货号:A258178
同义名:
Artesunic Acid; WR-256283
Artesunate 是一种青蒿素类化合物,对于小细胞肺癌细胞系H69的IC50值为<5 μM,是STAT-3和EXP1的潜在抑制剂,在体外对癌细胞有选择性细胞毒性。


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| 产品名称 | STAT1 ↓ ↑ | STAT3 ↓ ↑ | STAT5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Nifuroxazide | ✔ | 98% | |||||||||||||||||
| Fludarabine | ✔ | 98% | |||||||||||||||||
| Artesunate | ✔ | 98% | |||||||||||||||||
| BP-1-102 |
+++
STAT3, Kd: 504 nM |
99%+ | |||||||||||||||||
| Niclosamide |
++
STAT3, IC50: 0.7 μM |
98% | |||||||||||||||||
| Napabucasin | ✔ | 98% | |||||||||||||||||
| Cryptotanshinone |
++
STAT3, IC50: 4.6 μM |
98% | |||||||||||||||||
| Stattic |
+
STAT3, IC50: 5.1 μM |
98% | |||||||||||||||||
| NSC 74859 |
+
STAT3, IC50: 86 μM |
99%+ | |||||||||||||||||
| Ochromycinone | ✔ | 98% | |||||||||||||||||
| HO-3867 | ✔ | 97% | |||||||||||||||||
| C188-9 |
++++
STAT3, Kd: 4.7 nM |
99%+ | |||||||||||||||||
| HJC0152 | ✔ | 99% | |||||||||||||||||
| SH5-07 | ✔ | 95% | |||||||||||||||||
| SH-4-54 |
++++
STAT3, Kd: 300 nM |
+++
STAT5, Kd: 464 nM |
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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Artesunate is a semisynthetic analogue of artemisinin, extracted from the sweet wormwood plant. Artesunate reduced cell growth with IC50 values from 0.189 to 3.72 μM[2]. Moreover, both the antiproliferative and antiviral effects of artesunate at 10 μM were reversible[3]. In vivo, the artesunate dose (200 mg/kg/day) was well tolerated with no body weight loss during treatment and artesunate showed potent anti-tumor response in an aggressive B-cell lymphoma xenograft model [2]. |
| Concentration | Treated Time | Description | References | |
| HepG2R cells | 25 µM | 24 hours | Artesunate significantly enhanced the inhibitory effects of sorafenib on the growth of resistant cells and induced apoptosis. | Autophagy. 2024 Mar;20(3):541-556. |
| BMDM cells | 2 and 10 μg/ml | 24 h | ART administration strongly reduced the mRNA expression of IL-1β, IL-6, TNF-α and iNOS in LPS-stimulated BMDM cells | J Cell Mol Med. 2021 Sep;25(18):8775-8788. |
| mTEC cells | 2 and 10 μg/ml | 24 h | ART effectively alleviated LPS-induced necroptosis through Annexin V staining | J Cell Mol Med. 2021 Sep;25(18):8775-8788. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | High-fat diet-induced obese mice | Intraperitoneal injection | 20 mg/kg | Every two days for 3 weeks | Artesunate reduced food intake and promoted weight loss through the GDF15/GFRAL signalling axis | Nat Commun. 2024 Feb 3;15(1):1034 |
| BALB/c Nude mice | Sorafenib-resistant orthotopic xenograft HCC model | Oral | 30 or 60 mg/kg/2 days | Every 2 days for 8 weeks | Artesunate significantly slowed down the growth of sorafenib-resistant tumors and extended the overall survival of drug-resistant mice. | Autophagy. 2024 Mar;20(3):541-556. |
| Nude mice | Patient-derived xenograft model | Intraperitoneal injection | 5-ALA (80 mg/kg), Artesunate (40 mg/kg) | 5 times per week for 5 weeks | The combination of 5-ALA and artesunate significantly inhibited tumor growth in patient-derived xenograft models. | EMBO Mol Med. 2023 Mar 8;15(3):e16959 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00722150 | Falciparum Malaria | Not Applicable | Completed | - | Cambodia ... 展开 >> Tasanh Health Center Sam Lot District, Battambang, Cambodia 收起 << |
| NCT01074905 | Vivax Malaria | Phase 3 | Completed | - | Thailand ... 展开 >> Shoklo Malaria Research Unit Mae Sot, Thailand 收起 << |
| NCT01240603 | - | Completed | - | Cambodia ... 展开 >> National Center for Parasitology, Entomology, and Malaria Controk, Ministry of H Phnom Penh, Cambodia 收起 << | |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
13.01mL 2.60mL 1.30mL |
26.01mL 5.20mL 2.60mL |
|
| CAS号 | 88495-63-0 |
| 分子式 | C19H28O8 |
| 分子量 | 384.42 |
| SMILES Code | O=C(O)CCC(O[C@H]1O[C@@]2([H])[C@@]3(OO[C@](O2)(C)CC4)[C@]4([H])[C@H](C)CC[C@@]3([H])[C@H]1C)=O |
| MDL No. | MFCD00866204 |
| 别名 | Artesunic Acid; WR-256283; HSDB-7458; SM-804; Armax 200; NSC 712571 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 85 mg/mL(221.11 mM),配合低频超声助溶,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 以下溶解方案都请先按照体外实验的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
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