ARN-21934 | Topoisomerase IIα Inhibitor | AmBeed-信号通路专用抑制剂

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ARN-21934 {[allProObj[0].p_purity_real_show]}

货号：A1534057

ARN-21934是一种高选择性、具有良好血脑屏障 (BBB) 通透性的人的拓扑异构酶 II α (human topoisomerase II α) 抑制剂。ARN-21934 对 DNA 松弛的 IC50 为 2 μM，相比抗癌药物依托泊苷 (Etoposide; IC50=120 μM) 更为有效，并且在体内表现出良好的药代动力学特性，是一种有前途的抗癌先导化合物。

ARN-21934 化学结构
CAS号：2230854-93-8

ARN-21934 3D分子结构
CAS号：2230854-93-8

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ARN-21934 纯度/质量文件产品仅供科研

货号：A1534057 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

拓扑异构酶亚型比较

产品名称	Topo I ↓ ↑	Topo II ↓ ↑	Topo IV ↓ ↑	Topoisomerase ↓ ↑	其他靶点	纯度
Ellagic acid	✔					98%
β-Lapachone	✔					99%+
(s)-10-hydroxycamptothecin	✔					98+%
Camptothecin	++ Topo I, IC50: 0.68 μM					98%
Betulinic acid	++ Eukaryotic topoisomerase I, IC50: 5 μM					98%
Topotecan	++++ Topo I (MCF-7 Luc cells), IC50: 13 nM Topo I (DU-145 Luc cells), IC50: 2 nM					98%
Irinotecan HCl Trihydrate	✔					98%
SN-38	✔					98%
Levofloxacin hydrate		✔				98%
Dexrazoxane		✔				99%+
Ofloxacin		✔				98+%
Enoxacin		✔				99%+
Flumequine		+ Topo II, IC50: 15 μM				98%
Levofloxacin		✔				97%
Etoposide		✔				98%
Pefloxacin mesylate dihydrate		✔				99.5%
Marbofloxacin		✔				98+%
Voreloxin HCl		✔				98%
Mitoxantrone 2HCl		✔			PKC	98%
Nalidixic acid		✔				98%
Doxorubicin		✔				97%
Novobiocin sodium		✔				95%
Amonafide		✔				99%+
Pirarubicin		✔				98%+
Idarubicin HCl		+++ Topo II (MCF-7 cells), IC50: 3.3 ng/mL				99%+
Genistein		✔			EGFR	98%
Teniposide		✔				98%
Moxifloxacin		✔				98%
Ciprofloxacin			✔			98%
Clinafloxacin			✔			99%
Gatifloxacin				✔		98%
Daunorubicin HCl				+++ DNA synthesis, Ki: 20 nM		98%
Epirubicin HCl				✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ARN-21934 生物活性

描述

ARN-21934 is a highly selective, blood-brain barrier (BBB) penetrant inhibitor of human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM compared to Etoposide (IC50=120 μM). ARN-21934 demonstrates favorable in vivo pharmacokinetics and holds promise as a lead compound for anticancer research ^[1].

体内研究

ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) achieves a maximal plasma concentration of 0.68 μg/mL after 15 minutes. It exhibits a half-life of 149 minutes in circulation, remaining detectable in plasma 360 minutes post-injection. Moreover, ARN-21934 penetrates the brain, reaching maximum concentration at 60 minutes and remaining present for 360 minutes post-injection ^[1].

体外研究

ARN-21934 exhibits differential affinity for topoIIα and topoIIβ. It is more potent against the α isoform, with an IC50 value of 2 μM for DNA relaxation inhibition by topoIIα and 120 μM for topoIIβ ^[1].

ARN-21934 demonstrates activity against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells, with IC50 values ranging from 8.1 to 38.2 μM in a small panel of human cancer cell lines^[1].

ARN-21934 参考文献

[1]Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

ARN-21934 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.87mL

2.77mL

1.39mL

27.74mL

5.55mL

2.77mL

ARN-21934 技术信息

CAS号	2230854-93-8
分子式	C₂₁H₂₄N₆
分子量	360.46
SMILES Code	NC1CC2=C(NC3=CC=C(N(C)C)C=C3)N=C(C4=CC=NC=C4)N=C2CC1
MDL No.	MFCD34179494

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 7 mg/mL(19.42 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

ARN-21934 {[allProObj[0].p_purity_real_show]}

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ARN-21934 {[allProObj[0].p_purity_real_show]}

ARN-21934 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ARN-21934 质控信息

ARN-21934 生物活性

ARN-21934 参考文献

ARN-21934 实验方案

ARN-21934 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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ARN-21934 纯度/质量文件产品仅供科研