Aclacinomycin A hydrochloride(Synonyms: 盐酸阿柔比星; Aclarubicin hydrochloride)

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Aclacinomycin A hydrochloride (Synonyms: 盐酸阿柔比星; Aclarubicin hydrochloride) 纯度: 95.16%

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) 是一种荧光分子，是第一个发现对 20S 蛋白酶体 (20S proteasome) 的 CTRL (糜凝乳蛋白酶样) 活性具有离散特异性的非肽性抑制剂。同时也是 拓扑异构酶 I 和 II (topoisomerase I and II) 的双抑制剂。是一种有效蒽环类化疗试剂用于血癌和实体肿瘤的相关研究。

Aclacinomycin A hydrochloride(Synonyms: 盐酸阿柔比星; Aclarubicin hydrochloride)

Aclacinomycin A hydrochloride Chemical Structure

CAS No. : 75443-99-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4479 In-stock
5 mg ￥2800 In-stock
10 mg ￥4800 In-stock
25 mg ￥9800 In-stock
50 mg ￥16000 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome[1]. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II[2]. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors[3].

IC50 & Target

20S proteasome[1].
Topoisomerase I and II[2].
体外研究
(In Vitro)

Aclacinomycin A could efficiently enter living cells and emit fluorescence in situ. Aclacinomycin A (10 μM for 15 min) is sufficient for clear detection of fluorescence in most of the cultured cells. Aclacinomycin A treatment (10 μM Acla for 15 min) results in approximately 20% dead (or nearly dead) cells[1].
Aclacinomycin A (Aclarubicin) effectively induces incorporation of exon 7 into SMN2 transcripts from the endogenous gene in type I SMA fibroblasts as well as into transcripts from a SMN2 minigene in the motor neuron cell line NSC34 [2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Aclacinomycin A is very well absorbed in mice, rats, and dogs after its oral administration. The oral LD50 (76.5 mg/kg) is about twice the iv LD50 (35.6 mg/kg) in mice[4.
Aclacinomycin A (0.75-6 mg/kg, ip daily) dose-dependently exhibits tumor growth in mice-based Leukemia P-388 model[4.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DBA/2, CDF1 (BALB/c×DBA/2) mice with Leukemia P-388[4.
Dosage: 0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg.
Administration: Intraperitoneal administration daily for 10 days starting 3 hr after transplantation.
Result: Inhibited tumor growth.

Clinical Trial

分子量

848.33

Formula

C42H54ClNO15
CAS 号

75443-99-1
中文名称

盐酸阿柔比星
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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)
溶解性数据
In Vitro: 

DMSO : ≥ 125 mg/mL (147.35 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1788 mL 5.8939 mL 11.7879 mL
5 mM 0.2358 mL 1.1788 mL 2.3576 mL
10 mM 0.1179 mL 0.5894 mL 1.1788 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.45 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.45 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Isoe T, et al. Inhibition of different steps of the ubiquitin system by CDDP and aclarubicin. Biochim Biophys Acta. 1992 Sep 15;1117(2):131-5.

    [2]. Hajji N, et al. Induction of genotoxic and cytotoxic damage by aclarubicin, a dual topoisomerase inhibitor. Mutat Res. 2005 May 2;583(1):26-35.

    [3]. Iihoshi H, et al. Aclarubicin, an anthracycline anti-cancer drug, fluorescently contrasts mitochondria and reduces the oxygen consumption rate in living human cells. Toxicol Lett. 2017 Aug 5;277:109-114.

    [4]. Hori S, et al. Antitumor activity of new anthracycline antibiotics, aclacinomycin-A and its analogs, and their toxicity. Gan. 1977 Oct;68(5):685-90.