ICRF 192
ICRF 192 is a weak DNA topoisomerase II (DNA topoisomerase II) inhibitor with an IC50 of 91 μM. ICRF 192 forms an iron-chelating derivative via ring-opening hydrolysis, which can displace Fe3+ from the Fe3+-doxorubicin complex. ICRF 192 is used for studies on the structure-activity relationship of bisdioxopiperazines and the cardiotoxicity of anthracycline drugs.
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- CAS No.: 58893-33-7
- Formule: C12H18N4O4
- Masse moléculaire:282.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[3]|
Topoisomerase II 91 μM (IC50) |
In Vitro
IC50 192 exhibits essentially no inhibitory activity against the growth of Chinese hamster ovary (CHO) cells, which is consistent with its weak inhibitory activity against DNA topoisomerase II[1].
ICRF 192 (concentration range; 48 h) inhibits the growth of Chinese hamster ovary (CHO) AA8 cells with an IC50 of 340 μM[3].
ICRF 192 (over a range of concentrations) inhibits the growth of mouse L cells, with an IC50 of 720 μM[3].
ICRF 192 (0-100 μM; 30 min) inhibits the catalytic decatenation activity of DNA topoisomerase II derived from human leukemia K562 cells, with an IC50 of 91 μM[3].
ICRF 192 (20-200 μM; approximately 2-3 h) enters BHK-21S cells via simple diffusion, and the intracellular concentration reaches a level close to that of the extracellular medium[2].
ICRF 192 (100 μM; 24 h) does not undergo significant metabolism in BHK-21S cells, and the radioactivity associated with cellular DNA and RNA originates from incorporation via the one-carbon metabolic pathway, rather than covalent binding of the drug[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SHR, Aoki-Okamoto strain (adult male, 200-250 g, doxorubicin-induced chronic cardiotoxicity and nephrotoxicity model)[1]
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Dosage:50 mg/kg
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Administration:i.p.; once weekly; 12 weeks; 30 minutes prior to doxorubicin
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Result:Caused an average body weight decrease of 13 g in surviving rats.
Did not significantly reduce doxorubicin-induced myocardial lesions.
Among 10 evaluated animals, 1 animal had a myocardial lesion score of 2.0, 4 animals had a score of 2.5 and 5 animals had a score of 3.0.
Did not significantly reduce doxorubicin-induced renal lesions. Among 11 evaluated animals, 1 animal had a renal lesion score of 1, 4 animals had a score of 2 and 6 animals had a score of 3.
Resulted in 6 deaths among 11 animals before study completion.
Chemical Information
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CAS No. 58893-33-7
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Masse moléculaire 282.30
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Formule C12H18N4O4
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SMILES
O=C1NC(CN(CC(CC)N2CC(NC(C2)=O)=O)C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Herman EH, et al. Comparison of the protective effects against chronic doxorubicin cardiotoxicity and the rates of iron (III) displacement reactions of ICRF-187 and other bisdiketopiperazines. Cancer chemotherapy and pharmacology. 1997;40(5):400-408. [Content Brief]
[2]. Dawson KM. Studies on the stability and cellular distribution of dioxopiperazines in cultured BHK-21S cells. Biochem Pharmacol. 1975 Dec 15;24(24):2249-2253. [Content Brief]
[3]. Hasinoff BB, et al. A QSAR study comparing the cytotoxicity and DNA topoisomerase II inhibitory effects of bisdioxopiperazine analogs of ICRF-187 (dexrazoxane). Biochemical pharmacology. 1995 Sep 28;50(7):953-958. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ICRF 192 Related Classifications
HY-183524 Related Classifications
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