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Doxorubicin hydrochloride

SKU: orb1225510

Description

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. (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.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.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.(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.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number25316-40-9
MW579.99
Purity>98% (HPLC)
FormulaC27H29NO11·HCl
SMILESC[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O.Cl
TargetTopoisomerase
SolubilityWater: 20 mg/mL (34.48 mM); DMSO: 100 mg/mL warmed (172.41 mM)

Bioactivity

In Vivo
Animal model: Female MF1 nu/nu mice bearing MDA-G8 breast tumor xenograft (6-week-old). 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. Animal model: Male Sprague-Dawley rats. Dosage: 1%, 2%, 4%, 5%, 6%, 10%, 20%. Administration: Intrastriatal injection; Single dose. Result: In doses of 4, 5, 6, 10 or 20% caused obvious loss of ipsilateral SNc and VTA neuronsz and doses of 1 or 2% failed to produce obvious neuron loss.
In Vitro
Cell Viability Assay 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: IC50 was 1 μM for both MCF-10F and MDA-MB-231 cell lines. IC50 was 4 μM for MCF-7 cell line. Cell Cycle Analysis 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. 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

DOX

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Doxorubicin hydrochloride (orb1225510)

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