|(R)-2-((2R,5S,6R)-6-((2S,3S,4S,6R)-6-((2S,5S,7R,9S,10S,12R,15R)-2-((2R,5R,6S)-5-乙基-5-羟基-6-甲基四氢-2H-吡喃-2-基)-15-羟基-2,10,12-三甲基-1,6,8-三恶二螺[4.1.57.35]五癸基-13-烯-9-基)-3-羟基-4-甲基-5-氧代辛基-2-基)-5-甲基四氢-2H-吡喃-2-基)丁酸|CsnPharm

CAS No.: 53003-10-4

Salinomycin/盐霉素 Catalog No. CSN11885

Synonyms: Procoxacin;AHR-3096;HSDB-7032

Salinomycin, an antibiotic potassium ionophore, is an anti-coccidial drug and an autophagy modulator. It is also an inhibitor of Wnt/β-catenin signaling.

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靶点选择性

生物活性

实验方案

技术信息

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]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究

剂量

Mice^[4] (i.p.): 1 mg/kg - 5 mg/kg; rat^[5]: 20 mg/kg (s.c.), 80 mg/kg (p.o.)

给药途径

i.p., s.c., p.o.

动物药代数据

Animal	Mice^[6]
Dose	5 mg/kg
Administration	i.p.
MRT	83 min
T_1/2	117 min
T_max	0.5 h
V_z/F	6.85 l/kg
C_max	1716 nmol/l
AUC_0→∞	2.07 mg/l/h
CL/F	2.43 l/kg/h

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.3316 mL
- 6.6578 mL
- 13.3156 mL
- 5 mM
- 0.2663 mL
- 1.3316 mL
- 2.6631 mL
- 10 mM
- 0.1332 mL
- 0.6658 mL
- 1.3316 mL

技术信息

CAS号

53003-10-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C42H70O11

运输

蓝冰

分子量

751.00

别名

Procoxacin;AHR-3096;HSDB-7032;K 364;BioCox;Sacox;Salocin;Coxistac;盐霉素

溶解度

DMSO	400.0 mg/mL (532.6 mM)
Water	insoluble

动物实验配方

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Salinomycin/盐霉素 Catalog No. CSN11885

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