Idarubicin HCl

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

For research use only.

Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) 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. Idarubicin induces mTOR-dependent cytotoxic autophagy.

Idarubicin HCl Chemical Structure

CAS No. 57852-57-0

Selleck's Idarubicin HCl has been cited by 40 publications

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Biological Activity

Description Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) 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. Idarubicin induces mTOR-dependent cytotoxic autophagy.
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 MoroR5l1d3SxeHnjxsBie3OjeR?= NFLxepBEgXSxdH;4bYMh[WO2aY\peJkh[WejaX7zeEBMPTZ{IHXyfZRpem:uZYXr[Y1q[yClZXzsd{whUUN3ME2wMlAxOiEQvF2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODR{NUC5N{c,OTB2MkWwPVM9N2F-
K562 cells NH7sNmFEgXSxdH;4bYPDqGG|c3H5 Mo\lOUBl[Xm| MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEWg[IF6eyCkeTDYWHQh[XO|YYmsJGlEPTB;MD6wNVIh|ryP M2npXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe2NVQxLz5zOEC3OlE1ODxxYU6=
mouse DA-3 cells NVPydpRXS3m2b4TvfIlkyqCjc4PhfS=> MXqyOEBp M3LrbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGRCNTNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JHhVXCCjc4PhfUwhUUN3ME2yMlMh|ryP M1HZNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlY5Lz5{NEmwNFY3QDxxYU6=
human ES2 cells NWDCR|NZS3m2b4TvfIlkyqCjc4PhfS=> NX62O2lMOjRiaB?= MmfRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSXMzKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDYWHQh[XO|YYmsJGlEPTB;Mz6yJO69VQ>? NF;FZnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY3QCd-MkS5NFA3Pjh:L3G+
human K562 cells M4joeXBzd2yrZnXyZZRqd25iYYPzZZk> NE\5WHA4OiCq NWT5SHNxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEeyJIhzeyxiR1m1NF0{NjNizszN MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR{MEG3OUc,OjV2MkCxO|U9N2F-
human SKOV3 cells MYHDfZRwfG:6aXRCpIF{e2G7 M4n2N|I1KGh? NEHQbIZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCjZoTldkAzPCCqcoOgZpkhYFSWIHHzd4F6NCCLQ{WwQVQvPSEQvF2= M1rYS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlY5Lz5{NEmwNFY3QDxxYU6=
HepG2 cells MkP3SpVv[3Srb36gZZN{[Xl? MnjmTY5pcWKrdHnvckBw\iCuaY\ldkB{fGGpZTDQcIF{dW:maYXtJIJmemeqZXmgbY5n\WO2aX;uJIlvKEincFeyJINmdGy|LDDJR|UxRTZwNkKg{txO M1\rVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUi2NVI1Lz5{MkW4OlEzPDxxYU6=
human MCF7 cells M3z2WmN6fG:2b4jpZ:Kh[XO|YYm= M3P5cFI1KGh? Mk\CR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjCyOEBpenNiYomgXHRVKGG|c3H5MEBKSzVyPUeuN{DPxE1? NFPoWHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY3QCd-MkS5NFA3Pjh:L3G+
mouse DA-3 cells MYHDfZRwfG:6aXRCpIF{e2G7 NWP3T2JTOjBizszN MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDERU0{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjdDCyNEB2VSCkeTDYWHQh[XO|YYm= NUHubHloRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PjhpPkK0PVAxPjZ6PD;hQi=>
neural precursor cells M1XN[2Z2dmO2aX;uJIF{e2G7 M1yxcGlvcGmkaYTpc44hd2ZibnX1do9{eGincnWgdJJwdGmoZYLheIlwdiCxZjDtc5V{\SCwZYXyZYwheHKnY4Xyd49zKGOnbHzzJIJ6KE2WVDDhd5NigQ>? NU\IbohQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NVc3OzFpPkG3OFE4PjNzPD;hQi=>
VERO-E6 MmXqSpVv[3Srb36gZZN{[Xl? MYC0PEBpenN? NYfK[JB[XG:6aXPpeJkhS0N3MDDh[4FqdnO2IG\FVm8uTTZiY3XscJMh\GW2ZYLtbY5m\CCjdDC0PEBpd3W{czDifUBpcWeqIHPvcpRmdnRiaX3h[4lv\yBqc3Ht[UBkd26maYTpc45{KGG|IELfUGV[KHerdHjveZQh\Xiyb4P1doUhfG9iMD6wNUBOV0liU1HSV{BEd1ZvMjD2bZJ2eyluIFPDOVA:OC5{zszN MlfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVEyPy9pPlPoSW1DVDxxYU6=
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 (from 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 Research:

[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 Research:

[7]

  • Animal Models: Rat, rabbit, mouse, dog
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 533.95
Formula

C26H27NO9.HCl

CAS No. 57852-57-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=CC=CC=C5C4=O)O)(C(=O)C)O)N)O.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02652871 Completed Drug: LY2510924|Drug: Idarubicin|Drug: Cytarabine Leukemia M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program May 9 2016 Phase 1
NCT02056782 Completed Drug: PGX-ODSH-2013-AML-1 Acute Myeloid Leukemia Cantex Pharmaceuticals|Translational Drug Development December 2013 Phase 1
NCT02028949 Completed Drug: Zavedos®|Other: Blood samples Unresectable Non-metastatic Hepatocellular Carcinoma|Child A/B7 Cirrhosis Centre Hospitalier Universitaire Dijon November 22 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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