Idarubicin hydrochloride

SKU: orb1301162

Description

Idarubicin hydrochloride, sold as Zavedos, is the hydrochloride salt form of the anthracycline Idarubicin. It functions as a DNA topoisomerase II inhibitor, exhibiting potent activity against MCF-7 breast cancer cells with an IC50 of 3.3 ng/mL. This compound is widely used in cancer research for in vitro cytotoxicity studies and in vivo models of leukemia and solid tumors.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57852-57-0
• MW: 533.95
• Purity: 98.91% (May vary between batches)
• Formula: C₂₆H₂₇NO₉·HCl
• SMILES: Cl.C[C@@H]1O[C@H](C[C@H](N)[C@@H]1O)O[C@H]1C[C@@](O)(Cc2c(O)c3C(=O)c4ccccc4C(=O)c3c(O)c12)C(C)=O
• Target: DNA/RNA Synthesis,Topoisomerase,c-Myc,Antifungal,Antibacterial,Antibiotic,Autophagy
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:255 mg/mL (477.57 mM);H2O:5 mg/mL (9.36 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.18 mM)

Bioactivity

• Target IC50:
  Topo II (MCF-7 cells):3.3 ng/mL
• In Vivo:
  Reduction of Idarubicin is dependent upon ketone reductases, and proceeds more stereoselectively than that of most ketones giving rise to the (13S)-epimer almost exclusively. The high stereospecificity in Idarubicin reduction might result from chiral induction due to the presence of asymmetric centres near to the carbonyl group in Idarubicin.
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• In Vitro:
  Idarubicin has significant cytotoxic activity against multicellular spheroids, comparable to the antiproliferative effects on monolayer cells. Idarubicin inhibits CYP450 2D6. Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively. Idarubicin is able to overcome P-glycoprotein-mediated multidrug resistance. Idarubicin inhibits PMN superoxide radical formation. Idarubicin could be coupled to the monoclonal antibodies (anti-Ly-2.1, anti-L3T4, or anti-Thy-1) with retention of protein solubility and antibody activity. Idarubicin inhibits the proliferation of NALM-6 cells with an IC50 of 12 nM.
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• Cell Research:
  The anti-proliferative activity of the Idarubicin in the conjugate is compared to that of free drug by measuring the inhibition of [3H]thymidine uptake. Briefly, NALM-6 cells (1.5 × 106/mL) are added to a flat-bottomed microtitre plate (100 μL/well) and incubated for 1 hours at 37ºC. Free Idarubicin and Idarubicin-mAb conjugates are sterilised by filtration and diluted in sterile PBS; various concentrations are added to the wells (100 μL/well) in duplicate and the plates are incubated at 37ºC, 7% CO2 for 24 hours. Following incubation, 50 μL medium containing 1 μCi [3H]thymidine is added to each well and the plates are incubated for a further 4 hours. Cells are harvested onto glass-fibre filter-paper, dried and counted in a scintillation counter. Specificity studies are performed using the same technique where the ability of Idarubicin-anti-CD19 conjugates to kill CD19 + cells is compared to the cytotoxicity of irrelevant Idarubicin-JGT conjugates. NALM-6 cells (1.5× 106/mL, 300 μL tube) are incubated for 30 rain on ice with various concentrations of Idarubicin-anti-CD 19 or Idarubicin-JGT conjugates. Following three washes in ice-cold RPMI-1640 medium (4 mL/wash), the cells are resuspended in fresh medium and transferred to 96-well plates (100 μL/well). Each tube is set up in duplicate and two wells are plated out per tube (a total of 4 wells per drug concentration). Cells are pulsed with [3H]thymidine 24 hours later and harvested. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Topoisomerase, Topo II (MCF-7 cells), Zavedos, Bacterial, Antibiotic, Autophagy, 4-Demethoxydaunorubicin, 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl, 4-Demethoxydaunorubicin hydrochloride, 4-Demethoxydaunorubicin Hydrochloride, c-Myc, breast tumor, DNA/RNA Synthesis, DNA synthesis, inhibit, Myc, Fungal, Idamycin, Idarubicin, Idarubicin HCl, Idarubicin Hydrochloride, Idarubicin hydrochloride, Inhibitor, leukaemias, MCF-7

Compound Identifiers

PubChem CID

636362