Idarubicin HCl
(Synonyms: 盐酸伊达比星; 4-Demethoxydaunorubicin hydrochloride) 目录号 : GC14969
Idarubicin HCl是一种口服蒽环类抗白血病药物。
Cas No.:57852-57-0
Sample solution is provided at 25 µL, 10mM.
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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.
Idarubicin HCl是一种口服蒽环类抗白血病药物 [1]。Idarubicin HCl能稳定拓扑异构酶II与DNA之间的复合物，从而阻止DNA修复和正常复制。这最终导致DNA断裂累积、复制停滞，并诱导细胞周期停滞和细胞凋亡 [2-3]。Idarubicin HCl主要用于治疗成人急性髓系白血病 [4]。
在T47D细胞中，Idarubicin HCl（0.1-10μM；24-72h）处理后，细胞活力显著降低 [5]。在成纤维细胞中，Idarubicin HCl（0.5-10μM；24h）诱导线粒体膜电位随时间依赖性下降，并显著增加细胞内钙离子浓度和胱天蛋白酶3活性 [6]。
在U937细胞异种移植小鼠模型中，decitabine与Idarubicin HCl（0.5mg/kg；ip；7d）联合应用可有效抑制肿瘤生长 [7]。在LNCaP细胞异种移植小鼠模型中，Idarubicin HCl（0.25mg/kg；ip；25d）单独使用或与abiraterone acetate联合使用可显著抑制肿瘤生长并延长小鼠生存期 [8]。
| 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: | |
| Cas No. | 57852-57-0 | SDF | |
| 别名 | 盐酸伊达比星; 4-Demethoxydaunorubicin hydrochloride | ||
| 化学名 | 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 | ||
| 分子式 | C26H27NO9.HCl | 分子量 | 533.95 |
| 溶解度 | ≥ 26.7mg/mL in DMSO | 储存条件 | 4°C, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet