Aldoxorubicin
Based on 22 publication(s) in Google Scholar
Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
For research use only. We do not sell to patients.
- Purity: 95.56%
- CAS No.: 1361644-26-9
- Formula: C37H42N4O13
- Molecular Weight:750.75
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Storage:
-80°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Aldoxorubicin
More- ACS Nano. 2026 Mar 10;20(9):7928-7939. [Abstract]
- Acta Pharm Sin B. 2023 Apr;13(4):1429-1437. [Abstract]
- Sci Adv. 2019 Aug 14;5(8):eaaw6081. [Abstract]
- Small. 2023 May;19(21):e2205606. [Abstract]
- Nano Res. 08 February 2022.
- Int J Nanomedicine. 2022 Sep 20:17:4401-4417. [Abstract]
- Br J Pharmacol. 2017 Sep;174(17):2862-2879. [Abstract]
- Small Sci. 2023 Aug;3(8):2300067. [Abstract]
- Pharmaceutics. 2021 May 5;13(5):661. [Abstract]
- Bioeng Transl Med. 2022 Jul 30;8(1):e10377. [Abstract]
- ACS Biomater Sci Eng. 2026 Jun 23. [Abstract]
- Int J Mol Sci. 2023 Feb 27;24(5):4590. [Abstract]
- J Drug Deliv Sci Technol. 2020, 102048.
- Bioconjug Chem. 2025 Feb 19;36(2):190-202. [Abstract]
- Bioconjug Chem. 2023 Sep 20;34(9):1585-1595. [Abstract]
- Bioconjug Chem. 2019 Dec 18;30(12):3098-3106. [Abstract]
- ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]
- Biotechnol J. 2020 Dec;15(12):e2000077. [Abstract]
- Patent. US20220298225A1.
- Patent. US20200376013A1.
- Oncotarget. 2018 Oct 9;9(79):34935-34944. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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IF
All Topoisomerase Isoforms
More
Biological Activity
Topoisomerase II[4]
Aldoxorubicin (INNO-206) (0.27 to 2.16 μM) inhibits blood vessel formation and reduces multiple myeloma cell growth in a pH-dependent fashion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1361644-26-9
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Appearance Solid
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Molecular Weight 750.75
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Formula C37H42N4O13
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Color Brown to red
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SMILES
[H][C@@]1(O[C@H]2C[C@@](/C(CO)=N/NC(CCCCCN3C(C=CC3=O)=O)=O)(O)CC(C2=C4O)=C(O)C5=C4C(C6=C(OC)C=CC=C6C5=O)=O)O[C@@H](C)[C@@H](O)[C@@H](N)C1
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Synonyms
INNO-206; DOXO-EMCH
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Shipping
Shipping with dry ice.
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Storage
-80°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (22)
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Journal Impact Factor
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Most Recent
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ACS Nano
A Biomimetic Microparticle Disrupting the Intracellular/Extracellular pH Homeostasis of Tumor Cells for Cancer Chemo-Immunotherapy. [Abstract]2026 Mar 10;20(9):7928-7939. PMID: 41729031 -
Acta Pharm Sin B
2023 Apr;13(4):1429-1437. PMID: 37139433 -
Sci Adv
Engineered collagen-binding serum albumin as a drug conjugate carrier for cancer therapy. [Abstract]2019 Aug 14;5(8):eaaw6081. PMID: 31453327
Aldoxorubicin purchased from MedChemExpress. Usage Cited in: Sci Adv. 2019 Aug 14;5(8):eaaw6081. [Abstract]
Aldoxorubicin, Dox-SA, or Dox-CBD-SA (5 mg/kg on a Dox basis) was administered to tumor-free FVB mice via tail vein injection. Blood plasma was collected at the indicated time points.
Aldoxorubicin purchased from MedChemExpress. Usage Cited in: Sci Adv. 2019 Aug 14;5(8):eaaw6081. [Abstract]
MMTV-PyMT tumor-bearing mice were treated with aldoxorubicin, Dox-SA, or Dox-CBD-SA (4.16 mg/kg on a Dox basis). At the indicated time points, tumors were harvested, and the amount of Dox within the tumors was quantified.
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Small
Overcoming Non-Specific Interactions for Efficient Encapsulation of Doxorubicin in Ferritin Nanocages for Targeted Drug Delivery. [Abstract]2023 May;19(21):e2205606. PMID: 36748864 -
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Int J Nanomedicine
Tumor Microenvironment Multiple Responsive Nanoparticles for Targeted Delivery of Doxorubicin and CpG Against Triple-Negative Breast Cancer. [Abstract]2022 Sep 20:17:4401-4417. PMID: 36164553 -
Br J Pharmacol
A novel individual-cell-based mathematical model based on multicellular tumour spheroids for evaluating doxorubicin-related delivery in avascular regions. [Abstract]2017 Sep;174(17):2862-2879. PMID: 28608595
Aldoxorubicin purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2017 Sep;174(17):2862-2879. [Abstract]
HSA decorated with Cy7 could be imaged. Through this strategy, the drug distribution of the HSA-decorated form and unbound form are imaged, and the merge rates are also calculated.
