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Doxorubicin/阿霉素 {[allProObj[0].p_purity_real_show]}

货号:A206785 同义名: Hydroxydaunorubicin

Doxorubicin is a Topoisomerase II (Top2) catalytic inhibitor, also is a broad spectrum antibiotic used in the treatment of cancers, with IC50 of 374 nM for Hela cells.

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Doxorubicin/阿霉素 化学结构 CAS号:23214-92-8
Doxorubicin/阿霉素 化学结构
CAS号:23214-92-8
Doxorubicin/阿霉素 3D分子结构
CAS号:23214-92-8
Doxorubicin/阿霉素 化学结构 CAS号:23214-92-8
Doxorubicin/阿霉素 3D分子结构 CAS号:23214-92-8
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Doxorubicin/阿霉素 纯度/质量文件 产品仅供科研

货号:A206785 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid 98%
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

98%
Irinotecan HCl Trihydrate 98%
SN-38 98%
Levofloxacin hydrate 98%
Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99.5%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone 2HCl PKC 98%
Nalidixic acid 98%
Doxorubicin 97%
Novobiocin sodium 95%
Amonafide 99%+
Pirarubicin 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

99%+
Genistein EGFR 98%
Teniposide 98%
Moxifloxacin 98%
Ciprofloxacin 98%
Clinafloxacin 99%
Gatifloxacin 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Doxorubicin/阿霉素 生物活性

靶点
  • Topo II

描述 Doxorubicin is a Topoisomerase II (Top2) catalytic inhibitor, also is a broad spectrum antibiotic used in the treatment of cancers, with IC50 of 374 nM for Hela cells.

Doxorubicin/阿霉素 细胞实验

Cell Line
Concentration Treated Time Description References
B16F10 melanoma cells 5 µM 6 hours Induce apoptosis to model apoptotic tumor cells Nat Commun. 2023 Mar 25;14(1):1675.
CT26 cells 10 µM 1, 2, 4, or 8 hours To evaluate the intracellular trafficking profiles of DNCaNPs, showing significantly enhanced DOX fluorescence inside the nuclei Nanomicro Lett. 2020 Nov 22;13(1):29.
CT26 multicellular spheroids (MCSs) 5 µM 12 hours To study the pH-responsive penetration ability of DNCaNPs, showing homogeneous distribution of DOX fluorescence at pH 6.5 Nanomicro Lett. 2020 Nov 22;13(1):29.
CT26 cells 5 µM 24 hours To assess the capacity of DNCaNPs to induce immunogenic cell death (ICD), showing increased ATP release Nanomicro Lett. 2020 Nov 22;13(1):29.
4T1 20 µM 4 hours DOX was able to induce EMT in CSCs, making the breast cancer cells more aggressive and metastatic J Nanobiotechnology. 2024 May 25;22(1):285.
MDAMB-231 20 µM 4 hours DOX was able to induce EMT in CSCs, making the breast cancer cells more aggressive and metastatic J Nanobiotechnology. 2024 May 25;22(1):285.
CT26 cells 5 µM 4 or 12 hours To evaluate CRT expression and HMGB1 release, showing increased CRT expression and HMGB1 release after DNCaNPs treatment Nanomicro Lett. 2020 Nov 22;13(1):29.
MDA-MB-231 cells 64 μg/mL 24 hours Evaluate the cytotoxicity of HA-LP-EPS/DOX on MDA-MB-231 cells, results showed that HA-LP-EPS/DOX was more cytotoxic than LP-EPS/DOX, likely due to HA-targeted modification increasing cellular uptake and improving DOX delivery efficiency. Small. 2022 Apr;18(16):e2107690.
WI-38 cells 1 μg/mL 120 minutes Evaluate the uptake of OCT-conjugated micelles in WI-38 cells, showing no significant difference between targeted and non-targeted micelles Biomaterials. 2016 Jun;91:1-10.
BON cells 1 μg/mL 120 minutes Evaluate the uptake of OCT-conjugated micelles in BON cells, showing a 4-fold higher uptake compared to non-targeted micelles Biomaterials. 2016 Jun;91:1-10.
DHL-4 cells 200 ng/ml 24 hours Doxorubicin treatment caused significant decreases in mitochondrial Complex I and II activities in wt p53 cells, but had minimal effect in mutant p53 cells Apoptosis. 2011 Mar;16(3):301-10
IGROV-1 ovarian cancer cells 200 nM 6 hours Evaluate the synergistic antiproliferative effects of IMGN853 with doxorubicin, showing that combination treatment had synergistic effects. Neoplasia. 2016 Dec;18(12):775-784
H9C2 cells 2 μM 6 h To evaluate the effect of DOX on H9C2 cells. Results showed that DOX significantly increased lipid peroxidation levels in H9C2 cells. Redox Biol. 2024 Apr;70:103024

Doxorubicin/阿霉素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c Nude mice Lung cancer mouse model Intravenous injection 0.1 mg/kg Every three days for a total of 5 injections To evaluate the anticancer efficacy of Lonidamine in combination with Doxorubicin in a lung cancer mouse model, the results showed that the combination significantly suppressed tumor growth. Drug Deliv. 2022 Dec;29(1):192-202
BALB/c mice 4T1.2 tumor model Intravenous injection 5 mg/kg Once every 3 days for 3 times To evaluate the in vivo antitumor efficacy of DOX/PSSN10 mixed micelles, results showed significant tumor growth inhibition and prolonged survival. Acta Pharmacol Sin. 2017 Jun;38(6):823-834.
NPG mice Leukemia mice model Tail vein injection 4 mg/kg Two doses, 11 days apart To evaluate the antitumor efficacy of dual-targeting nanovesicles in leukemia mice models. Results showed that dual-targeting nanovesicles significantly prolonged the survival time of mice and reduced bone marrow necrosis. Acta Pharm Sin B. 2020 Nov;10(11):2183-2197.
BALB/c mice Breast cancer model Tail vein injection 5 mg/kg Single dose To study the pharmacokinetics and tissue distribution of DOX in mice Heliyon. 2024 Jul 26;10(15):e35123
Female BALB/c nude mice Female BALB/c nude mice Intravenous injection 1.3 mg/kg Single dose To evaluate the pharmacokinetics of doxorubicin and its metabolites Elife. 2022 Dec 7;11:e77443
Wistar rats Intraperitoneal injection 3 mg DOX equivalent/kg body weight Every 6 days for a total of 4 doses over 24 days Compare the concentration of metabolites in urine after treatment with different DOX nanoformulations Molecules. 2022 Feb 9;27(4):1177
Female BALB/c nude mice Female BALB/c nude mice Intravenous injection 1.3 mg/kg Single dose To evaluate the pharmacokinetics of doxorubicin and its metabolites Molecules. 2020 Mar 10;25(5):1254
Athymic nude mice KB or MIA Paca-2 xenografts Intravenous injection 10 mg/kg Single photo-treatment The use of leaky HPPH liposomes significantly improved doxorubicin bioavailability compared to stable standard liposomes, leading to rapid tumor eradication J Control Release. 2015 Dec 28;220(Pt A):484-494
BALB/c nude mice PC-3 xenograft model Intravenous injection 10 mg/kg Single dose, observed for 22 days To evaluate the therapeutic efficacy of DSPC/MonY-BN/Dox in the PC-3 xenograft model. Results showed that DSPC/MonY-BN/Dox at a dose of 10 mg/kg produced 60% tumor growth inhibition compared to the control group, while DSPC/Dox only produced 36% inhibition. Int J Nanomedicine. 2012;7:2007-17

Doxorubicin/阿霉素 动物研究

Dose Rat: 1 mg/kg - 3 mg/kg[3] (i.v.); 6 mg/kg - 18 mg/kg[4] (i.p.); 20 mg/kg[5] (i.p.)
Administration i.v., i.p.
Pharmacokinetics
Animal Mice[6] Rats[6]
Dose 10 mg/kg 1 mg/kg
Administration i.v. i.v.
Cmax 2115 ± 61 ng/ml 470 ± 144 ng/ml
AUCinf 2204 ng/ml·h 468 ± 66 ng/ml·h
AUClast 2037 ± 82 ng/ml·h 356 ± 20 ng/ml·h

