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编 号:F293968
分子式:C27H30ClNO11
分子量:579.98
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10mM*1mL in DMSO
890
In-stock
50mg
720
In-stock
100mg
1280
In-stock
200mg
2400
In-stock
500mg
4000
In-stock
1g
5760
In-stock
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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.

体内研究:
Doxorubicin hydrochloride 可用于动物建模,构建动物心衰模型。与生理盐水相比,单独使用 Doxorubicin hydrochloride (2 mg/kg) 或唑来膦酸 (100 μg/kg) 处理不会显著降低最终肿瘤体积。接受 Doxorubicin hydrochloride 加唑来膦酸处理的小鼠的最终肿瘤体积明显小于仅接受 Doxorubicin hydrochloride 处理的小鼠。Doxorubicin (4%- 20%; Intrastriatal 注射; 单剂量) 在 Sprague-Dawley 小鼠中具有神经毒性。Doxorubicin 在酸性条件下可以通过 PH-敏感键偶联在金纳米颗粒 (Au NPs) 上面,从而能通过血脑屏障,最大的吸收波长为 528 nm。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.

体外研究:
盐酸 Doxorubicin hydrochloride (1-8 μM;24 和 48 小时) 以时间和剂量依赖性方式降低 MCF-10F、MCF-7 和 MDA-MB-231 细胞的活力。 Doxorubicin hydrochloride (1 μM;3 和 24 小时) 导致 Hct-116 人结肠癌细胞在 G0/G1 期减少和在 G2 期积累。盐酸 Doxorubicin hydrochloride (MCF-10F 和 MDA-MB-231 细胞为 1 μM,MCF-7 细胞为 4 μM;48 小时) 通过上调 Bax、caspase-8 和 caspase-3 以及下调 Bcl-2 蛋白表达诱导细胞凋亡。Doxorubicin 可以标记神经元细胞,且罗丹明滤袋下呈鲜红色,在儿茶酚胺滤袋下呈淡红橙色。Doxorubicin (5 μM; 10-30 分钟) 在 B16-F10 黑色素瘤细胞系 CRL-6475 细胞中能以时间依赖方式在细胞中积累,且可以通过绿色或红色荧光来进行检测 (绿色荧光的检测灵敏度更高), 最大激发波长 (λex) 和最大发射波长为 (λem) 分别为 470 nm 和 560 nm.
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