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。
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技术支持
免费溶解
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。 |
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 | |
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 |
|
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 |
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 |