Acriflavine
(Synonyms: 吖啶黄; Acriflavinium chloride 3,6-Acridinediamine mix) 目录号 : GC32083
Acriflavine是用于标记高分子量RNA的荧光染料。它也是一种局部防腐剂。
Cas No.:8048-52-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice: CML mice are treated daily with acriflavine (8 mg/kg) or PBS via intraperitoneal injection, for 10 days starting from day 7 after bone marrow transplantation[2]. |
References: [1]. Voss DM, et al. Disruption of the monocarboxylate transporter-4-basigin interaction inhibits the hypoxic response, proliferation, and tumor progression. Sci Rep. 2017 Jun 27;7(1):4292. | |
Acriflavine is a fluorescent dye for labeling high molecular weight RNA. It is also a topical antiseptic.
Acriflavine is identified as a potent inhibitor of the MCT4 that can inhibit the binding between Basigin and MCT4. Acriflavine significantly inhibits growth and self-renewal potential of several glioblastoma neurosphere lines[1]. The HIF-1 inhibitor acriflavine decreases survival and growth of CML cells. It targets stem cell potential of CML cells[2].
Acriflavine treatment inhibits intratumoral expression of VEGF and tumor vascularization[1]. In a murine CML model, acriflavine decreases leukemia development and reduces LSC maintenance[2]. Acriflavine retards tumor growth in a murine model of breast cancer. The combination of sunitinib with acriflavine significantly decreases vascular endothelial growth factor and TGF-β expression and reduces tumor vasculature followed by increased intratumor necrosis and apoptosis[3].
[1]. Voss DM, et al. Disruption of the monocarboxylate transporter-4-basigin interaction inhibits the hypoxic response, proliferation, and tumor progression. Sci Rep. 2017 Jun 27;7(1):4292. [2]. Cheloni G, et al. Targeting chronic myeloid leukemia stem cells with the hypoxia-inducible factor inhibitor acriflavine. Blood. 2017 Jun 2. pii: blood-2016-10-745588. [3]. Yin T, et al. HIF-1 Dimerization Inhibitor Acriflavine Enhances Antitumor Activity of Sunitinib in Breast Cancer Model. Oncol Res. 2014;22(3):139-45.
| Cas No. | 8048-52-0 | SDF | |
| 别名 | 吖啶黄; Acriflavinium chloride 3,6-Acridinediamine mix | ||
| Canonical SMILES | NC(C=C1)=CC(C1=C2)=NC3=C2C=CC(N)=C3.NC(C=C4)=CC(C4=C5)=[N+](C)C6=C5C=CC(N)=C6.[Cl-] | ||
| 分子式 | C14H14ClN3 | 分子量 | 259.73 |
| 溶解度 | Water : ≥ 25 mg/mL (96.25 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8502 mL | 19.2508 mL | 38.5015 mL |
| 5 mM | 0.77 mL | 3.8502 mL | 7.7003 mL |
| 10 mM | 0.385 mL | 1.9251 mL | 3.8502 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Proflavine/Acriflavine derivatives with versatile biological activities
J Appl Toxicol 2020 Jan;40(1):64-71.PMID:31222780DOI:10.1002/jat.3818.
Proflavine derivatives are extremely interesting chemotherapeutic agents, which have shown promising pharmaceutical potential due to their wide range of biological activities. This review summarizes the current state of research into the anticancer, antimicrobial, antimalarial and antileishmanial properties of these attractive compounds. Our attention has focused on new classes of proflavine conjugates, which display significant levels of anticancer activity. Highly promising cytotoxic properties have been identified in proflavine conjugates with imidazolidinones, ureas and thioureas. In particular, proflavine-dialkyldithioureas displayed substantial cytotoxic effect against the human leukemia HL-60 cells with IC50 values from 7.2 to 34.0 μm. As well, palladium complexes with proflavine ligand have important biologic activity. The LC50 values of these complexes were significantly lower than that of cisplatin against the SK-BR-3 cell line.
Acriflavine, an Acridine Derivative for Biomedical Application: Current State of the Art
J Med Chem 2022 Sep 8;65(17):11415-11432.PMID:36018000DOI:10.1021/acs.jmedchem.2c00573.
