Imexon
Based on 1 publication(s) in Google Scholar
Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 98.12%
- CAS No.: 59643-91-3
- Formula: C4H5N3O
- Molecular Weight:111.10
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Imexon
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
324 μM
Compound: imexon
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Inhibition of cell growth in (A375) melan cell line
Inhibition of cell growth in (A375) melan cell line
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[PMID: 9986721] |
| A549 | IC50 |
>72 μM
Compound: imexon
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Inhibition of cell growth in (A-549) lung cell line
Inhibition of cell growth in (A-549) lung cell line
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[PMID: 9986721] |
| L1210 | IC50 |
477 μM
Compound: imexon
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Inhibition of cell growth in (L1210 leukemia) MDR cells determined by MTT assay
Inhibition of cell growth in (L1210 leukemia) MDR cells determined by MTT assay
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[PMID: 9986721] |
| L1210 | IC50 |
612 μM
Compound: imexon
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Inhibition of cell growth in drug sensitive L1210 leukemia cell line determined by MTT assay
Inhibition of cell growth in drug sensitive L1210 leukemia cell line determined by MTT assay
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[PMID: 9986721] |
| MCF7 | IC50 |
>18 μM
Compound: imexon
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Inhibition of cell growth in (MCF7 breast) dox cell line
Inhibition of cell growth in (MCF7 breast) dox cell line
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[PMID: 9986721] |
| MCF7 | IC50 |
>18 μM
Compound: imexon
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Inhibition of cell growth in (MCF7 breast) mitox cell line
Inhibition of cell growth in (MCF7 breast) mitox cell line
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[PMID: 9986721] |
| MCF7 | IC50 |
>18 μM
Compound: imexon
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Inhibition of cell growth in drug sensitive MCF-7 breast cell line
Inhibition of cell growth in drug sensitive MCF-7 breast cell line
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[PMID: 9986721] |
| OVCAR-3 | IC50 |
640 μM
Compound: imexon
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Inhibition of cell growth in (OVCAR-3) ovarian cell line
Inhibition of cell growth in (OVCAR-3) ovarian cell line
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[PMID: 9986721] |
| RPMI-8226 | IC50 |
115 μM
Compound: imexon
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Inhibition of cell growth in drug resistant 8226 myeloma cell line
Inhibition of cell growth in drug resistant 8226 myeloma cell line
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[PMID: 9986721] |
| RPMI-8226 | IC50 |
17 μM
Compound: imexon
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Inhibition of cell growth in drug sensitive 8226 myeloma cell line
Inhibition of cell growth in drug sensitive 8226 myeloma cell line
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[PMID: 9986721] |
| WiDr | IC50 |
>72 μM
Compound: imexon
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Inhibition of cell growth in drug resistant WiDr colon cell line
Inhibition of cell growth in drug resistant WiDr colon cell line
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[PMID: 9986721] |
| WiDr | IC50 |
>72 μM
Compound: imexon
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Inhibition of cell growth in drug sensitive WiDr colon cell line
Inhibition of cell growth in drug sensitive WiDr colon cell line
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[PMID: 9986721] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 59643-91-3
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Appearance Solid
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Molecular Weight 111.10
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Formula C4H5N3O
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Color White to off-white
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SMILES
O=C1N2CC2C(N)=N1
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Synonyms
BM 06002
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Roman NO, et al. Imexon enhances gemcitabine cytotoxicity by inhibition of ribonucleotide reductase. Cancer Chemother Pharmacol. 2011 Jan;67(1):183-92. [Content Brief]
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.
Imexon Related Classifications
HY-15385 Related Classifications
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