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Imexon

Catalog No. T15566   CAS 59643-91-3
Synonyms: BM 06002

Imexon is an iminopyrrolidone aziridine. It has anti-cancer activity.

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Imexon Chemical Structure
Imexon, CAS 59643-91-3
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 2,120.00
50 mg 8-10 weeks $ 2,780.00
100 mg 8-10 weeks $ 3,700.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Imexon is an iminopyrrolidone aziridine. It has anti-cancer activity.
In vitro Imexon induces single-stranded breaks in the human A375 melanoma cells but only obviously at the highest concentrations for each agent compared to controls. Imexon causes oxidative stress in the ER, activates an ER stress response. Imexon does not obviously 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 plus DTIC cytotoxicity is additive[2]. Imexon display inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, (IC50s: 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM).[3].
In vivo When administered at 100 mg/kg, Imexon demonstrates enhanced efficacy in suppressing Panc-1 tumor growth in SCID mice when used alongside GEM, evidencing a synergistic effect. Concurrently, pairing Imexon with DTIC elevates peak plasma levels of Imexon in mice without tumors. This drug duo also augments the plasma Imexon area under the curve (AUC) by 22% (p=0.026). Despite this, a regimen of Imexon (100 mg/kg/day, intravenously) leads to weight loss in SCID mice carrying human A375 melanoma tumors, without significantly impacting tumor progression[2].
Synonyms BM 06002
Molecular Weight 111.1
Formula C4H5N3O
CAS No. 59643-91-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

Imexon 59643-91-3 Others BM 06002 BM06002 BM-06002 inhibitor inhibit

 

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