Cat. No.: HY-17381A

Idarubicin

(Synonyms: 4-Demethoxydaunorubicin)

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts.

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Pureté: 99.89%
CAS No.: 58957-92-9
Formule: C₂₆H₂₇NO₉
Masse moléculaire:497.49

Stockage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Idarubicin Chemical Structure

CAS No.: 58957-92-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (19)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Topoisomerase II

Voir tous les produits spécifiques à Isoform Topoisomerase :

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis :

Voir tous les produits spécifiques à Isoform Antibiotic :

Cellular Effect

Cell Line	Type	Value	Description	References
DA-3 cell line	IC₅₀	2.3 μM Compound: IDR	Cytotoxicity against mouse DA-3 cells after 24 hrs by XTT assay Cytotoxicity against mouse DA-3 cells after 24 hrs by XTT assay	[PMID: 24900668]
HepG2	IC₅₀	12.3 μM Compound: 92308741	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	6.62 μM Compound: 92308741	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
K562	GI₅₀	3.3 μM Compound: idarubicin	Antiproliferative activity against human K562 cells after 72 hrs Antiproliferative activity against human K562 cells after 72 hrs	[PMID: 25420175]
K562	IC₅₀	0.012 μM Compound: idarubicin	Cytotoxicity against human K562 cells after 5 days by XTT assay Cytotoxicity against human K562 cells after 5 days by XTT assay	[PMID: 18076140]
K562	IC₅₀	0.027 μM Compound: 17	Cytotoxicity against human K562 cells incubated for 2 hrs by cell titre blue viability assay Cytotoxicity against human K562 cells incubated for 2 hrs by cell titre blue viability assay	[PMID: 37561481]
K562	IC₅₀	0.027 μM Compound: 5	Cytotoxicity against human K562 cells incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay Cytotoxicity against human K562 cells incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay	[PMID: 39088428]
K562	IC₅₀	0.041 μM Compound: 5	Cytotoxicity against human K562 cells overexpressing ABCB1 incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay Cytotoxicity against human K562 cells overexpressing ABCB1 incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay	[PMID: 39088428]
K562	IC₅₀	0.116 μM Compound: 5	Cytotoxicity against human K562 cells overexpressing ABCG2 incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay Cytotoxicity against human K562 cells overexpressing ABCG2 incubated for 2 hrs followed by compound washout and measured after 72 hrs by Celltiter-blue viability assay	[PMID: 39088428]
K562	IC₅₀	2 nM Compound: Idarubicin	Cytotoxic activity against K562 erythroleukemic cells Cytotoxic activity against K562 erythroleukemic cells	[PMID: 10425093]
MCF7	IC₅₀	7.3 μM Compound: IDR	Cytotoxicity against human MCF7 cells after 24 hrs by XTT assay Cytotoxicity against human MCF7 cells after 24 hrs by XTT assay	[PMID: 24900668]
MEL-JUSO	IC₅₀	0.089 μM Compound: 17	Cytotoxicity against human MEL-JUSO cells incubated for 2 hrs by cell titre blue viability assay Cytotoxicity against human MEL-JUSO cells incubated for 2 hrs by cell titre blue viability assay	[PMID: 37561481]
SK-OV-3	IC₅₀	4.5 μM Compound: IDR	Cytotoxicity against human SKOV3 cells after 24 hrs by XTT assay Cytotoxicity against human SKOV3 cells after 24 hrs by XTT assay	[PMID: 24900668]
U2OS	IC₅₀	0.024 μM Compound: 17	Cytotoxicity against human U2OS cells incubated for 2 hrs by cell titre blue viability assay Cytotoxicity against human U2OS cells incubated for 2 hrs by cell titre blue viability assay	[PMID: 37561481]

