Art. -Nr.: HY-16261

Aldoxorubicin

(Synonyms: INNO-206; DOXO-EMCH)

22 Cited Publications

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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.

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Reinheit: 95.56%
CAS. Nr.: 1361644-26-9
Formel: C₃₇H₄₂N₄O₁₃
Molecular Weight:750.75

Speicherung:

-80°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Aldoxorubicin Chemical Structure

CAS. Nr.: 1361644-26-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Topoisomerase II^[4]

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

Alle ADC Payloads Isoform-spezifische Produkte anzeigen :

In Vitro

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.

In Vivo

Aldoxorubicin (INNO-206) (10.8 mg/kg, i.v.) shows significantly smaller tumor volumes and IgG levels on days 28, and is well tolerated with 90% of mice surviving until the termination of the study in the mice bearing the LAGκ-1A tumor^[1]. Aldoxorubicin (INNO-206) shows a good safety profile at doses up to 260 mg/mL doxorubicin equivalents, and is able to induce tumor regressions in breast cancer, small cell lung cancer and sarcoma in phase I study^[2]. Aldoxorubicin (INNO-206) shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1361644-26-9
Appearance Solid
Molecular Weight 750.75
Formel C₃₇H₄₂N₄O₁₃
Color Brown to red
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
Synonyms

INNO-206; DOXO-EMCH
Versand

Shipping with dry ice.
Speicherung

-80°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (22)

All In Vivo Efficacy StudyIF

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Journal Impact Factor

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

Doxorubicin-conjugated siRNA lipid nanoparticles for combination cancer therapy. [Abstract]

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.
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
Nano Res

08 February 2022.
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.
Small Sci

iRGD-targeted Physalis Mottle Virus-like Nanoparticles for Targeted Cancer Delivery. [Abstract]

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
J Drug Deliv Sci Technol

2020, 102048.
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

Physalis Mottle Virus-Like Nanocarriers with Expanded Internal Loading Capacity. [Abstract]

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
Patent

US20220298225A1.
Patent

US20200376013A1.
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

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3320 mL

6.6600 mL

13.3200 mL

5 mM

0.2664 mL

1.3320 mL

2.6640 mL

10 mM

0.1332 mL

0.6660 mL

1.3320 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Eric Sanchez, et al. Anti-Myeloma Effects of the Novel Anthracycline Derivative INNO-206. Clin Cancer Res.2012 18; 3856.

[2]. Kratz, F. INNO-206 (DOXO-EMCH), an Albumin-Binding Prodrug of Doxorubicin Under Development for Phase II Studies. Current Bioactive Compounds, 2011, 7(1): 33-38(6)

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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
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

Keywords

Aldoxorubicin

22 Cited Publications

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Aldoxorubicin

Toxins for Antibody-Drug Conjugate Research Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Aldoxorubicin

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aldoxorubicin

Toxins for Antibody-Drug Conjugate Research Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Aldoxorubicin

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (22)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Aldoxorubicin Related Classifications

HY-16261 Related Classifications