Idarubicin (Synonyms: 4-Demethoxydaunorubicin)

Name: Idarubicin
Brand: MedChemExpress
SKU: HY-17381A
Rating: 5.0 (17 reviews)

Cat. No.: HY-17381A Purity: 99.89%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 58957-92-9

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Idarubicin:

Idarubicin hydrochloride In-stock

17 Publications Citing Use of MCE Idarubicin

Cell Proliferation/Viability Assay

Flow Cytometry

In Vivo Efficacy Study

: 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).

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

: 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.

: 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Topoisomerase II

Cellular Effect

Cell Line	Type	Value	Description	References
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.

Clinical Trial

Molecular Weight

497.49

Formula

C₂₆H₂₇NO₉

CAS No.

58957-92-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (255 KB) HNMR (278 KB) RP-HPLC (220 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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

Idarubicin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Idarubicin58957-92-94-DemethoxydaunorubicinTopoisomeraseBacterialFungalAutophagyc-MycDNA/RNA SynthesisAntibioticMycleukaemiasMCF-7breast tumorDNA synthesisInhibitorinhibitorinhibit

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Idarubicin (Synonyms: 4-Demethoxydaunorubicin)

Customer Review

Other Forms of Idarubicin:

Idarubicin Related Antibodies

17 Publications Citing Use of MCE Idarubicin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Topoisomerase Isoform Specific Products:

View All DNA/RNA Synthesis Isoform Specific Products:

View All Antibiotic Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Idarubicin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Idarubicin Related Classifications

Keywords:

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