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盐霉素 /Salinomycin {[allProObj[0].p_purity_real_show]}

货号:A721014 同义名: Procoxacin;from Streptomyces albus

Salinomycin(Procoxacin),一种多醚钾离子载体抗生素,选择性抑制革兰氏阳性细菌的生长,是Wnt/β-连环蛋白信号通路的强效抑制剂,阻断Wnt诱导的LRP6磷酸化。沙利霉素对人类癌症干细胞具有选择性活性。

Salinomycin 化学结构 CAS号:53003-10-4
Salinomycin 化学结构
CAS号:53003-10-4
Salinomycin 3D分子结构
CAS号:53003-10-4
Salinomycin 化学结构 CAS号:53003-10-4
Salinomycin 3D分子结构 CAS号:53003-10-4
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Salinomycin 纯度/质量文件 产品仅供科研

货号:A721014 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
Lys05 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。

Salinomycin 生物活性

描述 Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, both targets on human cancer stem cells and works as an an antibacterial and coccidiostat compound[1][2]. Salinomycin exhibited selective toxicity for mesenchymally transdifferentiated epithelial cells. Salinomycin reduced the proportion of CSCs by >100-fold relative to paclitaxel. Pretreatment with salinomycin resulted in a >100-fold decrease in tumor-seeding ability relative to paclitaxel pre-treatment for both the HMLER and 4T1 cancer lines. Daily intraperitoneal administration of 5mg/kg salinomycin delayed palpable tumor formation by 2 weeks in mice xenograft SUM159 cells, with increased necrosis and apoptosis, and focally expressed E-cadherin protein observed[1]. The killing CSCs activity of salinomycin is most likely by interfering with ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways[2]. The role of salinomycin involving in autophagy may also account for its anticancer effects[3].
作用机制 The effect of salinomycin on ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways, as well as autophagy, may contribute to the anticancer effects of salinomycin.[1][2][3]

Salinomycin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
BALB/3T3 cells Cytotoxicity assay 72 h Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50=28.08 μM 23079523
HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.29 μM 25644674
HL60/Vinc cells Cytotoxicity assay 72 h Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50=3.44 μM 23079523
HT-29 cells Proliferation assay 72 h Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.03 μM 25644674

Salinomycin 动物研究

Dose Mice[4] (i.p.): 1 mg/kg - 5 mg/kg; rat[5]: 20 mg/kg (s.c.), 80 mg/kg (p.o.)
Administration i.p., s.c., p.o.
Pharmacokinetics
Animal Mice[6]
Dose 5 mg/kg
Administration i.p.
MRT 83 min
T1/2 117 min
Tmax 0.5 h
Vz/F 6.85 l/kg
Cmax 1716 nmol/l
AUC0→∞ 2.07 mg/l/h
CL/F 2.43 l/kg/h

Salinomycin 参考文献

[1]Gupta PB, Onder TT, et al. Identification of selective inhibitors of cancer stem cells by high-throughput screening. Cell. 2009 Aug 21;138(4):645-659.

[2]Naujokat C, Steinhart R, et al. Salinomycin as a drug for targeting human cancer stem cells. J Biomed Biotechnol. 2012;2012:950658.

[3]Jiang J, Li H, et al. Salinomycin, as an autophagy modulator-- a new avenue to anticancer: a review. J Exp Clin Cancer Res. 2018 Feb 13;37(1):26.

[4]Ojo OO, Bhadauria S, et al. Dose-dependent adverse effects of salinomycin on male reproductive organs and fertility in mice. PLoS One. 2013 Jul 1;8(7):e69086.

[5]Dewangan J, Srivastava S, et al. Salinomycin: A new paradigm in cancer therapy. Tumour Biol. 2017 Mar;39(3):1010428317695035.

[6]Boehmerle W, Muenzfeld H, et al. Specific targeting of neurotoxic side effects and pharmacological profile of the novel cancer stem cell drug salinomycin in mice. J Mol Med (Berl). 2014 Aug;92(8):889-900.

Salinomycin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.33mL

0.27mL

0.13mL

6.66mL

1.33mL

0.67mL

13.32mL

2.66mL

1.33mL

Salinomycin 技术信息

CAS号53003-10-4
分子式C42H70O11
分子量 750.999
别名 Procoxacin;from Streptomyces albus;Salocin;Sacox;K 364;HSDB 7032;AHR 3096;Bio-cox;Coxistac
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 35 mg/mL(46.6 mM),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

动物实验配方
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