Idarubicin HCl

Catalog No.S1228 Synonyms: 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl

Idarubicin HCl Chemical Structure

Molecular Weight(MW): 533.95

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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In DMSO USD 150 In stock
USD 70 In stock
USD 120 In stock
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  • Clin Cancer Res, 2016, 22(3):746-56.. Idarubicin HCl purchased from Selleck.

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562 erythroleukemic cells Ml30R5l1d3SxeHnjxsBie3OjeR?= MVnDfZRwfG:6aXOgZYN1cX[rdImgZYdicW6|dDDLOVYzKGW{eYTodo9t\XWtZX3pZ{Bk\WyuczygTWM2OD1yLkCwNkDPxE1? NG\0S4cyODR{NUC5Ny=>
K562 cells MoHKR5l1d3SxeHnjxsBie3OjeR?= NIrPOW42KGSjeYO= M{m2bmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhUUN3ME2wMlAyOiEQvF2= NEPtXocyQDB5NkG0NC=>
mouse DA-3 cells MorTR5l1d3SxeHnjxsBie3OjeR?= M37ZdlI1KGh? NYHRcIN[S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhTEFvMzDj[YxteyCjZoTldkAzPCCqcoOgZpkhYFSWIHHzd4F6NCCLQ{WwQVIvOyEQvF2= M2TISFI1QTByNk[4
human ES2 cells MmPRR5l1d3SxeHnjxsBie3OjeR?= M1XZc|I1KGh? NXS3Z3p3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTVN{IHPlcIx{KGGodHXyJFI1KGi{czDifUBZXFRiYYPzZZktKEmFNUC9N{4zKM7:TR?= MV[yOFkxODZ4OB?=
human K562 cells NF;DN2JRem:uaX\ldoF1cW:wIHHzd4F6 MX[3NkBp NFT2dJdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiN{KgbJJ{NCCJSUWwQVMvOyEQvF2= NHrqT4UzPTR{MEG3OS=>
human SKOV3 cells NYLnNYtMS3m2b4TvfIlkyqCjc4PhfS=> Mn;lNlQhcA>? NV72NpR4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFiWVDDhd5NigSxiSVO1NF01NjVizszN M3PweFI1QTByNk[4
HepG2 cells NEPI[5dHfW6ldHnvckBie3OjeR?= NFrodpFKdmirYnn0bY9vKG:oIHzpeoVzKHO2YXflJHBt[XOvb3TpeY0h[mW{Z3jlbUBqdm[nY4Tpc44hcW5iSHXwS|Ih[2WubIOsJGlEPTB;Nj62NkDPxE1? M4DEdVIzPTh4MUK0
human MCF7 cells NGPNZ5dEgXSxdH;4bYPDqGG|c3H5 NVvRPJRsOjRiaB?= NWHI[4IzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkAzPCCqcoOgZpkhYFSWIHHzd4F6NCCLQ{WwQVcvOyEQvF2= Mlj3NlQ6ODB4Nki=
mouse DA-3 cells NW[4RmZHS3m2b4TvfIlkyqCjc4PhfS=> NFnkd3IzOCEQvF2= M{XtV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGRCNTNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHH0JFIxKHWPIHL5JHhVXCCjc4PhfS=> NFLsV44zPDlyME[2PC=>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:

[5]

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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 Research:

[6]

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  • 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.


    (Only for Reference)
Animal Research:

[7]

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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (187.28 mM)
Water 7 mg/mL warmed (13.1 mM)
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:

* 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 Information

Molecular Weight 533.95
Formula

C26H27NO9.HCl

CAS No. 57852-57-0
Storage powder
in solvent
Synonyms 4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02635074 Recruiting Recurrent Adult Acute Myeloid Leukemia Bruno C. Medeiros|National Cancer Institute (NCI)|Stanford University November 2016 Phase 1
NCT02527174 Not yet recruiting Leukemia, Myeloid, Acute|Leukemia, Monocytic, Acute|Leukemia, Myelomonocytic, Acute|Leukemia, Erythroblastic, Acute|Leukemia, Megakaryoblastic, Acute University of Alberta November 2016 Phase 1
NCT02937662 Not yet recruiting Acute Myeloid Leukemia Institute of Hematology & Blood Diseases Hospital October 2016 Phase 2
NCT02905994 Not yet recruiting AML Massachusetts General Hospital|Boehringer Ingelheim September 2016 Phase 1
NCT02668653 Recruiting Acute Myeloid Leukemia|Leukemia Daiichi Sankyo Inc. September 2016 Phase 3
NCT02873338 Recruiting Acute Myeloid Leukemia Cantex Pharmaceuticals August 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID