Idarubicin prevents DNA from unwinding by interfering with the enzyme topoisomerase II. Idarubicin belongs to the family called antitumor antibiotics. Idarubicin inhibits the proliferation of NALM-6 cells with an IC50 of 12 nM. Idarubicin has significant cytotoxic activity against multicellular spheroids, comparable to the antiproliferative effects on monolayer cells. Idarubicin is currently combined with cytosine arabinoside as a first line treatment of acute myeloid leukemia. Idarubicin plus Decitabine and cytarabine has entered in a phase II clinical trial in the treatment of adult acute myeloid leukemia, and adult acute monoblastic leukemia, refractory anemia with excess blasts.
|Cell lines||K562S and K562R cells|
|Preparation method||MTT assay
K562S and K562R cells were cultured in a 96-well plate (SPL) at a density of 1 × 104 cells in 100 μL of medium per well and treated with the indicated concentration of Imatinib or the AGM130 compound for 72 h. To measure the cell viability, the EZ-Cytox Cell Viability Assay kit was used. Ten microliters of MTT reagent was evenly treated in each well and incubated at 37 ◦C and 5% CO2 for 6 h. At the end of the incubation, the MTT factors of incubated cells in the plate were measured at the 450 nm wavelength using an ELISA detector.
|Incubation time||72 h|
|Animal models||Imatinibresistant K562 cells xenograft model using BALB/c nude mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
5'-OH-5-nitro-Indirubin oxime (AGM130), an Indirubin derivative, induces apoptosis of Imatinib-resistant chronic myeloid leukemia cells.
Kim WS, et al. Leuk Res. 2013 Apr;37(4):427-33. PMID: 23337400.
Prognostic significance of alterations in IDH enzyme isoforms in patients with AML treated with high-dose cytarabine and idarubicin.
Ravandi F, et al. Cancer. 2012 May 15;118(10):2665-73. PMID: 22020636.
Phase 2 randomized study of p53 antisense oligonucleotide (cenersen) plus idarubicin with or without cytarabine in refractory and relapsed acute myeloid leukemia.
Cortes J, et al. Cancer. 2012 Jan 15;118(2):418-27. PMID: 21717444.
Daunorubicin versus mitoxantrone versus idarubicin as induction and consolidation chemotherapy for adults with acute myeloid leukemia: the EORTC and GIMEMA Groups Study AML-10.
Mandelli F, et al. J Clin Oncol. 2009 Nov 10;27(32):5397-403. PMID: 19826132.
Stereoselectivity of idarubicin reduction in various animal species and humans.
Strolin Benedetti M, et al. Xenobiotica. 1991 Apr;21(4):473-80. PMID: 1897247.
|Related Topoisomerase Products|
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
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