Acriflavine (ACF) has been known for years as an antibacterial drug. The identification of key oncogenic mechanisms has brought, in recent years, a significant increase in studies on ACF as a multipurpose drug that would improve the prognosis for cancer patients. ACF interferes with the expression of the hypoxia inducible factor, thus acting on metastatic niches of tumors and significantly enhancing the effects of other anticancer therapies. It has been recognized as the most potent HIF-1 inhibitor out of the 336 drugs approved by the FDA. This work presents up-to-date knowledge about the mechanisms of action of ACF and its related prodrug systems in the context of anticancer and SARS-CoV-2 inhibitory properties. It explains the multitask nature of this drug and suggests mechanisms of ACF's action on the coronavirus. Other recent reports on ACF-based systems as potential antibacterial and antiviral drugs are also described.
Acriflavine in aqueous solution: excitation and hydration
J Mol Model 2022 Jun 20;28(7):194.PMID:35723744DOI:10.1007/s00894-022-05182-z.
Using TD-DFT/DFT, the ground and excited states of the Acriflavine dye were studied in an aqueous medium. The mutual influence of photoexcitation and strong hydrogen bonds with the solvent was studied by comparing the purely implicit and combined modeling of the aqueous environment of the dye. The excitation of Acriflavine was calculated considering the vibronic coupling. The effect of photoexcitation on dye vibrations was analyzed. The spatial structure of the Acriflavine H-dimer was obtained and its absorption was estimated.
Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses
Cell Chem Biol 2022 May 19;29(5):774-784.e8.PMID:35021060DOI:10.1016/j.chembiol.2021.11.006.
The COVID-19 pandemic caused by SARS-CoV-2 has been socially and economically devastating. Despite an unprecedented research effort and available vaccines, effective therapeutics are still missing to limit severe disease and mortality. Using high-throughput screening, we identify Acriflavine (ACF) as a potent papain-like protease (PLpro) inhibitor. NMR titrations and a co-crystal structure confirm that Acriflavine blocks the PLpro catalytic pocket in an unexpected binding mode. We show that the drug inhibits viral replication at nanomolar concentration in cellular models, in vivo in mice and ex vivo in human airway epithelia, with broad range activity against SARS-CoV-2 and other betacoronaviruses. Considering that Acriflavine is an inexpensive drug approved in some countries, it may be immediately tested in clinical trials and play an important role during the current pandemic and future outbreaks.
Repurposing of Acriflavine to Target Chronic Myeloid Leukemia Treatment
Curr Med Chem 2021;28(11):2218-2233.PMID:32900342DOI:10.2174/0929867327666200908114411.
Drug repurposing has lately received increasing interest in several diseases especially in cancers, due to its advantages in facilitating the development of new therapeutic strategies, by adopting a cost-friendly approach and avoiding the strict Food and Drug Administration (FDA) regulations. Acriflavine (ACF) is an FDA approved molecule that has been extensively studied since 1912 with antiseptic, trypanocidal, anti-viral, anti-bacterial and anti-cancer effects. ACF has been shown to block the growth of solid and hematopoietic tumor cells. Indeed, ACF acts as an inhibitor of various proteins, including DNA-dependent protein kinases C (DNA-PKcs), topoisomerase I and II, hypoxia-inducible factor 1α (HIF-1α), in addition to its recent discovery as an inhibitor of the signal transducer and activator of transcription (STAT). Chronic myeloid leukemia (CML) is a clonal myeloproliferative disorder characterized by the expression of the constitutively active tyrosine kinase BCR-ABL. This protein allows the activation of several signaling pathways known for their role in cell proliferation and survival, such as the JAK/STAT pathway. CML therapy, based on tyrosine kinase inhibitors (TKIs), such as imatinib (IM), is highly effective. However, 15% of patients are refractory to IM, where in some cases, 20-30% of patients become resistant. Thus, we suggest the repurposing of ACF in CML after IM failure or in combination with IM to improve the anti-tumor effects of IM. In this review, we present the different pharmacological properties of ACF along with its anti-leukemic effects in the hope of its repurposing in CML therapy.