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Small Sci
2023 Aug;3(8):2300067. PMID: 38465197 -
Pharmaceutics
Evaluation of a Keratin 1 Targeting Peptide-Doxorubicin Conjugate in a Mouse Model of Triple-Negative Breast Cancer. [Abstract]2021 May 5;13(5):661. PMID: 34063098 -
Bioeng Transl Med
Nanoalbumin-prodrug conjugates prepared via a thiolation-and-conjugation method improve cancer chemotherapy and immune checkpoint blockade therapy by promoting CD8+ T-cell infiltration. [Abstract]2022 Jul 30;8(1):e10377. PMID: 36684090 -
ACS Biomater Sci Eng
MT3-KN035 Nanoparticles Based on PD-L1 Nanobodies Allow for Multiple Drug Conjugations that Promote Chemo- and Immunosynergistic Therapies. [Abstract]2026 Jun 23. PMID: 42334414 -
Int J Mol Sci
A Novel Homodimer Peptide-Drug Conjugate Improves the Efficacy of HER2-Positive Breast Cancer Therapy. [Abstract]2023 Feb 27;24(5):4590. PMID: 36902021 -
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Bioconjug Chem
Modular Synthesis of Anti-HER2 Dual-Drug Antibody-Drug Conjugates Demonstrating Improved Toxicity. [Abstract]2025 Feb 19;36(2):190-202. PMID: 39841105 -
Bioconjug Chem
2023 Sep 20;34(9):1585-1595. PMID: 37615599 -
Bioconjug Chem
Targeting Triple Negative Breast Cancer Cells with Novel Cytotoxic Peptide-Doxorubicin Conjugates. [Abstract]2019 Dec 18;30(12):3098-3106. PMID: 31715102 -
ACS Med Chem Lett
High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. [Abstract]2015 Jun 22;6(8):948-52. PMID: 26288699 -
Biotechnol J
Doxorubicin-Loaded Physalis Mottle Virus Particles Function as a pH-Responsive Prodrug Enabling Cancer Therapy. [Abstract]2020 Dec;15(12):e2000077. PMID: 32918857 -
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Oncotarget
Aldoxorubicin and Temozolomide combination in a xenograft mice model of human glioblastoma. [Abstract]2018 Oct 9;9(79):34935-34944. PMID: 30405885 -
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvent & Solubility
DMSO : ≥ 50 mg/mL (66.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cells are seeded at 1×105 cells/100 μL/well in 96-well plates in RPMI-1640 media with FBS for 24 hours before treatment. Cells are cultured in the presence of medium, Aldoxorubicin (INNO-206) or doxorubicin for 48 hours. Next, cell viability is quantified using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay. Each well is treated with MTS for 1 to 4 hours, after which absorbance at 490 nm is recorded using a 96-well plate reader. The quantity of formazan product as measured is directly proportional to the number of living cells. Data graphed are means±SEM using 3 replicates per data point.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For the LAGκ-1A experiment, Aldoxorubicin (INNO-206) is administered to SCID mice at 10.8 mg/kg (doxorubicin equivalent dose of 8.0 mg/kg) once weekly. Mice are treated with conventional doxorubicin at 4.0 and 8.0 mg/kg once weekly. For the LAGκ-2 experiment, Aldoxorubicin (INNO-206) is administered once weekly (W) at doses of 2.7 and 5.4 mg/kg, or on 3 consecutive days (W-F) weekly at doses of 0.9 and 1.8 mg/kg. PS-341 is administered twice weekly (W, F) at a dose of 0.5 mg/kg. Doxorubicin is administered to SCID mice at 2, 4, and 8 mg/kg, and PLD is administered to SCID mice at 2 mg/kg once weekly. Each drug is administered i.v. in a volume of 100 μL.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (583 KB)
- English - EN (583 KB)
- Français - FR (583 KB)
- Deutsch - DE (583 KB)
- Norwegian - NO (583 KB)
- Español - ES (583 KB)
- Swedish - SV (583 KB)
- Italian - IT (583 KB)
- Korean - KR (583 KB)
- Portuguese - PT (583 KB)
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Handling Instructions (2659 KB)
References
[3]. Graeser R, et al. INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model. Invest New Drugs. 2010 F [Content Brief]
[4]. Walker L, et al. Cell penetrating peptides fused to a thermally targeted biopolymer drug carrier improve the delivery and antitumor efficacy of an acid-sensitive doxorubicin derivative. Int J Pharm. 2012 Oct 15;436(1-2):825-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3320 mL | 6.6600 mL | 13.3200 mL | 33.3000 mL |
| 5 mM | 0.2664 mL | 1.3320 mL | 2.6640 mL | 6.6600 mL | |
| 10 mM | 0.1332 mL | 0.6660 mL | 1.3320 mL | 3.3300 mL | |
| 15 mM | 0.0888 mL | 0.4440 mL | 0.8880 mL | 2.2200 mL | |
| 20 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6650 mL | |
| 25 mM | 0.0533 mL | 0.2664 mL | 0.5328 mL | 1.3320 mL | |
| 30 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1100 mL | |
| 40 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8325 mL | |
| 50 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6660 mL | |
| 60 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5550 mL |
Aldoxorubicin Related Classifications
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