YK-4-279

YK-4-279是EWS-FLI1RNA helicase A (RHA)结合的有效抑制剂。

YK-4-279 Chemical Structure

YK-4-279 Chemical Structure

CAS: 1037184-44-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 810.81 现货
10mg RMB 810.04 现货
50mg RMB 2600.09 现货
200mg RMB 6932.83 现货
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客户使用Selleck的YK-4-279发表文献11

客户使用该产品的1个实验数据

产品质控

批次: 纯度: 99.93%
99.76

YK-4-279相关产品

DNA/RNA Synthesis抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
TC71 Growth inhibition assay 3 days Growth inhibition of human TC71 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.92μM 25432018
TC32 Growth inhibition assay 3 days Growth inhibition of human TC32 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay, GI50=0.94μM 25432018
COS7 Function assay Inhibition of transcriptional activity of full-length EWS-FLI1 (unknown origin) expressed in COS7 cells by NR0B1-luciferase reporter gene assay, IC50=0.35μM 25432018
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 YK-4-279是EWS-FLI1RNA helicase A (RHA)结合的有效抑制剂。
靶点
RHA [1]
体外研究(In Vitro)
体外研究活性 在包含EWS-FLI1的TC32细胞中,YK-4-279通过阻断EWS-FLI1与RHA的相互作用减少细胞周期素D的水平。YK-4-279也能特异性抑制ESFT细胞生长,并诱导细胞凋亡。[1] YK-4-279也会抑制融合阳性前列腺癌细胞中ERG 和 ETV1的生物活性,并进一步减少细胞运动和侵袭。[2]
实验图片 检测方法 检测指标 实验图片 PMID
Growth inhibition assay Cell viability 29212266
Western blot PARP / Cleaved PARP / Caspase 3 / Cleaved Caspase 3 p-HH3(Ser10) / Histone H3 / p-Aurora A (T288) / Aurora A / Aurora B / Cyclin B / p53 / p21 29212266
体内研究(In Vivo)
体内研究活性 在体内,YK-4-279 (1.5 mg/dose i.p.)抑制ESFT异种移植瘤的生长。[1]在小鼠模型中,YK-4-279选择性防止前列腺癌在融合阳性LNCaP-luc-M肿瘤中的生长和转移。[3]
动物实验 Animal Models 负荷前列腺癌 PC3,TC71 或 CHP-100 异种移植物的裸鼠
Dosages 1.5 mg/dose
Administration i.p.

化学信息&溶解度

分子量 366.20 分子式

C17H13Cl2NO4

CAS号 1037184-44-3 SDF Download YK-4-279 SDF
Smiles COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 73 mg/mL ( 199.34 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 73 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
I would like to know whether YK-4-279 is the racemate version, or whether it is the + R-enantiomer or the – S-enantiomer of the compound?

回答:
For our S7679 YK-4-279, it is a recemate.

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