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Idarubicin HCl (Synonyms: 4Demethoxydaunorubicin, 4DMD, NSC 256439)

カタログ番号GC14969

イダルビシン HCl は、アントラサイクリン系抗白血病薬です。

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Idarubicin HCl 化学構造

Cas No.: 57852-57-0

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$55.00
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1mg
$19.00
在庫あり
5mg
$46.00
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10mg
$77.00
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25mg
$127.00
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50mg
$178.00
在庫あり
100mg
$249.00
在庫あり

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顧客レビュー

カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.

Description of Idarubicin HCl

Idarubicin HCl is an orally active anthracycline antileukemic agent [1]. Idarubicin HCl stabilizes the complex between topoisomerase II and DNA, preventing DNA repair and normal replication. This ultimately leads to accumulation of DNA breaks, replication arrest, and induction of cell cycle arrest and apoptosis [2-3]. Idarubicin HCl is primarily used to treat adult acute myeloid leukemia [4].

In T47D cells, the cell viability of cells was significantly reduced after Idarubicin HCl (0.1-10μM;24-72h) treatment [5]. In fibroblasts, Idarubicin HCl (0.5-10μM; 24h) induces a time-dependent decrease in mitochondrial membrane potential and significantly increases intracellular calcium concentration and caspase-3 activity [6].

In U937 cells xenograft mice model, combination of decitabine and Idarubicin HCl (0.5mg/kg; ip; 7d) effectively inhibits tumor growth [7]. In LNCaP cells xenograft mice model, Idarubicin HCl (0.25mg/kg; ip; 25d) alone or in combination with abiraterone acetate significantly reduced tumor growth and prolonged mouse survival [8].

References:
[1]. Orlandi P, Barbara C, Bocci G, et al. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids[J]. Journal of chemotherapy, 2005, 17(6): 663-667.
[2]. Dartsch D C, Gieseler F. Repair of idarubicin-induced DNA damage: a cause of resistance?[J]. DNA repair, 2007, 6(11): 1618-1628.
[3]. van den Boogaard W M C, Komninos D S J, Vermeij W P. Chemotherapy side-effects: not all DNA damage is equal[J]. Cancers, 2022, 14(3): 627.
[4]. Sherif H A, Magdy A, Elshesheni H A, et al. Treatment outcome of doxorubicin versus idarubicin in adult acute myeloid leukemia[J]. Leukemia Research Reports, 2021, 16: 100272.
[5]. Zhong S, Li C, Han X, et al. Idarubicin stimulates cell cycle-and TET2-dependent oxidation of DNA 5-methylcytosine in cancer cells[J]. Chemical Research in Toxicology, 2019, 32(5): 861-868.
[6]. Dragojew S, Marczak A, Maszewski J, et al. The induction of apoptosis by daunorubicin and idarubicin in human trisomic and diabetic fibroblasts[J]. Cellular & molecular biology letters, 2008, 13(2): 182-194.
[7]. Li K, Hu C, Mei C, et al. Sequential combination of decitabine and idarubicin synergistically enhances anti-leukemia effect followed by demethylating Wnt pathway inhibitor promoters and downregulating Wnt pathway nuclear target[J]. Journal of translational medicine, 2014, 12(1): 167.
[8]. Zhang Y, Wei W, Li C, et al. Idarubicin combats abiraterone and enzalutamide resistance in prostate cells via targeting XPA protein[J]. Cell Death & Disease, 2022, 13(12): 1034.

Protocol of Idarubicin HCl

Cell experiment [1]:

Cell lines

T47D cells

Preparation Method

Human breast cancer cell line T47D was cultured in Roswell Park Memorial Institute (RPMI)-1640 medium supplemented with 10% fetal bovine serum, 100U/mL penicillin, and 100μg/mL streptomycin in a humidified incubator at 37℃ and 5% CO2. When the cell confluence reached approximately 70%, fresh medium containing a certain concentration of Idarubicin HCl was used to continue culturing for 24 hours or longer. After a period of Idarubicin HCl treatment, cells were collected for genomic DNA extraction.

Reaction Conditions

0.1-10μM;24-72h

Applications

The cell viability of cells was significantly reduced after Idarubicin HCl treatment.
Animal experiment [2]:

Animal models

U937 cells xenograft mice model

Preparation Method

The AML cell line U937 (1 × 107 cells/animal) was injected subcutaneously into the right flank of 6- to 8-week-old NOD-SCID mice. When tumors reached a volume of ~50 mm3, the animals were randomly divided into four groups. A total of 16 mice were divided into four groups of 4. Five consecutive days of decitabine (0.5mg/kg/day) were followed by three days of Idarubicin HCl (0.5mg/kg/day), or five days of decitabine alone followed by three days of Idarubicin HCl alone. An untreated control group received PBS. Drug and PBS were injected intraperitoneally.

Dosage form

0.5mg/kg; ip; 7d

Applications

Combination of decitabine and Idarubicin HCl effectively inhibits tumor growth.

References:
[1]. Zhong S, Li C, Han X, et al. Idarubicin stimulates cell cycle-and TET2-dependent oxidation of DNA 5-methylcytosine in cancer cells[J]. Chemical Research in Toxicology, 2019, 32(5): 861-868.
[2]. Li K, Hu C, Mei C, et al. Sequential combination of decitabine and idarubicin synergistically enhances anti-leukemia effect followed by demethylating Wnt pathway inhibitor promoters and downregulating Wnt pathway nuclear target[J]. Journal of translational medicine, 2014, 12(1): 167.

Chemical Properties of Idarubicin HCl

Cas No. 57852-57-0 SDF
同義語 4Demethoxydaunorubicin, 4DMD, NSC 256439
Chemical Name 9-acetyl-7-(4-amino-5-hydroxy-6-methyloxan-2-yl)oxy-6,9,11-trihydroxy-8,10-dihydro-7H-tetracene-5,12-dione;hydrochloride
Canonical SMILES CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=CC=CC=C5C4=O)O)(C(=O)C)O)N)O.Cl
Formula C26H27NO9.HCl M.Wt 533.95
溶解度 ≥ 26.7mg/mL in DMSO Storage 4°C, away from moisture and light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Idarubicin HCl

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.8728 mL 9.3642 mL 18.7283 mL
5 mM 374.6 μL 1.8728 mL 3.7457 mL
10 mM 187.3 μL 936.4 μL 1.8728 mL
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