Doxorubicin/阿霉素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01891539 - Unknown December 2017 Italy ... 展开 >> Azienda Ospedaliera Ospedali Riuniti Marche Nord, Presidio Ospedaliero San Salvatore Recruiting Pesaro, PU, Italy, 61122 Contact: Giammaria Fiorentini, MD    +390721364124    giammaria.fiorentini@ospedalimarchenord.it    Principal Investigator: Giammaria Fiorentini, MD 收起 <<
NCT00815945 Mesenchymal Tumor ... 展开 >> Carcinosarcoma Leiomyosarcoma 收起 << Phase 2 Completed - Germany ... 展开 >> Charité, Campus Virchow Klinikum, Frauenklinik Berlin, Germany, 13353 Malteser Krankenhaus, Gynäkologie und Geburtshilfe Bonn, Germany, 53123 Klinikum Bremen-Mitte gGmbH, Frauenklinik Bremen, Germany, 28177 Universitätsklinikum Carl Gustav Carus, Klinik und Poliklinik für Frauenheilkunde und Geburtshilfe Dresden, Germany, 01307 Evangelisches Krankenhaus Düsseldorf, Frauenklinik Duesseldorf, Germany, 40217 Universitätsklinikum Essen, Frauenklinik Essen, Germany, 45122 Klinikum der J. W. Goethe-Universität, Klinik für Gynäkologie und Geburtshilfe Frankfurt, Germany, 60590 University Hospital Hamburg-Eppendorf Hamburg, Germany, 20251 Gynäkologisch-onkologische Praxis Hannover, Germany, 30177 St. Vincentius Kliniken AG, Frauenklinik Karlsruhe, Germany, 76135 Universitätsklinikum Giessen und Marburg GmbH, Klinik für Gynäkologie, Gynäkologische Endokrinologie und Onkologie Marburg, Germany, 35043 Klinikum Großhadern, Frauenklinik München, Germany, 81377 Universitätsklinikum Tübingen, Frauenklinik Tübingen, Germany, 72076 Universitätsklinikum Ulm, Universitätsfrauenklinik Ulm, Germany, 89075 Dr. Horst Schmidt Kliniken GmbH, Klinik für Gynäkologie und gynäkologische Onkologie Wiesbaden, Germany, 65199 收起 <<
NCT00755261 Sarcoma Soft ... 展开 >>Tissue Sarcoma 收起 << Phase 2 Terminated(The study has been ... 展开 >>terminated due to low accrual.) 收起 << - United States, Maryland ... 展开 >> Johns Hopkins SKCCC Baltimore, Maryland, United States, 21231 收起 <<

Doxorubicin/阿霉素 参考文献

[1]Nitiss JL. Targeting DNA topoisomerase II in cancer chemotherapy. Nat Rev Cancer. 2009 May;9(5):338-50.

[2]El-Zawahry A, McKillop J, Voelkel-Johnson C. Doxorubicin increases the effectiveness of Apo2L/TRAIL for tumor growth inhibition of prostate cancer xenografts. BMC Cancer. 2005 Jan 7;5:2.

[3]Wapstra FH, van Goor H, et al. Dose of doxorubicin determines severity of renal damage and responsiveness to ACE-inhibition in experimental nephrosis. J Pharmacol Toxicol Methods. 1999 Apr-Jun;41(2-3):69-73.

[4]Alshabanah OA, Hafez MM, et al. Doxorubicin toxicity can be ameliorated during antioxidant L-carnitine supplementation. Oxid Med Cell Longev. 2010 Nov-Dec;3(6):428-33. Epub 2010 Nov 1.

[5]Sun XP, Wan LL, et al. Scutellarin protects against doxorubicin-induced acute cardiotoxicity and regulates its accumulation in the heart. Arch Pharm Res. 2017 Jul;40(7):875-883.

[6]Chung SW, Kim GC, et al. Metronomic oral doxorubicin in combination of Chk1 inhibitor MK-8776 for p53-deficient breast cancer treatment. Biomaterials. 2018 Nov;182:35-43.

Doxorubicin/阿霉素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.20mL

1.84mL

0.92mL

18.40mL

3.68mL

1.84mL

Doxorubicin/阿霉素 技术信息

CAS号23214-92-8
分子式C27H29NO11
分子量 543.52
SMILES Code [H][C@@]1(O[C@H]2C[C@](O)(C(CO)=O)CC(C2=C3O)=C(O)C4=C3C(C5=C(OC)C=CC=C5C4=O)=O)O[C@@H](C)[C@@H](O)[C@@H](N)C1
MDL No. MFCD00869292
别名 Hydroxydaunorubicin
运输蓝冰
InChI Key AOJJSUZBOXZQNB-TZSSRYMLSA-N
Pubchem ID 31703
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

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