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Product Citations(1)

J Phys Chem B, 2013, ahead of print

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Idarubicin HCl is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Chemotherapeutic Agent Library (96-well) FDA Approved Drug Library (96-well)

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Cat.No.	Product Name	Solubility (25°C)
S1208	Doxorubicin (Adriamycin)	20 mg/mL	109 mg/mL	<1 mg/mL
S1225	Etoposide (VP-16)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1231	Topotecan HCl	92 mg/mL	92 mg/mL	<1 mg/mL
S1288	Camptothecin	<1 mg/mL	3 mg/mL	<1 mg/mL
S1198	Irinotecan	<1 mg/mL	10 mg/mL	<1 mg/mL
S1223	Epirubicin HCl	116 mg/mL	116 mg/mL	3 mg/mL
S2217	Irinotecan HCl Trihydrate (Campto)	2 mg/mL	135 mg/mL	7 mg/mL
S1228	Idarubicin HCl	10 mg/mL	107 mg/mL	<1 mg/mL
S1465	Moxifloxacin HCl	<1 mg/mL	88 mg/mL	<1 mg/mL
S1367	Amonafide	<1 mg/mL	57 mg/mL	4 mg/mL
S1393	Pirarubicin	<1 mg/mL	126 mg/mL	<1 mg/mL
S1327	Ellagic acid	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1342	Genistein	<1 mg/mL	54 mg/mL	2 mg/mL
S1463	Ofloxacin (Floxin)	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1889	Mitoxantrone	89 mg/mL	89 mg/mL	<1 mg/mL
S3181	Flumequine	<1 mg/mL	3 mg/mL	<1 mg/mL
S4119	Pefloxacin Mesylate Dihydrate	67 mg/mL	9 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Product Citations Tech Support & FAQs

Biological Activity

Description	Idarubicin HCl (Idamycin, Zavedos, 4-demethoxydaunorubicin) 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.
Targets	Topo II (MCF-7 cells)	Multicellular spheroids
IC50	3.3 ng/mL	7.9 ng/mL ^[1]
In vitro	Idarubicin has significant cytotoxic activity against multicellular spheroids, comparable to the antiproliferative effects on monolayer cells. ^[1] Idarubicin inhibits CYP450 2D6. Idarubicin is much more effective than doxorubicin or epirubicin. ^[2] Idarubicin is about 57.5-fold and 25-fold more active, 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]
Clinical Trials	Idarubicin plus Decitabine and cytarabine has entered in a phase II clinical trial in the treatment of adult acute myeloid leukemia, and adult acute monoblastic leukemia, refractory anemia with excess blasts.
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.

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.

1

References

Chemical Information

Download Idarubicin HCl SDF

Molecular Weight (MW)	533.95
Formula	C₂₆H₂₇NO₉.HCl
CAS No.	57852-57-0
Synonyms	Idamycin, Zavedos, 4-demethoxydaunorubicin

Solubility (25°C) DMSO 107 mg/mL Water 10 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

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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Research Area

Product Citations (1)

Structure-Dependent Complexation of Fe3+ by Anthracyclines. 2. The Roles of Methoxy and Daunosamine Functionalities. [Nawara K, et al. J Phys Chem B 2013;ahead of print]
PubMed: 23692121

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Amonafide
Amonafide (NSC-308847) is a selective topoisomerase II inhibitor.
SN-38
SN-38 is an active metabolite of CPT-11 that inhibits DNA topoisomerase I.
ABT-888 (Veliparib)

ABT-888 (Veliparib, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM, respectively.
Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.
Iniparib (BSI-201)

BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor.
KU-55933

KU-55933 is a potent and specific ATM inhibitor with IC50 and K_i of 13 nM and 2.2 nM, respectively.
Rucaparib (AG-014699 , PF-01367338)

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM.
INO-1001
INO-1001 is a potent inhibitor of PARP with IC50 of 50 nM and a mediator of oxidant-induced myocyte dysfunction during reperfusion.
BIBR 1532
BIBR 1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM.

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Idarubicin HCl

Validation & Quality Control

Product Citations(1)

Quality Control & MSDS

Related Compound Libraries

Idarubicin HCl is available in the following compound libraries:

Product Information

Compare Topoisomerase Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: ^[5]

Cell Assay: ^[6]

Animal Study: ^[7]

References

Chemical Information

Research Area

Product Citations (1)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related Topoisomerase Inhibitors

Cell Cycle and DNA Damage Related Products

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1208	Doxorubicin (Adriamycin)	20 mg/mL	109 mg/mL	<1 mg/mL
S1225	Etoposide (VP-16)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1231	Topotecan HCl	92 mg/mL	92 mg/mL	<1 mg/mL
S1288	Camptothecin	<1 mg/mL	3 mg/mL	<1 mg/mL
S1198	Irinotecan	<1 mg/mL	10 mg/mL	<1 mg/mL
S1223	Epirubicin HCl	116 mg/mL	116 mg/mL	3 mg/mL
S2217	Irinotecan HCl Trihydrate (Campto)	2 mg/mL	135 mg/mL	7 mg/mL
S1228	Idarubicin HCl	10 mg/mL	107 mg/mL	<1 mg/mL
S1465	Moxifloxacin HCl	<1 mg/mL	88 mg/mL	<1 mg/mL
S1367	Amonafide	<1 mg/mL	57 mg/mL	4 mg/mL
S1393	Pirarubicin	<1 mg/mL	126 mg/mL	<1 mg/mL
S1327	Ellagic acid	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1342	Genistein	<1 mg/mL	54 mg/mL	2 mg/mL
S1463	Ofloxacin (Floxin)	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1889	Mitoxantrone	89 mg/mL	89 mg/mL	<1 mg/mL
S3181	Flumequine	<1 mg/mL	3 mg/mL	<1 mg/mL
S4119	Pefloxacin Mesylate Dihydrate	67 mg/mL	9 mg/mL	<1 mg/mL

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Product Categories

Idarubicin HCl

Validation & Quality Control

Product Citations(1)

Quality Control & MSDS

Related Compound Libraries

Idarubicin HCl is available in the following compound libraries:

Product Information

Compare Topoisomerase Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [5]

Cell Assay: [6]

Animal Study: [7]

References

Chemical Information

Research Area

Product Citations (1)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related Topoisomerase Inhibitors

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Kinase Assay: ^[5]

Cell Assay: ^[6]

Animal Study: ^[7]