In Vitro

The IC₅₀ of idarubicin is 3.3 ± 0.4 ng/mL on MCF-7 monolayers and 7.9 ± 1.1 ng/mL in multicellular spheroids^[1].
Idarubicin shows a greater cytotoxicity than daunorubicin or doxorubicin in various in vitro systems. This has been attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks^[2].
Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively^[3].
Idarubicin produces a concentration-dependent reduction in MCF-7 cell growth, with an IC₅₀ of approximately 0.01 μM. Idarubicin produces a concentration-dependent inhibition of DNA synthesis and a time- and concentration-dependent suppression of c-myc expression^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 58957-92-9
Appearance Solid
Masse moléculaire 497.49
Formule C₂₆H₂₇NO₉
Color Orange to red
SMILES

OC(C(C(C1=CC=CC=C21)=O)=C3C2=O)=C4[C@H](C[C@@](C(C)=O)(O)CC4=C3O)O[C@@](O[C@@H](C)[C@H]5O)([H])C[C@@H]5N
Synonyms

4-Demethoxydaunorubicin
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (19)

All Cell Proliferation/Viability AssayFlow CytometryWBIn Vivo Efficacy Study

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nat Cell Biol

Trafficking circuit of CD8+ T cells between the intestine and bone marrow governs antitumour immunity. [Abstract]

2024 Aug;26(8):1346-1358. PMID: 39039181

Idarubicin purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Aug;26(8):1346-1358. [Abstract]

Number of total BM cells and GFP⁺ AF9 cells after treatment with 5 mg/kg DOX or 1 mg/kg Idarubicin hydrochloride for 5 days (n = 3 per group).
Nat Commun

Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]

2020 Apr 14;11(1):1792. PMID: 32286289
Nucleic Acids Res

ZYH005, a novel DNA intercalator, overcomes all-trans retinoic acid resistance in acute promyelocytic leukemia. [Abstract]

2018 Apr 20;46(7):3284-3297. PMID: 29554366

Idarubicin purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2018 Apr 20;46(7):3284-3297. [Abstract]

NB4 and NB4-LR2 cells were treated with ZYH005, Arsenic trioxide (ATO), 5-fluorouracil (5-Fu), Cisplatin (DDP), Doxorubicin (DOX) and Idarubicin hydrochloride (IDA) at 0.05 μM for 24 h, and then cell apoptosis was determined.
Sci Adv

Tissue-specific inflammation induces cell state plasticity with oncogenic addiction in mucosal melanoma. [Abstract]

2026 Apr 3;12(14):eady4536. PMID: 41920996
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Cancer Lett

Synthetic lethality of combined AT-101 with idarubicin in acute myeloid leukemia via blockade of DNA repair and activation of intrinsic apoptotic pathway. [Abstract]

2019 Oct 1:461:31-43. PMID: 31301319
Anal Chem

Force-Dependent Intercalative Bulky DNA Adduct Formation Detected by Single-Molecule Stretching. [Abstract]

2022 Oct 4;94(39):13623-13630. PMID: 36129494
Cancer Cell Int

GANT61 surmounts drug resistance of ADR by upregulating lysosome activities and reducing BCL2 expression in HL-60/ADR cells. [Abstract]

2024 Dec 26;24(1):430. PMID: 39726048
Biochem Pharmacol

Deubiquitinase USP5 promotes acute myeloid leukemia through C2CD5 stabilization and PI3K/AKT/mTOR/HIF-1α-driven glycolysis. [Abstract]

2026 Feb:244:117591. PMID: 41344512
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
iScience

RHOF activation of AKT/β-catenin signaling pathway drives acute myeloid leukemia progression and chemotherapy resistance. [Abstract]

2024 Jun 8;27(7):110221. PMID: 39021805

Idarubicin purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jun 8;27(7):110221. [Abstract]

THP-1 and MOLM-13 cells (control for knockdown or shRHOF) were treated with 1.2 μM Ara-C and 0.03 μg/mL Idarubicin hydrochloride for 48 h to measure apoptosis via flow cytometry (n = 3). Student's t tests were used for comparing two variables.

