Daunorubicin HCl
(Synonyms: 盐酸柔红霉素; Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride) 目录号 : GC10354
Daunorubicin HCl是一种天然来源的蒽环类抗生素，通过嵌入DNA双链并抑制拓扑异构酶Ⅱ活性，阻断DNA复制与转录，从而诱导肿瘤细胞凋亡。
Cas No.:23541-50-6
Sample solution is provided at 25 µL, 10mM.
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Daunorubicin HCl is a natural anthracycline antibiotic that intercalates into DNA double strands and inhibits topoisomerase II activity, thereby blocking DNA replication and transcription and inducing tumor cell apoptosis[1]. Clinically, Daunorubicin HCl is primarily used for the treatment of acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL)[2-3]. In addition, Daunorubicin HCl has shown therapeutic potential against gliomas[4].
In vitro, treatment of human acute myeloid leukemia HL-60 cells with 0.1–1μM Daunorubicin HCl for 1h, followed by incubation in drug-free medium for 6–24h, rapidly induces apoptotic cell death[5]. Exposure of human acute myeloid leukemia U937 cells to 0.5–1μM Daunorubicin HCl for 2–24h significantly activates the PI3K/Akt signaling pathway, leading to cell cycle arrest and enhanced apoptosis[6].
In vivo, intraperitoneal administration of 2mg/kg Daunorubicin HCl every other day for 15 days in HCT116 colorectal cancer xenograft BALB/c nude mice markedly inhibited tumor growth, reduced GLI1 expression in tumor tissues, and induced tumor cell apoptosis[7]. Intravenous tail-vein injection of 10mg/kg Daunorubicin HCl for three consecutive days in C57BL/6 wild-type and Trp53-knockout mice elicited early, transient apoptosis in wild-type mice, with recovery to normal morphology by day 4. In contrast, Trp53-knockout mice exhibited delayed and persistent extensive necrosis and structural disruption despite the absence of early apoptosis[8].
References:
[1] Di Marco A, Cassinelli G, Arcamone F. The discovery of Daunorubicin HCl. Cancer Treat Rep. 1981;65 Suppl 4:3-8.
[2] Cann ML, Herring LE, Haar LL, et al. Dasatinib Is Preferentially Active in the Activated B-Cell Subtype of Diffuse Large B-Cell Lymphoma. J Proteome Res. 2019 Jan 4;18(1):522-534.
[3] Lin TY, Zhu Y, Li Y, et al. Daunorubicin HCl-containing CLL1-targeting nanomicelles have anti-leukemia stem cell activity in acute myeloid leukemia. Nanomedicine. 2019 Aug;20:102004.
[4] Casazza AM, Pratesi G, Giuliani F, et al. Antileukemic activity of 4-demethoxyDaunorubicin HCl in mice. Tumori. 1980 Oct 31;66(5):549-64.
[5] Côme MG, Skladanowski A, Larsen AK, et al. Dual mechanism of Daunorubicin HCl-induced cell death in both sensitive and MDR-resistant HL-60 cells. Br J Cancer. 1999 Mar;79(7-8):1090-7.
[6] Plo I, Bettaïeb A, Payrastre B, et al. The phosphoinositide 3-kinase/Akt pathway is activated by Daunorubicin HCl in human acute myeloid leukemia cell lines. FEBS Lett. 1999 Jun 11;452(3):150-4.
[7] Kim BR, Kim DY, Tran NL, et al. Daunorubicin HCl induces GLI1‑dependent apoptosis in colorectal cancer cell lines. Int J Oncol. 2024 Jun;64(6):66.
[8] Herfindal L, Myhren L, Gjertsen BT, et al. Functional p53 is required for rapid restoration of Daunorubicin HCl-induced lesions of the spleen. BMC Cancer. 2013 Jul 11;13:341.
