0018 mL 45.0045 mL
10 mM 0.9001 mL 4.5005 mL 9.0009 mL 22.5023 mL
15 mM 0.6001 mL 3.0003 mL 6.0006 mL 15.0015 mL
20 mM 0.4500 mL 2.2502 mL 4.5005 mL 11.2511 mL
25 mM 0.3600 mL 1.8002 mL 3.6004 mL 9.0009 mL
30 mM 0.3000 mL 1.5002 mL 3.0003 mL 7.5008 mL
40 mM 0.2250 mL 1.1251 mL 2.2502 mL 5.6256 mL
50 mM 0.1800 mL 0.9001 mL 1.8002 mL 4.5005 mL
60 mM 0.1500 mL 0.7501 mL 1.5002 mL 3.7504 mL
80 mM 0.1125 mL 0.5626 mL 1.1251 mL 2.8128 mL
100 mM 0.0900 mL 0.4500 mL 0.9001 mL 2.2502 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Imexon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Imexon59643-91-3BM 06002BM06002BM-06002OthersInhibitorinhibitorinhibit

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