EL-102

CAS: 1233948-61-2 货号: E656591 分子式: C19H16N2O3S2 分子量: 384.47 PubChem CID: 62705067
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级别和纯度: Moligand™ ? Moligand™ —— 阿拉丁的配体和生物活性小分子系列。适用于需要明确小分子工具的受体、通路和结合研究。 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
1ml
E656591-1ml
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¥1,899.90
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Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis , inhibits tubulin polymerisation and shows activities against prostate cancer . EL-102 can be used for the research of cancer

In Vitro

EL-102 (0-120 nM; 72 h) inhibits prostate cancer cells proliferation in vitro. EL-102 (0-100 nM; 72 h) shows cytotoxicity to prostate cancer cell lines. EL-102 (10-100 nM; 24-72 h) induces cellular apoptosis and affects cell cycle. EL-102 (10-100 nM; 24-48 h) affects PARP cleavage in DU145 cells. EL-102 (5 nM; 0-60 min) inhibits tubulin polymerisation activity. EL-102 (0-100 nM; 1 hour) inhibits Hif1α protein expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines Concentration: 0-120 nM Incubation Time: 72 hours Result: Inhibited proliferation of CWR22, 22Rv1, DU145, PC-3, DLKP and doxorubicin-selected variant DLKPA cells with IC 50 s of 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively. Cell Cytotoxicity AssayCell Line: CWR22, 22Rv1, DU145 and PC-3 cell lines Concentration: 0-100 nM Incubation Time: 72 hours Result: Exibited cytotoxicity to prostate cancer cell lines, and showed no additive effect on the inhibition of cell viability with docetaxel. Apoptosis AnalysisCell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines Concentration: 10 and 100 nM Incubation Time: 24, 48 and 72 hours Result: Induced cell apoptosis to inhibits cell viability with a dose of 100 nM. Western Blot AnalysisCell Line: DU145 cell line Concentration: 10 and 100 nM Incubation Time: 24 and 48 hours Result: Increased PARP cleavage in DU145 cells and showed a more dramatic effect with docetaxel adding. Cell Cycle AnalysisCell Line: DU145 cell line Concentration: 10 and 100 nM Incubation Time: 24, 48 and 72 hours Result: Increased loss of cells from G1 phase and accumulated cells in G2/M phase. Western Blot AnalysisCell Line: Prostate cancer cells Concentration: 10 , 50 and 100 nM Incubation Time: 24 and 48 hours Result: Modestly inhibited Hif1α expression at doses of 50 and 100 nM in normoxia.

In Vivo

EL-102 (12 and 15 mg/kg; p.o. 5-day on and 2-day off, from 13 to 37 days after tumour transplantation) potentiates effects of docetaxel in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice with CWR22 xenografts Dosage: 12 and 15 mg/kg Administration: Oral gavage; 12 and 15 mg/kg 5-day on and 2-day off; from 13 to 37 days after tumour transplantation Result: Showed no effect on tumor growth, but enhanced the effect of docetaxel on tumor .

IC50& Target:IC50: 24 nM (CWR22), 21.7 nM (22Rv1), 40.3 nM (DU145), 37.0 nM (PC-3), 14.4 nM (DLKP), 16.3 nM (DLKPA)

规格

规格或纯度
Moligand™, 10mM in DMSO
英文名称
EL-102
生化机理
EL-102 是一种缺氧诱导因子 1(Hif1α)抑制剂。EL-102 可诱导细胞凋亡,抑制微管蛋白聚合,并对前列腺癌有抑制作用。EL-102 可用于癌症研究。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=C(C=C(C=C1)C2=CSC(=C2)C#N)NS(=O)(=O)C3=CC=C(C=C3)OC
PubChem CID
分子量
384.47

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