Idarubicin HCl (Synonyms: 4Demethoxydaunorubicin, 4DMD, NSC 256439) |
| رقم الكتالوجGC14969 |
Idarubicin HCl هو عقار أنثراسيكلين مضاد للسرطان في الدم.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57852-57-0
Sample solution is provided at 25 µL, 10mM.
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Idarubicin is an inhibitor of DNA topoisomerase II [1].
Idarubicin is a synthetic anthracycline anticancer drug widely used in the treatment of acute myelogenous leukemia and some other hematological malignancies. It can be bioactivated by NADPH-cytochrome P450 reductase with resulting formation of single-strand breaks in DNA. This is the mechanism of Idarubicin ‘s antitumor effect [2].
Idarubicin is developed in an attempt to reduce the cardiotoxicity and enhance the therapeutic efficacy of the parent compound. Unlike the parent compound, Idarubicin can be given orally and has a better therapeutic index with respect to cardiotoxicity. Idarubicin has been shown to be an effective anti-leukemic agent in children and adults [3].
References:
[1] H. Dorota Halicka, M. Fevzi Ozkaynak, Oya Levendoglu-Tugal, Claudio Sandoval , Karen Seiter, Malgorzata Kajstura, Frank Traganos, Somasunadaram Jayabose, and Zbigniew Darzynkiewicz. DNA damage response as a biomarker in treatment of leukemias. Cell Cycle. 2009, 8(11): 1720–1724.
[2] Haydar Çelik and Emel Arinç. Evaluation of the Protective Effects of Quercetin, Rutin, Resveratrol, Naringenin and Trolox Against Idarubicin-Induced DNA Damage. J Pharm Pharmaceut Sci. 2010, 13(2): 231 – 241.
[3] Ching-Hon Pui, Siebold S. N. de Graaf, Lois W. Dow, John H. Rodman, William E. Evans, Bruce S. Alpert and Sharon B. Murphy. Phase I Clinical Trial of Orally Administered 4-Demethoxydaunorubicin (Idarubicin) with Pharmacokinetic and in Vitro Drug Sensitivity Testing in Children with Refractory Leukemia. Cancer Research. 1988, 48: 5348-5352.
| Cell experiment [1]: | |
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Cell lines |
NALM-6 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
0.1 nM ~ 10 μM; 24 hrs |
|
Applications |
In NALM-6 cells, Idarubicin inhibited cell proliferation with an IC50 value of 12 nM. |
| Animal experiment [2]: | |
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Animal models |
Rats, rabbits, mice and dogs |
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Dosage form |
2 mg/kg, 0 mg/kg ~ 75 mg/kg, 3 mg/kg and 0 mg/kg ~ 75 mg/kg; i.v. |
|
Applications |
Reduction of Idarubicin was dependent upon ketone reductases, and proceeds more stereoselectivity than that of most ketones. The high stereospecificity in Idarubicin reduction might be attributed to chiral induction under the presence of asymmetric centres near to the carbonyl group in Idarubicin. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Rowland AJ, Pietersz GA, McKenzie IF. Preclinical investigation of the antitumour effects of anti-CD19-idarubicin immunoconjugates. Cancer Immunol Immunother. 1993 Aug;37(3):195-202. [2]. Strolin Benedetti M, Pianezzola E, Fraier D, Castelli MG, Dostert P. Stereoselectivity of idarubicin reduction in various animal species and humans. Xenobiotica. 1991 Apr;21(4):473-80. |
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| Cas No. | 57852-57-0 | SDF | |
| المرادفات | 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 |
| الذوبان | ≥ 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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