[CAS NO. 25316-40-9]  Doxorubicinhydrochloride

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PRODUCTS SPECIFICATIONS [25316-40-9]

Store
Catalog
HY-15142
Brand
MCE
CAS
25316-40-9

DESCRIPTION [25316-40-9]

Overview

MDLMFCD00077757
Molecular Weight579.98
Molecular FormulaC27H30ClNO11
SMILESCOC1=C2C(C(C(C(O)=C(C[C@](C(CO)=O)(O)C[C@@H]3O[C@@]4([H])C[C@H](N)[C@H](O)[C@H](C)O4)C3=C5O)=C5C2=O)=O)=CC=C1.[H]Cl

For research use only. We do not sell to patients.

261 Publications Citing Use of MCE


Summary

Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic , is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC 50 s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase . Doxorubicin hydrochloride induces apoptosis and autophagy [1] [2] [3] .


IC50 & Target

Topoisomerase I

0.8 μM (IC 50 )

Topoisomerase II

2.67 μM (IC 50 )

Daunorubicins/Doxorubicins

HIV-1


In Vitro

Doxorubicin hydrochloride (1-8 µM; 24 and 48 hours) decreases the viability of MCF-10F, MCF-7 and MDA-MB-231 cells in a time- and dose-dependent manner [4] .
Doxorubicin hydrochloride (1 μM; 3 and 24 hours) results in Hct-116 human colon carcinoma cells reduction in G0/G1 phase and accumulation in G2 phase [5] .
Doxorubicin hydrochloride (1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells; 48 hours) induces apoptosis by upregulating Bax, caspase-8 and caspase-3 and downregulation of Bcl-2 protein expression [4] .

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

Cell Viability Assay [4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 0, 1, 2, 4 and 8 μM
Incubation Time: 24 and 48 hours
Result: IC 50 was 1 μM for both MCF-10F and MDA-MB-231 cell lines.
IC 50 was 4 μM for MCF-7 cell line.

Cell Cycle Analysis [5]

Cell Line: Hct-116 human colon carcinoma cells
Concentration: 1 μM
Incubation Time: 3 hours and 24 hours
Result: Both, bolus (3 h) and continuous (24 h) incubation led to a significant reduction of cells in G0/G1 and accumulation in G2 phase.

Western Blot Analysis [4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells
Incubation Time: 48 hours
Result: Bax protein expression was upregulated in MCF-10F and MDA-MB-231 cell lines but MCF-7 cells did not show any significant increase.
Caspase-8 gene expression was upregulated in MCF-10F, but it was downregulated in MCF-7 and MDA-MB-231 cells.

In Vivo

Treatment with Doxorubicin (2 mg/kg) or Zoledronic acid (100 μg/kg) alone does not statistically significantly decrease final tumor volume compared with saline. Mice treated with Doxorubicin plus Zoledronic acid have statistically significantly smaller final tumor volumes than those treated with Doxorubicin alone [6] .

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

Animal Model: Female MF1 nu/nu mice bearing MDA-G8 breast tumor xenograft (6-week-old) [6]
Dosage: Doxorubicin (2 mg/kg); Zoledronic acid (100 μg/kg)
Administration: Intravenous injection; once a week; 6 weeks
Result: Moderate inhibition of subcutaneous tumor growth in mice that were treated with 2 mg/kg Doxorubicin alone or with 100 μg/kg Zoledronic acid alone compared to the saline control.
Mice treated with Zoledronic acid and Doxorubicin together had statistically significant smaller mean tumor volumes on day 42 than those treated with Doxorubicin alone.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04535713 Sarcoma Oncology Research Center, LLC
Sarcoma
September 30, 2020 Phase 2
NCT01078441 National Cancer Institute (NCI)
Refractory Multiple Myeloma
September 2010 Phase 2
NCT01796197 Dana-Farber Cancer Institute
Breast Cancer
August 2013 Phase 2

Appearance

Solid


Source

Streptomyces peucetius var. Caesius


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 35.71 mg/mL ( 61.57 mM ; ultrasonic and warming and heat to 60°C)

H 2 O : 20 mg/mL ( 34.48 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7242 mL 8.6210 mL 17.2420 mL
5 mM 0.3448 mL 1.7242 mL 3.4484 mL
10 mM 0.1724 mL 0.8621 mL 1.7242 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2.75 mg/mL (4.74 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

5,12-Naphthacenedione, 10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-, hydrochloride (1:1), (8S,10S)-
Adriamycin, hydrochloride
5,12-Naphthacenedione, 10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-, hydrochloride, (8S-cis)-
5,12-Naphthacenedione, 10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-, hydrochloride, (8S,10S)-
Doxorubicin hydrochloride
Adriamycin
Adriacin
Adriblastina RD
Adriblastina
Adriblastin
ADR
DOX HCl
FI 6804
ADM hydrochloride
Hydroxydaunorubicin hydrochloride
FI 106
Adriablastina CS
Lipo-Dox
Adrosal
Ameisu hydrochloride
Myocet liposomal
Doxolipad
Caelyx pegylated liposomal
Doxorubicin-TEVA
Doxorubicin-LANS