Idarubicin purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jun 8;27(7):110221. [Abstract]

THP-1 and MOLM-13 cells (control for overexpression or RHOF) were treated with 1.2 μM Ara-C and 0.03 μg/mL Idarubicin hydrochloride for 48 h to measure apoptosis via flow cytometry (n = 3). Student's t tests were used for comparing two variables.
J Virol

Cellular DNA Topoisomerases Are Required for the Synthesis of Hepatitis B Virus Covalently Closed Circular DNA. [Abstract]

2019 May 15;93(11):e02230-18. PMID: 30867306

Idarubicin purchased from MedChemExpress. Usage Cited in: J Virol. 2019 May 15;93(11):e02230-18. [Abstract]

Idarubicin hydrochloride reduced HBV cccDNA levels in a dose-dependent manner, but had no effect on core DNA and DP-rcDNA levels.
Viruses

Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]

2020 Jun 10;12(6):628. PMID: 32532085
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Mol Carcinog

circSLC25A13 acts as a ceRNA to regulate AML progression via miR-616-3p/ADCY2 axis. [Abstract]

2023 Oct;62(10):1546-1562. PMID: 37493101
Hematology

XPO1 inhibitor selinexor suppresses homologous recombination by inhibiting E2F7 nuclear export in acute myeloid leukemia. [Abstract]

2026 Dec 31;31(1):2664314. PMID: 42026967
bioRxiv

2023 Jan 13.
University of Paris

2022 Sep 19.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (201.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0101 mL

10.0505 mL

20.1009 mL

5 mM

0.4020 mL

2.0101 mL

4.0202 mL

10 mM

0.2010 mL

1.0050 mL

2.0101 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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+
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Tween-80 + +
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Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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Références

[1]. Orlandi P, et al. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids. J Chemother. 2005 Dec;17(6):663-7. [Content Brief]

[2]. Robert J. Clinical pharmacokinetics of idarubicin. Clin Pharmacokinet. 1993 Apr;24(4):275-88. [Content Brief]

[3]. Siegsmund MJ, et al. Enhanced in vitro cytotoxicity of idarubicin compared to epirubicin and doxorubicin in rat prostate carcinoma cells. Eur Urol. 1997;31(3):365-70. [Content Brief]

[4]. Gewirtz DA, et al. Induction of DNA damage, inhibition of DNA synthesis and suppression of c-myc expression by the anthracycline analog, idarubicin (4-demethoxy-daunorubicin) in the MCF-7 breast tumor cell line. Cancer Chemother Pharmacol. 1998;41(5):361- [Content Brief]

[5]. Kinnunen U, et al. Idarubicin inhibits the growth of bacteria and yeasts in an automated blood culture system. Eur J Clin Microbiol Infect Dis. 2009 Mar;28(3):301-3. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0101 mL	10.0505 mL	20.1009 mL	50.2523 mL
	5 mM	0.4020 mL	2.0101 mL	4.0202 mL	10.0505 mL
	10 mM	0.2010 mL	1.0050 mL	2.0101 mL	5.0252 mL
	15 mM	0.1340 mL	0.6700 mL	1.3401 mL	3.3502 mL
	20 mM	0.1005 mL	0.5025 mL	1.0050 mL	2.5126 mL
	25 mM	0.0804 mL	0.4020 mL	0.8040 mL	2.0101 mL
	30 mM	0.0670 mL	0.3350 mL	0.6700 mL	1.6751 mL
	40 mM	0.0503 mL	0.2513 mL	0.5025 mL	1.2563 mL
	50 mM	0.0402 mL	0.2010 mL	0.4020 mL	1.0050 mL
	60 mM	0.0335 mL	0.1675 mL	0.3350 mL	0.8375 mL
	80 mM	0.0251 mL	0.1256 mL	0.2513 mL	0.6282 mL
	100 mM	0.0201 mL	0.1005 mL	0.2010 mL	0.5025 mL

Keywords

Idarubicin

19 Cited Publications

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Idarubicin

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Publications Citing Use of MedChemExpress (MCE) Idarubicin

Voir tous les produits spécifiques à Isoform Topoisomerase

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Voir tous les produits spécifiques à Isoform Antibiotic

Activité biologique

Chemical Information

Publications (19)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Idarubicin Related Classifications

HY-17381A Related Classifications