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Idarubicin HCl

Synonyms: 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl

Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.

Idarubicin HCl Chemical Structure

Idarubicin HCl Chemical Structure

CAS No. 57852-57-0

Purity & Quality Control

Idarubicin HCl Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562 erythroleukemic cells Cytotoxic assay Cytotoxic activity against K562 erythroleukemic cells, IC50=0.002 μM 10425093
K562 cells Cytotoxic assay 5 days Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=0.012 μM 18076140
mouse DA-3 cells Cytotoxic assay 24 h Cytotoxicity against mouse DA-3 cells after 24 hrs by XTT assay, IC50=2.3 μM 24900668
human ES2 cells Cytotoxic assay 24 h Cytotoxicity against human ES2 cells after 24 hrs by XTT assay, IC50=3.2 μM 24900668
human K562 cells Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs, GI50=3.3 μM 25420175
human SKOV3 cells Cytotoxic assay 24 h Cytotoxicity against human SKOV3 cells after 24 hrs by XTT assay, IC50=4.5 μM 24900668
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=6.62 μM 22586124
human MCF7 cells Cytotoxic assay 24 h Cytotoxicity against human MCF7 cells after 24 hrs by XTT assay, IC50=7.3 μM 24900668
mouse DA-3 cells Cytotoxic assay 20 μM Cytotoxicity against mouse DA-3 cells assessed as reduction in cell viability at 20 uM by XTT assay 24900668
neural precursor cells Function assay Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 17417631
VERO-E6 Function assay 48 hrs Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=0.2μM ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.
Features Idarubicin is a substrate for CYP450 2D6 and 2C9.
Targets
Topo II (MCF-7 cells) [1]
(Cell-free assay)		 Multicellular spheroids [1]
(Cell-free assay)
3.3 ng/mL 7.9 ng/mL
In vitro
In vitro

Idarubicin has significant cytotoxic activity against multicellular spheroids, comparable to the antiproliferative effects on monolayer cells. [1] Idarubicin inhibits CYP450 2D6.[2] 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. [3] Idarubicin inhibits PMN superoxide radical formation. [4] 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. [5] Idarubicin inhibits the proliferation of NALM-6 cells with an IC50 of 12 nM. [6]
Kinase Assay CYP450 metabolism experiments
Evaluation of Idarubicin metabolism by the CYP450 isoenzymes 3A4, 2D6, 2C8, 2C9, and 1A2 is completed using isolated human CYP450 proteins for each isoform. The high throughput P450 inhibition testing method is utilized for these evaluations. The metabolism experiments are designed to investigate the following properties of each drug: (1) if Idarubicin is a substrate of the CYP450 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes; (2) if metabolism is affected by known inhibitors of each isoenzyme; (3) if Idarubicin is inhibitors of CYP450 isoenzymes; and (4) if caspofungin or itraconazole inhibit the CYP450 metabolism of Idarubicin. Dibenzylfluorescein (DBF) (CYP3A4, CYP2C8, CYP2C9), 3-cyano-7-ethoxycoumarin (Cyp1A2), and 7-methoxy-4-(aminomethyl)-coumarin (MAMC) (CYP2D6) are the known substrates utilized as controls to confirm the respective isoenzyme activity and evaluate the effects of Idarubicin on the isoenzyme activity. In addition, ketoconazole, quercetin, suflaphenazole, furafylline, and quinidine are utilized as control CYP450 inhibitors for 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes, respectively. The substrate, inhibitor plus Idarubicin as indicated are added to each protein sample are incubated for 20 minutes- 60 minutes, as recommend by manufacturer, at 37oC. Reactions are stopped with an organic solvent solution and then samples are analyzed by fluorescence plate reader as appropriate. For each experiment, control samples with a known amount of substrate and synthesized metabolite, in the absence of the isoenzyme, are prepared for qualitative comparisons. All experiments are performed in triplicate.
Cell Research Cell lines NALM-6 cells
Concentrations 0.1 nM-10 μM
Incubation Time 24 hours
Method

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.
In Vivo
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. [7]
Animal Research Animal Models Rat, rabbit, mouse, dog
Dosages 2 mg/kg, 0 mg/kg -75 mg/kg, 3 mg/kg and 0 mg/kg -75 mg/kg
Administration Administered via i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05697510 Recruiting
Acute Myeloid Leukemia (AML)
Nantes University Hospital
 March 16 2023 Phase 1
NCT02652871 Completed
Leukemia
M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program
 May 9 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 533.95 Formula

C26H27NO9.HCl
CAS No. 57852-57-0 SDF Download Idarubicin HCl SDF
Smiles CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=CC=CC=C5C4=O)O)(C(=O)C)O)N)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (187.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 8 mg/mL

Ethanol : Insoluble


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