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產地	進口	級別	其他

注：本產品僅用于科研，不可用于臨床

生物活性

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 IC₅₀s 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^[1]^[2]^[3]

Topoisomerase I

0.8 μM (IC₅₀)

Topoisomerase II

2.67 μM (IC₅₀)

Daunorubicins/Doxorubicins

HIV-1

體外研究
(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:	IC₅₀ was 1 μM for both MCF-10F and MDA-MB-231 cell lines. IC₅₀ was 4 μM for MCF-7 cell line.

體內研究
(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

分子量

579.98

性狀

Solid

Formula

C₂₇H₃₀ClNO₁₁

CAS 號

25316-40-9

中文名稱

結構分類

Quinones
Anthraquinones

來源

Streptomyces peucetius var. Caesius

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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)

溶解性數據

In Vitro:

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

H₂O : 20 mg/mL (34.48 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質量	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

請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

請根據您的實驗動物和給藥方式選擇適當的溶解方案。以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.75 mg/mL (4.74 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution