[CAS NO. 57852-57-0]  Idarubicinhydrochloride

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PRODUCTS SPECIFICATIONS [57852-57-0]

Catalog
HY-17381
Brand
MCE
CAS
57852-57-0

DESCRIPTION [57852-57-0]

Overview

MDLMFCD00897212
Molecular Weight533.95
Molecular FormulaC26H28ClNO9
SMILESOC(C(C(C1=CC=CC=C21)=O)=C3C2=O)=C4[C@H](C[C@@](C(C)=O)(O)CC4=C3O)O[C@@](O[C@@H](C)[C@H]5O)([H])C[C@@H]5N.Cl

For research use only. We do not sell to patients.


Summary

Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts .


IC50 & Target

Topoisomerase II


In Vitro

The IC 50 of idarubicin is 3.3±0.4 ng/mL on MCF-7 monolayers and 7.9±1.1 ng/mL in multicellular spheroids [1] . Idarubicin has shown a greater cytotoxicity than daunorubicin or doxorubicin in various in vitro systems. This has been attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks [2] .Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively [3] . Idarubicin produces a concentration-dependent reduction in cell growth, with an IC 50 value of approximately 0.01 μM. Idarubicin produced a concentration-dependent inhibition of DNA synthesis [4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00542971 M.D. Anderson Cancer Center|Bayer
AML|Acute Myeloid Leukemia|Myelodysplastic Disorders
October 2007 Phase 1|Phase 2
NCT01534702 Hannover Medical School|Genzyme, a Sanofi Company
Acute Myeloid Leukemia
January 2012 Phase 1|Phase 2
NCT01700413 Grupo Cooperativo de Estudio y Tratamiento de las Leucemias Agudas y Mielodisplasias|Ministry of Health, Spain|Fundació Institut de Recerca de l´Hospital de la Santa Creu i Sant Pau
Di Novo Acute Myeloid Leukemia
October 2012 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL ( 156.06 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8728 mL 9.3642 mL 18.7283 mL
5 mM 0.3746 mL 1.8728 mL 3.7457 mL
10 mM 0.1873 mL 0.9364 mL 1.8728 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

5,12-Naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, hydrochloride (1:1), (7S,9S)-
5,12-Naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, hydrochloride, (7S-cis)-
5,12-Naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, hydrochloride, (7S,9S)-
4-Demethoxydaunorubicin hydrochloride
Idarubicin hydrochloride
Idamycin
Zavedos
4-DMD HCl
NSC 256439