Daunorubicin HCl是一种天然来源的蒽环类抗生素，通过嵌入DNA双链并抑制拓扑异构酶Ⅱ活性，阻断DNA复制与转录，从而诱导肿瘤细胞凋亡[1]。临床上主要用于治疗急性髓系白血病（AML）和急性淋巴细胞白血病（ALL）[2-3]。此外，Daunorubicin HCl还具备治疗神经胶质瘤等其他类型癌症的潜力[4]。
在体外，Daunorubicin HCl（0.1–1μM）处理人急性髓系白血病HL-60细胞1h，随后在不含药物培养基中继续培养6–24h，可诱导快速细胞凋亡[5]。Daunorubicin HCl（0.5–1μM）处理人急性髓系白血病U937细胞2–24h，可显著激活PI3K/Akt信号通路，诱导细胞周期阻滞并增强细胞凋亡[6]。
在体内，Daunorubicin HCl（2mg/kg）腹腔注射于HCT116结直肠癌异种移植BALB/c裸鼠模型，隔日一次，持续15天，Daunorubicin HCl显著抑制了肿瘤生长并降低肿瘤组织中GLI1表达水平，同时诱导肿瘤细胞凋亡[7]。Daunorubicin HCl（10mg/kg）尾静脉注射于C57BL/6野生型与Trp53敲除小鼠，连续3天。Daunorubicin HCl在野生型小鼠中引起早期、短暂的细胞凋亡，并在第4天恢复至正常形态；而在Trp53敲除小鼠中，尽管早期凋亡缺失，却于第4天出现延迟且持续的大面积坏死与结构紊乱[8]。
| Cell experiment [1]: | |
Cell lines | Human acute myeloid leukemia HL-60 cells |
Preparation Method | HL-60 cells were cultured in RPMI-1640 with 10% FCS at 37°C, 5% CO₂. For experiments, cells were seeded at 0.5 × 10⁶cells/mL and exposed to Daunorubicin HCl for 1h, then washed and maintained in drug-free medium for the indicated chase periods. |
Reaction Conditions | 0.5–1µM Daunorubicin HCl for 1h followed by 6–24h drug-free incubation. |
Applications | Daunorubicin HCl rapidly induced apoptotic cell death in HL-60 cells, evidenced by pyknotic nuclei, internucleosomal DNA fragmentation, and activation of caspases-3/8/9 and PARP cleavage. Cell cycle analysis revealed an early S-phase block and accumulation of sub-G1 apoptotic cells, confirming Daunorubicin HCl-mediated caspase-dependent apoptosis. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice bearing HCT116 colorectal-cancer xenografts. |
Preparation Method | HCT116 cells (2×10⁶) were subcutaneously implanted into the dorsal flank of 5-week-old female mice. Once tumors reached ≈100mm³, animals were randomized and treated with either vehicle (DMSO) or Daunorubicin HCl every other day for 15 days. |
Dosage form | 2mg/kg; intraperitoneal injection, every 48h for 15 days. |
Applications | Daunorubicin HCl profoundly inhibited tumor growth and reduced tumor weight without affecting body weight. Immunohistochemistry revealed marked suppression of GLI1 and elevation of p53 within tumor tissues, while TUNEL staining confirmed extensive apoptosis. |
References: | |
| Cas No. | 23541-50-6 | SDF | |
| 别名 | 盐酸柔红霉素; Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride | ||
| 化学名 | (8S,10S)-8-acetyl-10-(((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-6,8,11-trihydroxy-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride | ||
| Canonical SMILES | Cl[H].O=C(C([H])([H])[H])[C@@](C([H])([H])[C@]1([H])O[C@](C([H])([H])[C@]2([H])N([H])[H])([H])O[C@](C([H])([H])[H])([H])[C@@]2([H])O[H])(C([H])([H])C3=C1C(O[H])=C(C(C4=C5C([H])=C([H])C([H])=C4OC([H])([H])[H])=O)C(C5=O)=C3O[H])O[H] | ||
| 分子式 | C27H30ClNO10 | 分子量 | 563.98 |
| 溶解度 | ≥ 80mg/mL in DMSO | 储存条件 | 4°C, protect from 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 | 1.7731 mL | 8.8656 mL | 17.7311 mL |
| 5 mM | 0.3546 mL | 1.7731 mL | 3.5462 mL |
| 10 mM | 0.1773 mL | 0.8866 mL | 1.7731 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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