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Lonidamine (AF-1890), 类似线粒体丙酮酸载体 1 的抑制剂;线粒体丙酮酸载体 2 的抑制剂

Carbohydrate Metabolism Modulators
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货号 (SKU) 包装规格 是否现货 价格 数量
L409034-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

别名 氯尼达明 (AF-1890)
英文别名 Diclondazolic Acid, DICA | 1-​[(2,​4-​dichlorophenyl)​methyl]​-1H-​indazole-​3-​carboxylic acid
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Lonidamine (AF-1890)
生化机理 洛尼达明(AF 1890,Diclondazolic Acid,DICA)是一种口服小分子己糖激酶灭活剂。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 类似线粒体丙酮酸载体 1 的抑制剂;线粒体丙酮酸载体 2 的抑制剂
产品介绍


Information

Lonidamine (AF-1890) Lonidamine (AF 1890, Diclondazolic Acid, DICA) is an orally administered small molecule hexokinase inactivator.
In vitro

Lonidamine reduces the oxygen consumption in both normal and neoplastic cells, while it increases the aerobic glycolysis of normal cells but inhibited that of tumor cells. Lonidamine induces the permeabilization of ANT proteoliposomes in a cell-free system, yet has no effect on protein-free liposomes. Lonidamine adds to synthetic planar lipid bilayers containing ANT, eliciting ANT channel activities with clearly distinct conductance levels. Lonidamine provokes a disruption of the mitochondrial transmembrane potential which precedes signs of nuclear apoptosis and cytolysis. Lonidamine causes the dissipation of the mitochondrial inner transmembrane potential and the release of apoptogenic factors capable of inducing nuclear apoptosis in vitro. Lonidamine (50 mg/mL) induces apoptosis in adriamycin and nitrosourea-resistant cells (MCF-7 ADR(r) human breast cancer cell line, and LB9 glioblastoma multiform cell line), as demonstrated by sub-G1 peaks in DNA content histograms, condensation of nuclear chromatin, and internucleosomal DNA fragmentation. Lonidamine has a stronger effect on glioblastoma cell proliferation and metabolism in vitro than did either agent used alone.

In vivo

Lonidamine (160 mg/kg) combined with Diazepam is significantly more effective in reducing glioblastoma tumor growth than either drug alone in mice, this tumor growth retardation is maintained as long as treatment is given.
Cell Data

cell lines:T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, LNCaP, etc.

Concentrations:

Incubation Time:

Powder Purity:≥97%

关联靶点(人)

MPC2 Tbio 线粒体丙酮酸载体2(Mitochondrial pyruvate carrier 2) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MPC1L Tdark 线粒体丙酮酸载体1类蛋白(Mitochondrial pyruvate carrier 1-like protein) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

EC号 256-510-0
Isomeric SMILES C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O
关联CAS 50264-69-2
NSC Number 741419
MeSH Entry Terms 1-(2,4-dichlorobenzyl)indazole-3-carboxylic acid;AF 1890;diclondazolic acid;lonidamine
分子量 321.16
Reaxy-Rn 894483
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=894483&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro      
熔点 210 °C

安全和危险性(GHS)

象形图 GHS08,   GHS07
信号词 Danger
危险声明

H351: 怀疑引起遗传缺陷

H302: 吞食有害

H360: 可能损害生育力或未出生的孩子

预防措施声明

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P330: 漱口

P203: 使用前,获取、阅读并遵守所有安全说明。

P301+P317: 如果被吞咽:请寻求医疗帮助。

P318: 如果暴露或担心,请就医。

WGK Germany 3

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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