Idarubicin HCl

Catalog No.S1228

Idarubicin 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.

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Idarubicin HCl Chemical Structure

Idarubicin HCl Chemical Structure
Molecular Weight: 533.95

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Idarubicin 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.
Targets Topo II (MCF-7 cells) [1]
(Cell-free assay)
Multicellular spheroids [1]
(Cell-free assay)
IC50 3.3 ng/mL 7.9 ng/mL
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]
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]
Features Idarubicin is a substrate for CYP450 2D6 and 2C9.

Protocol(Only for Reference)

Kinase Assay:

[5]

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 Assay:

[6]

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.

Animal Study:

[7]

Animal Models Rat, rabbit, mouse, dog
Formulation Saline
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Orlandi P, et al. J Chemother. 2005, 17(6), 663-667.

[2] Colburn DE, et al. Hematology. 2004, 9(3), 217-221.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02703272 Not yet recruiting Lymphoma, Non-Hodgkin Janssen Research & Development, LLC October 2016 Phase 3
NCT02527174 Not yet recruiting Leukemia, Myeloid, Acute|Leukemia, Monocytic, Acute|Leukemia, Myelomonocytic, Acute|Leukemia, Erythroblastic, Acute|Leukemia, Megakaryoblastic, Acute University of Alberta June 2016 Phase 1
NCT02652871 Recruiting Leukemia M.D. Anderson Cancer Center|Eli Lilly and Company|High Im  ...more M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program May 2016 Phase 1
NCT02688140 Not yet recruiting Acute Promyelocytic Leukemia Technische Universität Dresden|Gruppo Italiano Malattie E  ...more Technische Universität Dresden|Gruppo Italiano Malattie EMatologiche dellAdulto|Groupe Francophone des Myelodysplasies|Haemato Oncology Foundation for Adults in the Netherlands|Programa para el Tratamiento de Hemopatías Malignas|German Federal Ministry of Education and Research|Teva Pharmaceuticals Europe April 2016 Phase 3
NCT02635074 Not yet recruiting Recurrent Adult Acute Myeloid Leukemia Bruno C. Medeiros|National Cancer Institute (NCI)|Stanfor  ...more Bruno C. Medeiros|National Cancer Institute (NCI)|Stanford University April 2016 Phase 1

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Chemical Information

Download Idarubicin HCl SDF
Molecular Weight (MW) 533.95
Formula

C26H27NO9.HCl

CAS No. 57852-57-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl
Solubility (25°C) * In vitro DMSO 100 mg/mL (187.28 mM)
Water 7 mg/mL warming (13.1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (7S,9S)-9-acetyl-7-((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyl-tetrahydro-2H-pyran-2-yloxy)-6,9,11-trihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride

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