YK-4-279
YK-4-279是EWS-FLI1与RNA helicase A (RHA)结合的有效抑制剂。
YK-4-279 Chemical Structure
CAS: 1037184-44-3
产品质控
批次：
纯度：
99.93%
99.93
YK-4-279相关产品
相关信号通路图
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-FLI1与RNA helicase A (RHA)结合的有效抑制剂。 | ||
|---|---|---|---|
| 靶点 |
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| 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) | |||
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体外溶解度 |
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 (199.34 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 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
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
只
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，注：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：取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：取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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