Idarubicin's half-life (IC50) in MCF-7 cell monolayers is 3.3 ± 0.4 ng/mL, but in multicellular spheroids, it is 7.9 ± 1.1 ng/mL [1]. In a number of in vitro systems, it was found that idarubicin was more cytotoxic than either daunorubicin or doxorubicin. This is explained by idarubicin's superior capacity to trigger topoisomerase II-mediated DNA break formation [2]. Idarubicin's activity is roughly 25 times higher than that of epirubicin and doxorubicin's, respectively, at 57.5 times [3]. With an IC50 of roughly 0.01 μM, idarubicin inhibits MCF-7 cell proliferation in a concentration-dependent manner. Idarubicin inhibits c-myc expression in a concentration-dependent manner as well as in a time- and concentration-dependent manner [4].

Absorption, Distribution and Excretion
This drug is primarily excreted via bile, with a small amount excreted via the kidneys, mainly as idarubicinol. Biological Half-Life 22 hours

Protein Binding

97%

[1]. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids. J Chemother. 2005 Dec;17(6):663-7.

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

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

[4]. 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-.

[5]. 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.

Idarubicin is a monosaccharide derivative belonging to the anthracycline antibiotics and deoxyhexosides. It is derived from the hydride of tetraphenylethylene. It is an oral anthracycline antitumor drug. This compound has shown activity against breast cancer, lymphoma, and leukemia, and has the potential to reduce cardiotoxicity. Idarubicin is an anthracycline topoisomerase inhibitor. Idarubicin's mechanism of action is as a topoisomerase inhibitor. Idarubicin is a semi-synthetic 4-demethoxy analog of the antitumor anthracycline antibiotic daunorubicin. Idarubicin can intercalate into DNA and interfere with the activity of topoisomerase II, thereby inhibiting DNA replication, RNA transcription, and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more effectively than other anthracycline antibiotic compounds. An oral anthracycline antitumor drug. This compound has shown activity against breast cancer, lymphoma, and leukemia. See also: Idarubicin hydrochloride (salt form). Drug Indications Idarubicin is used to treat acute myeloid leukemia (AML) in adults. This includes drugs classified as M1 to M7 in the French American British Biotechnology (FAB) classification. Mechanism of Action Idarubicin exerts its antimitotic and cytotoxic activity through several proposed mechanisms of action: it forms a complex with DNA by intercalating between base pairs and inhibits the activity of topoisomerase II by stabilizing the DNA-topoisomerase II complex, thereby preventing the rejoining portion of the topoisomerase II-catalyzed ligation-rejoining reaction. Pharmacodynamics Idarubicin is an anthracycline antitumor drug. General characteristics of this class of drugs include interacting with DNA in a variety of different ways, including intercalation (compression between base pairs), DNA strand breaks, and inhibition of topoisomerase II. Most of these compounds are isolated from natural sources and antibiotics. However, anthracyclines lack the specificity of antibacterial antibiotics and therefore produce significant toxicity. Anthracyclines are among the most important antitumor drugs currently available. Doxorubicin is widely used to treat a variety of solid tumors, while daunorubicin and idarubicin are specifically used to treat leukemia. Idarubicin can also inhibit polymerase activity, affect gene expression regulation, and generate free radicals that damage DNA. Idarubicin has antitumor effects against a variety of tumors, including xenografts and spontaneous tumors. Anthracycline drugs do not have cell cycle specificity.

C26H27NO9

497.168

58957-92-9

Idarubicin hydrochloride;57852-57-0

42890

Typically exists as solid at room temperature

1.6±0.1 g/cm3

725.4±60.0 °C at 760 mmHg

392.5±32.9 °C

0.0±2.5 mmHg at 25°C

1.706

2.95

5

10

3

36

912

6

C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C(C4=C(C(=O)C5=CC=CC=C5C4=O)C(=C32)O)O)(C(=O)C)O)N)O

XDXDZDZNSLXDNA-TZNDIEGXSA-N

InChI=1S/C26H27NO9/c1-10-21(29)15(27)7-17(35-10)36-16-9-26(34,11(2)28)8-14-18(16)25(33)20-19(24(14)32)22(30)12-5-3-4-6-13(12)23(20)31/h3-6,10,15-17,21,29,32-34H,7-9,27H2,1-2H3/t10-,15-,16-,17-,21+,26-/m0/s1

(7S,9S)-9-acetyl-7-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-8,10-dihydro-7H-tetracene-5,12-dione

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)